Distinguished Faculty

Anti-Inflammatories | Protein-Protein Interactions | Epigenetic Inhibitor Discovery 
Macrocyclics and Constrained Peptides | Fragment Based Drug Discovery | Kinase Inhibitor Chemistry
 

Anti-Inflammatories: Small Molecule Approaches (April 23-24) 

Lars Burgdorf, Ph.D., Principal Scientist, Medicinal Chemistry, Merck KGaA, Germany


Robert Carlson, Ph.D., Vice President, Preclinical Development and Product Leadership, Karyopharm Therapeutics

Robert Carlson, Ph.D. joined Karyopharm in September 2013 as Vice President, Preclinical Development, bringing with him over 20 years of drug discovery and development experience in a wide variety of therapeutic areas in both small and large companies. Just prior to Karyopharm, he was Vice President and Head of the Seattle site of JW Pharmaceuticals. From 2004 to 2012, he was Vice President and Head of Research in the Pharmaceutical Division of Myriad Genetics and the subsequent spinout Myrexis, which focused on cancer drug discovery and development. From 2001 to 2004, he was Director of Biology at Karo Bio, a Biotech company specializing in nuclear hormone receptor drug discovery. Prior to that, he spent a decade working in Big Pharma for Bayer and Hoechst-Roussel on cancer, inflammation and neurodegeneration drug discovery. Over his career, Robert has been responsible for advancing 11 compounds from discovery to development, including sorafenib as a member of the Discovery Project Team at Bayer. He earned a B.S. in Biochemistry from the University of Wisconsin-Madison, a Ph.D. in Biochemistry from Brandeis University and had postdoctoral training at the University of Michigan and Georgetown University.

Linda Casillas, Ph.D., Senior Scientific Investigator, Immuno-Inflammation Medicinal Chemistry, GlaxoSmithKline

Dr. Casillas is currently the co-leader of an immuno-inflammation kinase program leading a group of 20 medicinal chemists. With 15 years of medicinal chemistry experience at GSK, Dr. Casillas has worked on Hit to Lead and Lead Optimization programs in various target classes (kinase, GPCR, and ion channels) and has contributed to the discovery of multiple pre-clinical candidates. Prior to joining GSK, Dr. Casillas received her Ph.D. from Johns Hopkins University under the direction of Prof. Craig Townsend and a B.S. in chemistry from the University of Richmond.

Dan Dairaghi, Ph.D., Senior Director, Molecular Pharmacology and Biomarkers, ChemoCentyrx


Gerald Denis, Ph.D., Associate Professor, Cancer Center, Boston University School of Medicine

Dr. Gerald V. Denis is a molecular and cellular biologist, trained at the University of California, Berkeley. Dr Denis originated the field of mammalian BET protein function. Building on the knowledge base of BET protein mechanisms in Drosophila homeosis, he was the first to show that constitutive expression of a BET protein in mice is oncogenic. He also serendipitously discovered that reduced whole-body expression of the BET protein Brd2 in mice produces a hypomorphic animal model for ‘metabolically healthy’ obesity; a low-inflammatory profile contributes to protection of these mice from glucose intolerance. BET protein studies received tremendous new attention with 2010 reports that small molecule inhibitors of bromodomain proteins have anti-cancer properties. Chromatin interactions had not been thought previously to be ‘druggable’ targets.

These observations underpin a new hypothesis that reduced inflammation protects against obesity-associated cancers, in part through BET protein co-regulation of transcriptional networks, potentially opening a new avenue in cancer chemoprevention. Dr Denis is Associate Professor of Medicine and Pharmacology at Boston University School of Medicine, and immediate past Chair of the Basic Science Section of the Obesity Society.

Aleksey Kazantsev, Ph.D., Associate Professor, Neurology, Harvard Medical School and Massachusetts General Hospital


Alec Lebsack, Ph.D., Associate Scientific Director, Immunology Chemistry, Janssen Research & Development

Dr. Alec Lebsack obtained a B.S. in Biochemistry and Molecular Biology at the University of California, Santa Cruz and a Ph.D. in Organic Chemistry from the University of California, Irvine under the direction of Professor Larry E. Overman. His doctorate work resulted in the completion of several enantioselective total syntheses including rearranged spongian diterpene Shahamin K and polypyrrolidinoindoline alkaloids Quadrigemine C and Psycholeine. In 2002, Alec joined Merck & Co., Inc. in San Diego where he contributed to several programs including VLA-4 antagonists and high-affinity ligands to the 2-1 subunit of voltage gated calcium channels. Since joining Janssen in 2005, he has supported and led medicinal chemistry programs from project concept to selection of early development candidates on ion-channel, G-protein coupled receptor, and protein-protein interaction targets within the Pain and Immunology therapeutic areas. Alec’s work has resulted in 19 peer reviewed papers and patents.

David Y. Liu, Ph.D., CSO, Protagonist Therapeutics, Inc.

David Y. Liu joined Protagonist in 2013 as their Chief Scientific Officer and was most recently Chief Operating Officer and co-founder of Trenovus, Inc., as well as a strategic advisor to several other biotechnology companies. Prior to that he spent more than seven years at FibroGen, Inc. as Vice President with leadership responsibility for all therapeutic research and drug discovery, including interim leadership of the Clinical Development department. Prior to that, he spent 10 years as Director of Inflammation Research at Scios, Inc., now part of Johnson & Johnson. Dr. Liu’s biotech career began with Cetus Corporation (since acquired by Chiron and now Novartis) and COR Therapeutics (since acquired by Millenium/Takeda). Before joining the biotech industry he spent 10 years as an academic researcher at the Brigham and Women’s Hospital, Harvard Medical School and was Instructor and Assistant Professor in the Department of Medicine, Harvard Medical School. He completed his PhD in Microbiology and Immunology at Michigan State University after receiving a BS in chemistry at the University of Chicago.

Dustin McMinn, Ph.D., Associate Director, Medicinal Chemistry, Onyx Pharmaceuticals


Christel Menet, Ph.D., Senior Lead, Project Director, Autoimmune Disease, Galapagos

Dr. Christel Menet joined Galapagos in 2005, and over the past 8 yrs has taken on roles of increasing leadership and responsibility. Prior to Galapagos, she worked at Faust Pharmaceutical (French Biotech) and Evotec (UK) developing GLPG0555 – Phase 1; GLPG0778 – Jak1 selective, Phase II; GLPG0634 – Jak1, with positive results in Phase IIb; and others in preclinical development.

Kamal Puri, Ph.D., Associate Director, Research, Gilead Sciences, Inc.

Dr. Kamal D. Puri has more than 15 years of research and development experience in immunology, oncology vascular biology, and neurobiology. Dr. Puri is serving as Associate Director in the Research department at Gilead Sciences Inc. He was previously Head of Biology Research at Calistoga Pharmaceuticals in Seattle, USAand Senior Scientist and Biology Team Leader at ICOS Corporation, where he led several drug development projects focused on generating small molecule inhibitors appropriate for INDenabling studies and clinical trials. His work led to identification of several Drug Development Candidates, and several of which are currently being evaluated in clinical studies. Prior to joining ICOS, Dr. Puri held roles at CytoTherapeutics, Inc. Dr. Puri was awarded a doctorate in Molecular Biophysics from the Indian Institute of Science, Bangalore, India. He undertook his postdoctoral training at Harvard MedicalSchool in the laboratory of Dr. Timothy Springer.

Laura Silvian, Ph.D., Principal Scientist, Physical Biochemistry, Biogen Idec

Dr. Laura Silvian is a Principal Scientist and Head of the Physical Biochemistry group Drug Discovery at Biogen Idec in Cambridge, MA. She has been engaged in small molecule and biologics drug discovery for > 13 years. She conducted post-doctoral work in structural biology in the Ellenberger lab at Harvard Medical School. Prior to that she carried out PhD studies in crystallography with Tom Steitz in the Molecular Biophysics and Biochemistry department at Yale University. She has written several manuscripts and reviews on inhibitors of protein-protein interactions.

Paul R. Thompson, Ph.D., Associate Professor, Department of Chemistry, TSRI, Scripps Florida

Dr. Paul Thompson is an Associate Professor in the Department of Chemistry at The Scripps Research Institute, where his research focuses on the development of novel therapeutics for a range of diseases including cancer, rheumatoid arthritis, inflammatory bowel disease, and lupus. Paul received his BSc and PhD degrees from McMaster University in Canada before moving to the US to take a postdoctoral position with Philip Cole at the Johns Hopkins School of Medicine. Paul then moved to the University of South Carolina to begin his independent career before moving to Scripps Florida in May 2010. Paul has published more than 80 articles in major scientific journals including Nature, Cell, Nature Structural and Molecular Biology, and the Journal of the American Chemical Society. Paul has won a number of awards including a Canadian Institutes of Health Research Postdoctoral Fellowship and a Camille Dreyfus Teacher-Scholar Award.

Wendy Young, Ph.D., Director, Discovery Chemistry, Genentech

Wendy B. Young has nineteen years of industrial drug discovery experience, having led discovery efforts at both small biotech firms (Axys/Celera and Scios: 1995-2006) and larger companies (Genentech/Roche: 2006-present). Wendy is currently Director of Medicinal Chemistry at Genentech, where she is a leader of project teams and directs a large group of medicinal chemists. These teams have produced multiple clinical candidates, from a variety of target classes, currently under clinical evaluation in a range of indications. She was recently elected as Vice Chair of the ACS Medicinal Chemistry (ACS MEDI) Division which will culminate in her being Chair of the Division in 2017. Wendy received her Ph.D. from Princeton University under the direction of E.C. Taylor and carried out Postdoctoral Studies at Memorial Sloan Kettering Cancer Center with Professor Samuel Danishefsky. Wendy is listed as an inventor or author on over 65 patent and research publications and has given presentations at many national and international meetings.

 

Protein-Protein Interactions (April 23-24) 

Kate Ashton, Ph.D., Senior Scientist, Medicinal Chemistry, Amgen, Inc.

Dr. Kate Ashton received a Masters in Chemistry with Industrial Experience from the University of Edinburgh. She conducted her PhD thesis research on the synthesis and structure elucidation of Reidispongiolide A with Prof. Ian Paterson at the University of Cambridge, and her postdoctoral work on SOMO catalysis with Prof. David W. C. MacMillan at both Caltech and Princeton. She has been at Amgen for 6 years and has worked on indications for cancer, Alzheimer’s and diabetes.Dr Fecke works in the area of industrial early drug discovery since 1996. He is currently Group Leader in the Primary Pharmacology department at UCB Pharma (UK) and is involved in the identification and characterization of NCE and NBE drugs in molecular interaction assays for both immunological and CNS diseases. Prior to joining UCB, he worked for Novartis and Siena Biotech in the areas of transplant rejection, neurodegeneration and oncology. He obtained his PhD at the Heinrich-Heine-University Dusseldorf in Germany in 1994.

Julio Camarero, Ph.D., Associate Professor, Pharmacology and Pharmaceutical Sciences & Chemistry, University of Southern California

Professor Camarero started his studies in chemistry at the University if Barcelona (Spain), received his Master degree in 1992, and finished his PhD thesis there in 1996. Afterwards he joined the group of Professor Tom W. Muir at The Rockefeller University as a Burroughs Wellcome Fellow where he contributed to the development of new chemoselective ligation techniques for the chemical engineering of proteins. In 2000, he moved to the Lawrence Livermore National Laboratory as a Distinguished Lawrence Fellow where he became staff scientist and head of laboratory in 2003. He finally joined the University of Southern California in 2007 as an associate professor. His current research interests are focused in the development of new bioorganic approaches using protein splicing and synthetic protein chemistry for studying biological processes involved in bacterial pathogenicity and how can be modulated or inhibited by small molecules. Professor Camarero has authored over 70 peer-reviewed publications and four invited book chapters.

Kurt Deshayes, Ph.D., Senior Scientist, Early Discovery Biochemistry, Genentech


José Duca, Ph.D., Head, CADD Cambridge, Novartis Institutes for BioMedical Research, Inc.

Dr. José Duca is Head of Computer Aided Drug Discovery (CADD) in Cambridge, Novartis Institutes for BioMedical Research (NIBR). José joined Novartis in 2010. Previously he had been with the Schering-Plough Research Institute and Merck Research Laboratories in Kenilworth, NJ, USA for 10 years where he had increasing responsibilities in the CADD group. His scientific fields of expertise within computational chemistry include – but are not limited to – molecular modeling, ab initio calculations, molecular recognition, QM-MM methods and structure-based drug design. He received his Ph.D. in Chemistry from the National University of Córdoba, Argentina. He joined Prof. Tony Hopfinger’s group in the College of Pharmacy at the University of Illinois at Chicago as a Postdoctoral Fellow.

Lee D. Fader, Ph.D., Principal Scientist, Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc.

Dr. Lee Fader obtained his B.Sc. in chemistry from Concordia University. Following his undergraduate studies, he moved to McGill University to pursue his PhD Degree under the supervision of Dr. Youla Tsantrizos.  He then moved to the Swiss Federal Institute of Technology as an NSERC Postdoctoral fellow with Professor Erick Carreira. In 2004, he joined Boehringer Ingelheim (Canada) Ltd. in the medicinal chemistry department where his focus was on the discovery of small molecule antiviral agents. In 2013, Dr. Fader joined the department of medicinal chemistry at Boehringer Ingelheim Pharmaceuticals, Inc. as Lab Leader and Principal Scientist where his focus is on small molecule drug discovery in the areas of immunology and cardiometabolic disorders.
 

Wolfgang Fecke, Ph.D., Group Leader, Primary Pharmacology, UCB Pharma

Dr Fecke works in the area of industrial early drug discovery since 1996. He is currently Group Leader in the Primary Pharmacology department at UCB Pharma (UK) and is involved in the identification and characterization of NCE and NBE drugs in molecular interaction assays for both immunological and CNS diseases. Prior to joining UCB, he worked for Novartis and Siena Biotech in the areas of transplant rejection, neurodegeneration and oncology. He obtained his PhD at the Heinrich-Heine-University Dusseldorf in Germany in 1994.

Maria Gaczynska, Ph.D., Associate Professor, Molecular Medicine, University of Texas Health Science Center at San Antonio

Dr. Maria Gaczynska’s expertise spans areas as diverse as cell biology, protein biochemistry, biophysics and single-molecule imaging. She has more than 20 years of experience with biochemistry, cell biology and structural biology of the proteasome. She worked as a postdoctoral fellow in the laboratory of one of founding fathers of the ubiquitin-proteasome field, Dr. A.L. Goldberg (Harvard Medical School). In the laboratories of Drs. Goldberg and Ploegh (MIT Center for Cancer Research) Dr. Gaczynska played a major role in the discovery of immunoproteasomes and subsequent characterization of their first specific inhibitors. As an independent investigator, together with Dr. Osmulski, she has taken on the vast and novel field of allosteric regulation of the proteasome. Her laboratory laid the groundwork for the use of atomic force microscopy (AFM) to probe interaction of the proteasome with regulatory proteins, molecular dynamics of the proteasome and its response to drugs. The lab is vigorously pursuing development of small-molecule allosteric regulators of the proteasome with anti-cancer and anti-inflammatory properties. In addition to studying the proteasome, the lab’s AFM studies are also applied to studying amyloid and serpin polymers, DNA-protein complexes, membrane channels and whole cells, most notably circulating tumor cells.

Jason E. Gestwicki, Ph.D., Associate Professor, Department of Pharmaceutical Chemistry, University of California, San Francisco


Rhian Holvey, Ph.D., Postdoc, Department of Chemistry, University of Cambridge

Rhian Holvey is currently doing a postdoc at Cambridge University following up on the PhD project she designed as part of the Cambridge PhD Training Programme in Chemical Biology and Molecular Medicine with Professor Chris Abell, Dr. Murray Stewart and Professor David Neal. Her thesis, on fragment-based design of inhibitors of the TPX2 - importin-α interaction as a novel anti-cancer target, was submitted in January 2014. She obtained an MChem degree from the University of Oxford where her final year project was synthesizing novel inhibitors of LDH-A as potential anti-cancer drugs with Dr. Angela Russell.

Roderick Hubbard, Ph.D., Senior Fellow, Research & Development, Vernalis; Professor, University of York

Dr. Rod Hubbard has been working with methods for analysis and exploitation of protein structure for over 30 years. In the 1980s, he developed molecular modelling methods; in the 1990s he helped build the Structural Biology Lab at the University of York. Since 2001, he has spent varying amounts of his time with Vernalis, establishing and applying structure and fragment-based methods for drug discovery.

Aleksey Kazantsev, Ph.D., Associate Professor, Neurology, Harvard Medical School and Massachusetts General Hospital


Anthony D. Keefe, Ph.D., Senior Director, Lead Discovery, X-Chem Inc.

Anthony Keefe has worked with DNA-Encoded combinatorial libraries and their affinity-based selection since 1997.  Since 2010 he has held the position of Senior Director of Lead Discovery at X-Chem Inc. in Waltham, Massachusetts.  At X-Chem he runs the group that is responsible for the discovery of drug-like small-molecules that inhibit proteins of therapeutic interest using the affinity-mediated selection of DNA-encoded chemically-generated libraries.  From 2001-2009 he worked forArchemix Corporation in Cambridge, Massachusetts with aptamers - protein-binding oligonucleotides that are discovered in large libraries of stochastically-generated oligonucleotides using affinity-based selection.  From 1997-2001 he worked in the lab of 2009 Nobel Laureate Jack Szostak at Harvard Medical School/Massachusetts General Hospital developing and using mRNA Display – a technology in which large libraries of stochastically-generated DNA-encoded proteins may be interrogated for the functional entities they contain. Anthony received a PhD in Chemistry from the University of Birmingham, UK, in 1989 and a BSc. in Chemistry from Exeter University, UK, in 1985.

Roman Kombarov, Ph.D., Project Manager, ASINEX

Roman Kombarov studied organic and medicinal chemistry at Moscow State University and received his PhD in bioorganic chemistry in the group of Prof. Yurovskaya. In 2000 he joined ASINEX, a company focusing on small-molecule compound libraries, as a group leader. Dr. Kombarov has extensive project leadership experience in international drug discovery programs having participated in the completion of hit-to lead projects in oncology, CNS and anti-infectives. His current role includes coordination of multiple lead generation projects and the development of innovative strategies for compound library design.

Elmar Nurmemmedov, Ph.D., Scientist, Molecular Experimental Medicine, The Scripps Research Institute

Dr. Elmar Nurmemmedov holds BSc in biology from Middle East Tech University, Turkey. He holds PhD in molecular biophysics from Lund University, Sweden. Currently Elmar is affiliated both to Scripps Research Institute and Harvard Medical School. Elmar is involved as a scientist in drug discovery in the field of oncology.

Laura Silvian, Ph.D., Principal Scientist, Physical Biochemistry, Biogen Idec

Dr. Laura Silvian is a Principal Scientist and Head of the Physical Biochemistry group Drug Discovery at Biogen Idec in Cambridge, MA. She has been engaged in small molecule and biologics drug discovery for > 13 years. She conducted post-doctoral work in structural biology in the Ellenberger lab at Harvard Medical School. Prior to that she carried out PhD studies in crystallography with Tom Steitz in Molecular Biophysics and Biochemistry department at Yale University. She has written several manuscripts and reviews on inhibitors of protein-protein interactions.

Daqing Sun, Ph.D., Principal Scientist, Medicinal Chemistry, Amgen

Dr. Daqin Sun received a Ph.D. at University of Alberta with Professor Hsing-Jang Liu where Dr. Sun discovered a Lewis acid-mediated polyene cyclization process of β–keto ester and successfully applied the new methodology in the total synthesis of two natural products. He conducted postdoctoral research at University of California, Los Angeles (UCLA) with Michael Jung on development of new methods for the total synthesis of the very cytotoxic natural products, tedanolide and 13-deoxytedanolide. In 2001 Dr. Sun went on to work at Tularik Inc. as a scientist in Department of Medicinal Chemistry and achieved the title of senior scientist in 2004. He was promoted to the position of principal scientist/group leader at Amgen, Inc. in 2010. During 13 years with Tularik/Amgen, Dr. Sun worked on three small molecule projects, IRAK4 inhibitor (inflammation), 11β-HSD1 inhibitor (metabolic disease), and p53-MDM2 inhibitor (oncology). He led the teams to discovered three clinical candidates, AMG 456 (11β-HSD1 inhibitor), AMG 232 and AM-7209 (p53-MDM2 inhibitors). AMG 232 is currently in the clinic trials for the treatment of cancer.

Mohammed Yousef, Ph.D., Senior Field Application Scientist, Bio-Rad Laboratories 
Dr. Yousef is a senior Field Application Scientist at Bio-Rad. Dr. Yousef has a Ph.D. in Chemical Engineering from the University Iowa .  He has more than 14 years experience in bio-molecules characterization and interactions using various biophysical techniques especially surface plasmon resonance (SPR).  Before joining Bio-Rad, Dr. Yousef did his postgraduate training at Argonne National Laboratory and was the technical director of the Biophysics Core Facility at the University of Chicago.

 

Epigenetic Inhibitor Discovery (April 23-24) 

Brian Albrecht, Ph.D., Senior Director, Medicinal Chemistry, Constellation Pharmaceuticals

Brian is currently the Senior Director of Medicinal Chemistry at Constellation Pharmaceuticals. He joined Constellation as one of its first scientists in 2008 and has run the medicinal chemistry department since. Brian has been instrumental in the discovery and development of CPI-0610, Constellation’s clinical BET bromodomain inhibitor currently in Phase I for lymphoma. Prior to Constellation, Brian held several positions at Amgen working in the oncology and neuroscience therapeutic areas. He received his BA in chemistry from Lafayette College in Easton, PA and completed his graduate work at Colorado State University.

Paul Bonin, Principal Scientist, Assay Development and Pharmacology, Primary Pharmacology Group, Pfizer, Inc.

Dr. Bonin began his career as a “drug hunter” working with the former Upjohn Company in Kalamazoo, MI. Dr. Bonin has over 25 years of experience developing unique cellular and biochemical assays to support the identification of novel chemical entities for various disease areas. Currently he is part of Pfizer’s Primary Pharmacology and Assay Development Group (PPG) in Groton, CT.

Stuart Conway, Ph.D., Associate Professor, Chemistry, University of Oxford

Stuart Conway is a Lecturer (Associate Professor) in Chemistry at the University of Oxford and the Fellow in Organic Chemistry at St Hugh’s College, Oxford. He studied Chemistry with Medicinal Chemistry at the University of Warwick before undertaking Ph .D. studies with Prof. David Jane in the Department of Pharmacology at the University of Bristol. Stuart completed post-doctoral studies with Prof. Andrew Holmes FRS at the University of Cambridge working on the synthesis of inositol polyphosphates. In 2003, he was appointed as a Lecturer in Bioorganic Chemistry at the University of St. Andrews and in 2008 he took up his current position. Between March and August 2013 Stuart was a Visiting Associate at the California Institute of Technology, hosted by Prof. Bob Grubbs and Prof. Dianne Newman.

Helena Danielson, Ph.D., Professor, Biochemistry, Uppsala University; CSO, R&D, Beactica

Helena Danielson is Professor of Biochemistry at Uppsala University in Sweden since 2002 and Chief Scientific Officer of Beactica AB. She is a specialist in enzyme-based drug discovery and molecular recognition. Her education includes a Master of Science in Chemical Engineering at Lund University in 1982 and, as a Fulbright scholar, a Master of Science in Biochemistry, University of Rochester, Rochester, NY, USA in 1984, and a Ph. D. in Biochemistry at Stockholm University in 1987. As a post-doc at Karolinska Institutet in Stockholm, Helena started a research project on HIV protease as a drug target for AIDS, and has since expanded her research to other enzymes and diseases, more recently also with an interest in membrane receptors and neurological drug targets. Helena has focused on developing enzymology for drug discovery, and in particular biomolecular interaction analysis for detailed studies of enzyme-inhibitor interactions and other important recognition processes in the life science area. Helena Danielson co-founded Beactica AB in 2006. The company is a specialist drug discovery company that generates novel drug leads from low molecular weight fragments by integrating biomolecular interaction analysis with in silico molecular docking techniques.

Matthew Fuchter, Ph.D., Senior Lecturer, Synthetic and Medicinal Chemistry, Department of Chemistry, Imperial College London

Matthew Fuchter is a Senior Lecturer in Synthetic and Medicinal Chemistry at Imperial College London. He is Co-Director of an Imperial College MRes course in drug discovery, a Research Board member of the Institute of Chemical Biology and a Managerial Board member for an anti-cancer drug discovery group, CD3. His multidisciplinary research group use expertise in chemical synthesis to impact molecular science in chemistry, materials and medicine. A central theme within this framework is the design and development of small molecule tools to study epigenetic processes mis-regulated in disease, and their subsequent translational use in novel therapeutic strategies.

Stefan Günther, Ph.D., Professor, Institute of Pharmaceutical Sciences, Pharmaceutical Bioinformatics, University of Freiburg

Dr. Guenther received his Diploma in Biology from the Christian-Albrechts-University in 2001; his Master of Computer Science from the University of Applied Science in 2004; and his Dr. rer. nat. from the Fee University in Berlin and the Charité - University Medicine in 2008. His positions include a postdoctoral fellowships with Dr. R. Preissner at the Charité - University Medicine and with Prof. Dr. E. Klipp, at the Humboldt-University. In 2009, Dr. Guenther accepted the position of Junior Professor of Pharmaceutical Bioinformatics at the University of Freiburg, Germany.

Edward Holson, Ph.D., Director, Medicinal Chemistry, Stanley Center for Psychiatric Research, The Broad Institute of MIT and Harvard

Ed Holson is the Director of the Medicinal Chemistry group in the Stanley Center for Psychiatric Research and a Director of Chemistry in the Chemical Biology Platform at the Broad Institute. In February 2008, Holson joined the medicinal chemistry group at the Stanley Center to design and implement strategies toward developing novel therapies in central nervous system related disorders including schizophrenia, bipolar disorder, and cognitive impairment. These strategies include the rational design and development of novel, potent and highly selective small molecules suitable for clinical development. His group is interested in a range of biology including epigenetics, G-protein coupled receptors, kinases, and protein-protein interactions. Prior to joining the Stanley Center, Holson worked for Infinity Pharmaceuticals and Merck & Co. in a variety of roles in medicinal chemistry and pharmaceutical development.

Jian Jin, Ph.D., Associate Professor and Director, Medicinal Chemistry, Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill

Dr. Jin is an Associate Professor in the Division of Chemical Biology and Medicinal Chemistry and Department of Pharmacology, an Associate Director of Medicinal Chemistry in the Center for Integrative Chemical Biology & Drug Discovery, and a Member of Lineberger Comprehensive Cancer Center at the University of North Carolina - Chapel Hill (UNC-CH). His current research interests include discovering chemical probes for histone methyltransferases and functionally selective GPCR ligands. Prior to joining UNC-CH in 2008, Dr. Jin had >10 years of drug discovery experience at GlaxoSmithKline, where he had most recently served as a Manager of Medicinal Chemistry from 2003 to 2008. Dr. Jin has published 76 peer-reviewed papers and is an inventor of 9 issued U.S. patents and 38 PCT patent applications.

Elisabeth Martinez, Ph.D., Assistant Professor, Pharmacology, University of Texas Southwestern Medical Center

Dr. Elisabeth Martinez is an Assistant Professor in the Department of Pharmacology and the Hamon Center for Therapeutic Oncology Research at UT Southwestern Medical Center. Her group's main interests include transcriptional and epigenetic regulation of gene expression in cancer and discovering new small molecules to modulate this process. Her publications in this area include several papers on the establishment and use of a cell-based system for epigenetic drug screens and the characterization of HDAC inhibitors as well as more recent studies on Jumonji demethylase inhibitors.

Susanne Muller-Knapp, Ph.D., Epigenetic Project Manager, Structural Genomics Consortium (SGC), Oxford

Susanne Müller-Knapp studied Human Biology in Marburg Germany followed by a Ph.D. in molecular biology at the Karolinska Institute in Stockholm, Sweden (1997). She then had more than 6 years of postdoctoral training in the area of inflammation and gene regulation in Stockholm and at the DIBIT San Raffaele Scientific Institute in Milan, Italy. In 2004 Susanne joined the Structural Genomics Consortium, SGC, in Oxford. The SGC is an international public private partnership that comprises 8 international pharmaceutical companies and a large network of academic and industrial collaborators. Susanne worked at the SGC first as External Research Manager and then Scientific Coordinator. Currently, she is the Project Manager of the Epigenetic Probe Project, which aims to create tool compounds with defined specificity and selectivity for epigenetic targets. She also heads the cell based assay group at the SGC establishing assays to test the cell activity of the identified inhibitors.

Zaneta Nikolovska-Coleska, Ph.D., Assistant Professor, Pathology, Medical School, University of Michigan

Dr. Nikolovska-Coleska received her B.S. in Pharmacy from University Ss. Cyril and Methodius, Skopje, Republic of Macedonia and her M.S. and Ph.D. in Pharmaceutical Chemistry from the same University. Dr. Nikolovska-Coleska did her postdoctoral training in drug discovery at the University of Michigan with Professor Shaomeng Wang. Dr. Nikolovska-Coleska joined the Department of Pathology, Medical School, University of Michigan in 2008 where she is also affiliated with the Interdepartmental Program in Medicinal Chemistry as well as with the Chemical Biology Program. Dr. Nikolovska-Coleska serves as a Director of the Molecular Cell Pathology Graduate Program. Her research interest is focused on development small-molecule modulators of protein-protein interactions involved in programmed cell death and epigenetic modifications.

Jun Qi, Ph.D., Senior Research Scientist, Medical Oncology, Dana-Farber Cancer Institute

Jun Qi, Ph. D. is a Senior Research Scientist in the Medical Oncology Department at Dana-Farber Cancer Institute, and is leading the synthetic chemistry effort in Dr. James Bradner’s laboratory. Dr. Qi received his BS in Chemistry from Fudan University in China, and MS degree from Wayne State University. He then obtained his Ph.D. in Chemistry from University of Michigan with William Roush, and completed his postdoctoral training at Massachusetts Institute of Technology. Since his joining in Dr. Bradner’s lab in 2009, Dr. Qi’s study has been focusing on design and synthesis the small molecule inhibitors targeting gene regulation pathways for cancer therapy. His recent discovery of the small molecule inhibitor of bromodomains, JQ1, has been utilized to understanding the fundamental roles of epigenetic reader proteins, and has been studied by more than two hundred research groups worldwide. Dr. Qi has contributed to the Bradner group’s recent publications in Nature and Cell. His recent work has generated a large impact on targeting epigenetic proteins for cancer therapy. He has also been invited to review manuscripts for several journals, such as Journal of the American Chemical Society.

Gregg Siegal, Ph.D., CEO, ZoBio

Gregg Siegal obtained his Ph.D. on studies of eukaryotic DNA replication at the University of Rochester in the USA under the supervision of Professor Robert Bambara. Subsequently he post-Doc’ed in the laboratories of Professor Kurt Wüthrich at the ETH in Switzerland and Professor Paul Driscoll at the Ludwig Institute of Cancer Research in the UK. It was during his post-Doctoral work that Dr. Siegal was exposed to NMR as a tool for both structural biology and drug discovery. He moved to Leiden University in 1997 where he received a Dutch Royal Society Fellowship to form his own research group. His current research interests focus on the development and application of innovative drug discovery technologies. In 2004 he spun out the company ZoBio to commercialize the TINS ligand screening technology developed in his group and presently serves as the Chief Executive Officer in addition to his position within the University. ZoBio has been profitable from its inception and currently employs eleven scientists.

Takayoshi Suzuki, Ph.D., Professor, Graduate School of Medical Science, Kyoto Prefectural University of Medicine

Takayoshi Suzuki received his B.Sc. and M.Sc. from the University of Tokyo (1995 and 1997, respectively), then became a Researcher at Japan Tobacco Inc. from 1997–2002. He subsequently joined the Graduate School of Pharmaceutical Sciences, Nagoya City University, as an assistant professor (2003–2009) and lecturer (2009–2011). During that time, he received his Ph.D. from the Graduate School of Pharmaceutical Sciences, the University of Tokyo. He spent one year as a visiting investigator at The Scripps Research Institute, California (2007–2008). He has worked as a full professor at the Graduate School of Medical Science, Kyoto Prefectural University of Medicine (2011 to present).

Xiang Wang, Ph.D., Assistant Professor, Chemistry and Biochemistry, University of Colorado at Boulder

 

Macrocyclics and Constrained Peptides (April 24-25) 

Prabhat Arya, Ph.D., Professor, Chemistry and Chemical Biology, DRILS University of Hyderabad, India

Dr. Prabhat Arya’s group, for almost two decades, has been focused on exploring novel chemical space by building a toolbox of compounds that are more close to bioactive natural products. They develop methods to build macrocyclic diversity because macrocyclic natural products have an excellent track record as modulators of the broad pathway arenas of oncology and other disease areas. The team has written several leading research review articles (i.e. Chem. Rev., Curr. Opin. Chem. Biol.; Chem. Biol.; Chem. & Eng. News; etc.) on the need to strengthen the advanced organic chemistry efforts to producing next generation small molecules for undertaking biological targets that are related to PPI and BMI. Over the years, Dr. Arya has trained more than 50 post doctoral fellows, several graduate and undergraduate students on this topic and delivered ~125 lectures at various scientific meetings and research institutions. He served on various NIH and CIHR and NCIC (Canada) grant panels and worked in the committees that were assigned the task of establishing large scale chemical biology research programs within US and Canada. Prior to making an adventurous move to India in July 2009, he was a Research Officer at the National Research Council of Canada for nearly 20 years and also had Adjunct Professorships at Biochemistry, McGill University, Chemistry and Biochemistry, University of Ottawa, Ottawa Health Research Institute (OHRI).

Adrian Culf, Ph.D., Research Scientist, Medicinal Chemistry, Atlantic Cancer Research Institute

Dr. Adrian Culf has a Ph.D. in bio-organic chemistry from the University of Surrey, UK (John Jones (Surrey) and Bill Lockley (Astra Zeneca)) in the area of small molecule-large molecule interactions. Post-doctoral fellowship at UCSB (John Gerig) working on carbonic anhydrase and PLA2 inhibitors. 20 years work experience in medicinal chemistry. Presently at the Atlantic Cancer Research Institute in Moncton, Canada. Research interests include synthesis of bio-active small molecules, diagnostic imaging and peptide mimics for studying protein-protein interactions.

Max Cummings, Ph.D., Principal Scientist, Discovery Sciences, Janssen

Dr. Max Cummings is a Computational Chemist at Janssen R&D, working on drug discovery in various therapeutic areas. He earned his Ph.D. in Biochemistry under the supervision of Randy J. Read at the University of Alberta. Dr. Cummings worked in medicinal chemistry and enzymology at SynPhar (now NAEJA), Edmonton, Canada, from 1988-1996, and in the computational chemistry group at SmithKline Beecham (now GSK), King of Prussia, USA, from 1997-2000. In 2000 he joined the computational chemistry group at 3-Dimensional Pharmaceuticals, Exton, USA, which later become part of J&J PRD. In 2007 he moved to Tibotec BVBA, a J&J company, in Mechelen, Belgium, and in 2011 returned to the Janssen R&D site in Spring House, USA. Dr. Cummings has contributed to several discovery projects that have delivered one or more compounds to clinical evaluation, including the HCV compounds Simeprevir and TMC055.

Dmitry Genis, Ph.D., CEO, ASINEX

Dr. Dmitry Genis graduated from Moscow State University in 1993 and obtained a PhD in 1997. In 1994, Dr. Genis was one of the founders of ASINEX and held the position of Research Director until 2001 when he became the CEO. Dr. Genis has successfully guided ASINEX from being a start-up company of 3 employees to becoming a well-recognized name in the drug discovery sector, currently employing 200 staff.


Danielle Guarracino, Ph.D., Assistant Professor, Chemistry, The College of New Jersey

Dr. Danielle Guarracino received her B.A. in Chemistry and Biological Sciences with a concentration in Biochemistry in 2002 from Cornell University. She then pursued graduate studies at Yale University where she received an M.S. in 2004 and a Ph.D. in Bioorganic Chemistry in 2008. While at Yale she worked for Professor Alanna Schepartz on a Chemical Biology project involving optimization of beta-peptide foldamer structure and function with applications towards the novel viral target, Severe Acute Respiratory Syndrome. From there, Dr. Guarracino performed post-doctoral research with Professor Paramjit Arora at New York University from 2008-2010, working on oligooxopiperazines as alpha-helical mimetics. From 2010 to the present, Dr. Guarracino has been a tenure-track Assistant Professor at The College of New Jersey, where she has taught undergraduate classes in General Chemistry, Organic Chemistry, Biochemistry, and upper-level Chemical Biology. Her research focuses on using macrocyclic peptides as first generation therapeutics to probe hormone-receptor interactions.

Vincent Guerlavais, Ph.D., Distinguished Scientist, Aileron Therapeutics

Dr. Vincent Guerlavais joined Aileron Therapeutics as Principal Scientist in 2008 and has focused his research on developing new stapling chemistries and designing bioactive cell-permeable stapled peptides. His work has supported both Aileron’s R&D pipeline and collaboration with Roche which has successfully advanced the preclinical development of a novel class of dual MDM2/MDMX inhibitors. Prior to Aileron, Dr. Guerlavais began his career at Medarex (now a wholly-owned subsidiary of Bristol Myers Squibb) where he designed ultra-potent cytotoxic prodrugs chemically linked with fully human antibodies. His work contributed to the development of the company's first Antibody-Drug Conjugate (ADC) clinical candidate MDX-1203. Dr. Guerlavais earned his Ph.D. in organic chemistry from the University of Montpellier under the supervision of Professor Jean Martinez. His thesis research led to the discovery of a potent ghrelin agonist AEZS-130 (Macimorelin, SolorelTM) which is currently being developed by Aeterna Zentaris for treating cancer cachexia (phase II) and as a diagnostic test for Adult Growth Hormone Deficiency (NDA filing). Dr. Guerlavais received a B.S. in chemistry from the University of Versailles in 1996.

ChiChi Huang, Ph.D., Scientific Director, Antibody Drug Discovery, Janssen R&D, LLC

Dr. Chichi Huang is a protein chemist with industrial experience in the design and engineering of protein therapeutics. He received his Ph.D. in Biochemistry from Tufts University Sackler School of Graduate Biomedical Sciences, Boston, MA. He completed his post-doctoral training in Dr. Timothy Springer’s Lab at Harvard Medical School, for studying the structure and function of beta2 integrins. Chichi Huang spent more than five years in the Pfizer Global Research Center at Groton, Connecticut, working on vaccine design and development. Since joined Centocor, Johnson and Johnson in 2002, he has been working on several antibody and peptide therapeutic projects and some of them are or will be in clinical trials.

Scott Lokey, Ph.D., Professor, Department of Chemistry and Biochemistry, University of California, Santa Cruz

Dr. Scott Lokey conducted his PhD at 
the University of Texas Austin, working with Dr Brent Iverson on the synthesis 
of artificial peptides designed to fold 
into unusual structures and interact with DNA. He then moved to the Institute of Chemistry and Cell Biology at Harvard Medical School, where he worked under the direction of Dr. Timothy Mitchison to develop cyclic peptide libraries for input into cell biological assays. He is currently Professor in the Department of Chemistry and Biochemistry at UCSC and Director of the UCSC Chemical Screening Center. His research focuses on the synthesis of natural product-inspired macrocycles and the study of their ability to diffuse across biological membranes.

Mark Peterson, Ph.D., Vice President, IP & Operations, R&D, Tranzyme Pharma, Inc.

Dr. Mark Peterson was Vice President, IP & Operations at Tranzyme Pharma from 2003 until it was acquired by Ocera Pharmaceuticals in 2013. He was previously with Monsanto and Advanced ChemTech, where he worked in a wide variety of research areas including structure-based design, solid phase organic chemistry, combinatorial libraries, synthesis automation, heterocycles, unnatural amino acids, peptides and peptidomimetics. With Tranzyme Pharma since 1999, Dr. Peterson led the chemistry R & D efforts during the technology development stage of the company and the initiation of its drug discovery programs before assuming his present position in 2003. A native of Wisconsin, he received his Ph.D. in Organic Chemistry from Washington State University and conducted post-doctoral research at the University of Minnesota prior to starting his industrial career. He is author or co-author of over80 publications and abstracted presentations plus two book chapters, as well as co-inventor on over 20 patents.

Anders Poulsen, Ph.D., Senior Research Scientist, Experimental Therapeutics Centre, A*STAR

Dr. Anders Poulsen is a senior scientist at The Experimental Therapeutics Centre in Singapore. He has a M.Sc. degree in applied chemistry from The Technical University of Denmark and a Ph.D. in medicinal chemistry from The University of Copenhagen. He has 15 years working experience as a computational chemist in pharma and biotech industry. Dr. Poulsen is the author of 25 papers and 10 patent applications and co-inventor of several clinical candidates.

Gloria Serra, Ph.D., Professor, Medicinal Chemistry, Organic Chemistry, Facultad de Química, Universidad de la República

Dr. Gloria Serra, (Ph.D. Chemistry 1998), is a full time Associate Professor of Medicinal Chemistry at Department of Organic Chemistry, Universidad de la República, Uruguay, South America. Dr. Serra’s research focuses on the total synthesis of natural products and analogs with antimalarial, anti-trypanosomal or cytotoxic activity and on the investigation and development of synthetic methodologies to obtain bioactive oxazoles, thiazoles and peptides macrocycles. She is the principal investigator of projects funded by different Agencies from Uruguay, South America and FIRCA-NIH, USA. Awards and honors include Investigator II of the National Agency for Investigation and Innovation, Uruguay; lecturer at Universities and Congresses in USA, Europe and Latin America; member of Scientific Committees of International Symposiums. She has published numerous papers, reviews and book chapters in the area of organic chemistry and medicinal chemistry.

Nicholas Terrett, Ph.D., CSO, Ensemble Therapeutics Corp

Dr. Nicholas Terrett was born in London and educated at the University of Cambridge, and has worked at both GSK and Pfizer as a medicinal and technology chemist. At Pfizer he was the lead chemist and inventor for the program that discovered sildenafil (Viagra™, Revatio™). Nick established Pfizer’s combinatorial chemistry group, and was also responsible for high throughput screening and the materials management groups. From 2003 to 2006 Nick was Senior Director and Head of Chemical Sciences at Pfizer, Cambridge MA. Since 2006 Nick has been Chief Scientific Officer for Ensemble Therapeutics, a biotech company in Cambridge, MA. Ensemble uses a DNA-programmed chemistry technology platform to generate large libraries of macrocycles successfully used to find unprecedented small molecule leads against challenging protein-protein interactions.

Marc Thommen, Ph.D., Head, Technology Platforms, Polyphor Dr. Marc Thommen received his Ph.D. in Chemistry from the University of Bern in 1995. From 1995 to 1997 he studied in the group of Prof. Dr. Barry M. Trost at Stanford University as a postdoctoral fellow before joining the Novartis catalysis R&D department in Basel as lab head. In the course of the spin-off of the Scientific Services department in 1999, which led to the foundation of Solvias AG, he managed numerous collaboration projects associated with pre-clinical and phase 1 & 2 supply and later led the catalysis and chiral ligand commercialization project. In 2005 he was appointed head of product management of Solvias before joining Polyphor in 2007 as head of the technology platforms unit

Peter Timmerman, Ph.D., CSO, Pepscan Therapeutics

Peter Timmerman studied Organic and Analytical Chemistry at the ‘Vrije Universiteit’ of Amsterdam (1984-1989). He obtained a PhD-degree in Supramolecular Chemistry (summa cum laude) from the University of Twente with David N. Reinhoudt (1994). He was Assistant Professor in Supramolecular Chemistry at the University of Twente from 1995-2001, whereafter he joined Pepscan Therapeutics in 2001. He is the inventor of Pepscan’s proprietary and broadly applicable ‘2-CLIPS’ technology for conformationally constraining peptides. The technology is a.o. applied to the mapping of conformational and discontinuous antibody binding sites. Lately, Bicycle Therapeutics was granted a non-exclusive license on the CLIPS-technology for development of therapeutic 2-CLIPS peptides. Timmerman also led the development of a therapeutic peptide-based anti-VEGF-vaccine that is currently in Phase-IIa clinical testing. Since March 2007 he holds a Special Chair in ‘Protein Mimetic Chemistry’ at the Faculty of Science of the University of Amsterdam. Timmerman is co-author of >80 peer-reviewed scientific papers and >10 patents. 


Dietmar Wolf, Ph.D., Executive Vice President, AnalytiCon Discovery, LLC

Dietmar Wolf studied organic chemistry at University of Muenster and TU Berlin (Germany) followed by a postdoctoral position on marine natural products at the University of Oklahoma (USA). In 1998 he started as research scientist at AnalytiCon AG (Germany) and moved on to the position as project leader at AnalytiCon Discovery GmbH (Germany). In 2011 he established the subsidiary AnalytiCon Discovery, LLC in Maryland (USA) and is – as Executive VP - responsible for the development of new business opportunities in the U.S.applying AnalytiCon’s proprietary natural product platforms.

Qinghai Zhang, Ph.D., Associate Professor, Integral Structural and Computational Biology, The Scripps Research Institute

Qinghai Zhang obtained his Ph. D. in organic chemistry from Shanghai Institute of Organic Chemistry in 2001, and did postdoctoral research on protein biochemistry and biophysics at The Scripps Research Institute from 2001 to 2004. He was subsequently promoted to assistant professor and is now an associate professor in Department of Integral Structural and Computational Biology at Scripps. His current research interests center on the development of chemical tools, ligands, and methodologies enabling the structural and functional characterization of membrane-associated proteins.

 

Fragment Based Drug Discovery (April 24-25) 

Valerio Berdini, Ph.D., Associate Director, Computational Chemistry, Astex Pharmaceutical

Dr. Valerio Berdini got his degree in chemistry at Rome University in Italy in 1995 which he followed with two years on a fully funded research project on drug design and computational chemistry. He then worked for three years as a research scientist at Dompè S.p.A., in Italy. Valerio moved to Astex in Cambridge in September 2001 as a full time molecular modeller where he progressed to the role of Associate Director. In the years Valerio has been working on several structure-based projects focusing primarily, but not exclusively, on Kinases inhibitors design. Using Astex state-of-the-art Fragment Based approach he is co-author of many patents, medicinal Chemistry papers and has been involved in the design of several of Astex clinical candidates.

Ben Davis, Ph.D. Research Fellow, Biology, Vernalis

Dr. Ben Davis studied protein folding by NMR for his PhD with Professor Alan Fersht at Cambridge University Chemical Laboratory, before moving to Dr Paul Driscoll’s NMR group at University College London where he worked on protein-ligand interactions in collaboration with Yamanouchi Pharmaceutical Company (now Astellas). In 1998 he joined RiboTargets, a biotech company formed out of the Laboratory of Molecular Biology in Cambridge UK, where he worked on applying structure based drug discovery techniques to a variety of RNA and protein targets. In 2003 RiboTargets merged with Vernalis, and focussed research towards protein targets. Since 2001, he has been heavily involved in the development and application of fragment based lead discovery technologies to a wide range of therapeutic targets.

Mark Elban, Ph.D., Investigator, CSC Chemistry, RD Platform Technology & Science, GlaxoSmithKline

Dr. Mark Elban received his PhD under the guidance of Sidney Hecht at the University of Virginia studying the synthesis of DNA damaging agents. Later he studied under Amos Smith III for his post doc working on the synthesis of HIV entry inhibitors and the lituarines. He has since worked four years for GlaxoSmithKline in the fragment based drug discovery group.

Daniel A. Erlanson, Ph.D., President and Co-Founder, Carmot Therapeutics, Inc.

Dr. Daniel A. Erlanson is the co-founder of Carmot Therapeutics, Inc. (http://www.carmot.us), a small-molecule drug discovery company applying fragment-based approaches to a variety of therapeutic targets. Prior to Carmot, Dr. Erlanson spent a decade developing fragment-based drug discovery technologies at Sunesis Pharmaceuticals, which he joined at the company's inception. Before Sunesis, he was an NIH postdoctoral fellow with James A. Wells at Genentech. Dr. Erlanson earned his Ph.D. in chemistry from Harvard University in the laboratory of Gregory L. Verdine and his BA in chemistry from Carleton College. As well as co-editing the first book on fragment-based drug discovery, Dr. Erlanson is an inventor on more than a dozen issued patents and published patent applications and an author of more than two dozen scientific publications. He is also editor in chief of Practical Fragments (http://practicalfragments.blogspot.com/), a blog devoted to fragment-based drug discovery.

Iwan de Esch, Ph.D., Professor, Medicinal Chemistry, VU University, Amsterdam

Dr. Iwan de Esch has academic and industrial experience in the design and synthesis of biologically active compounds. In recent years, he has set up a fragment-based drug discovery research line that efficiently develops optimized lead compounds for a wide variety of targets, including antimicrobial targets such as FtsQ. He has been involved in numerous PPPs, including several Top Institute Pharma projects, EU-FP7 projects (Fludrugstrategy, Neurocypres, Flucure), IMI projects (K4DD) and a Eureka’s Eurostar programme (Kinomed). The high valorisation potential of the work is illustrated by the formation of three successful spin-out companies that dr. de Esch co-founded, i.e., De Novo Pharmaceuticals Ltd, IOTA Pharmaceuticals Ltd and Griffin Discoveries BV. He published more than a hundred scientific publications and has filed several patent applications.

Fleur Ferguson, Ph.D. Student, Laboratory of Christopher Abell, Department of Chemistry, University of Cambridge

Fleur Feguson is a Chemistry PhD student at the University of Cambridge, funded by the BBSRC. She is working in the group of Prof. Chris Abell, and is also supervised by Dr. Alessio Ciulli (University of Dundee). Her PhD is focused on targeting the bromodomain of BAZ2B using fragment-based approaches, working in collaboration with the SGC, Oxford. She completed a Masters degree in Chemistry at Imperial College London in 2010, in which she obtained First Class honors and was awarded the Chemistry Departmental Prize for Overall Excellence. Fleur completed two summer internships working on cancer therapeutics at OSI Pharmaceuticals, NY (2008, 2009), which sparked her interest in medicinal chemistry. These experiences encouraged her to conduct her final year research project in the lab of Prof. Alan Spivey, investigating design and synthesis of inhibitors of the transcription factor LRH-1. After completing her PhD (expected October 2014) she would like to continue working in Chemical Biology and Medicinal Chemistry research.

Brad Jordan, Ph.D., Senior Scientist, Molecular Structure and Characterization, Amgen

Dr. Brad Jordan received his Ph.D. in Biochemistry from the University of Arkansas. His postdoctoral work was with Dr. Richard Kriwacki at St. Jude Children’s Research Hospital in Memphis, TN where he studied the structure and function of bacterial choline binding proteins using NMR spectroscopy. Brad has now been at Amgen for seven years and had been part of their Biophysics group, focusing primarily on NMR, SPR, and other Biophysical methods. He currently heads the Fragment Based Screening program.

Isabelle Krimm, Ph.D., Fragment-Based Screening & NMR Team, Institute of Analytical Sciences, University of Lyon, CNRS

Dr. Isabelle Krimm is currently working in the CNRS, University of Lyon, France. She obtained her PhD on structural biology studies of thioredoxine-dependent enzymes and toxins by NMR in 2000. She then joined the Commissariat à l’Energie Atomique to study lamin proteins by heteronuclear NMR. She obtained a CNRS position in 2002 and studied protein structures. Her current research focuses on fragment-based protein-ligand interactions by NMR, both for drug discovery and chemical biology.

Peter Kutchukian, Ph.D., Associate Principal Scientist, ChemInformatics, Merck and Co.


Woody Sherman,Ph.D., Vice President, Applications Science, Schrödinger

Woody Sherman is Vice President of Applications Science at Schrödinger. He received his B.S. in Physical Chemistry from the University of California at Santa Barbara where he studied nonlinear optical properties of organic polymers using computational quantum mechanics methods. He completed his Ph.D. at MIT working in Professor Bruce Tidor’s lab where he examined the role of electrostatics in protein-ligand binding and implemented a novel method for optimizing ligand binding specificity across a panel of targets. While in graduate school he completed an internship at Biogen where he helped develop novel methods to enhance antibody affinity through electrostatic charge optimization, resulting in a publication and patent. At Schrödinger, he is involved in applications projects, product development, methods development, and the deployment of Python-based tools. He also works closely with customers on research projects and collaborations. Woody has published on a broad range of topics, including induced-fit docking, ensemble docking, protein design, small molecule optimization, cheminformatics, hybrid ligand/structure-based methods, free energy simulations, charge optimization, pharmacophore modeling, and more. He is a reviewer for many top journals related to computational chemistry and drug design and is on the Editorial Board of both Chemical Biology & Drug Design and Journal of Chemical Information and Modeling. 


Arun Shukla, Ph.D., Assistant Professor, Medicine, Duke University Medical Center


Nicholas J. Skelton, Ph.D., Senior Scientist, Department of Discovery Chemistry, Genentech, Inc.


Andrew Stamford, Ph.D., Executive Director, Medicinal Chemistry, Merck


Francisco X. Talamas, Ph.D., former Associate Director and Head, Virology Chemistry, F. Hoffmann-La Roche, Inc.

Francisco Talamas received his Doctorate of Philosophy degree in Chemistry from the University of Alberta. After a post-doctoral fellowship at Harvard University working on the synthesis of Palytoxin under the direction of Professor Yoshito Kishi, Francisco spent six years at Syntex, Mexico working on inflammation programs. In 1996, he moved to Palo Alto CA, to join Roche Bioscience. During the next 14 years, he led several drug discovery projects in inflammation, CNS and virology that delivered candidates to Phase I clinical trials. In 2010, he moved to Nutley, NJ with Hoffmann-La Roche and stayed there for three years where he served as the head of virology chemistry supporting the virology disease area.

Steven J. Taylor, Ph.D., Director, Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc.

Dr. Steven Taylor received his Ph.D. in organic chemistry under the advisement of James Morken at the University of North Carolina at Chapel Hill. After completion of his doctoral work he moved to Harvard University where he worked with Stuart Schreiber on developing the diversity oriented synthesis of natural product-like alkaloids. Over the course of his career he has authored/coauthored more the 20 patents and peer reviewed publications. Steven joined Boehringer Ingelheim in 2004, and over the past 10 years has worked on multiple lead identification and lead optimization programs including sEH, MMP-13, Chymase, UT, and HCV Helicase. He was one of the founding members of the international Alternative Lead Identification team, and established the fragment based drug discovery program at BI Ridgefield. During this time, he was responsible for devising and implementing the chemistry strategy for the ALI team, which led to the successful delivery of compounds for multiple milestones. The most advance compound from these efforts completed phase 1 clinical trails in 2013. More recently he led the Parallel synthesis and Discovery Analytics group, and in collaboration with the research networking team he performed the first benchmarking analysis of the PS&A team to establish best practices vs. external competitors.

In addition, he has helped to establish a number of process improvements for the PS&A including expansion of the the infrastructure of the Analytics functions to support super critical CO2 purifications. In December of 2011 he was promoted to Director in the Medicinal Chemistry Department and is responsible for delivery of new chemical entities in to preclinical development for multiple projects in the Cardiometabolic and Inflammation Immunology portfolios.

Chris Williams, Ph.D., Principal Scientist, Chemical Computing Group

Originally trained as a chemical engineer, Chris Williams worked in the manufacturing of industrial explosives before embarking on graduate studies at McGill University under Dr. Tony Whitehead. Chris received his Ph.D. in 1996, after which he worked at various colleges before starting full-time as an application scientist at Chemical Computing Group in 1998. Chris Williams is still at Chemical Computing group, where he has been a Principal Scientist since 2002.


Damian W. Young, Ph.D., Assistant Professor, Departments of Pathology and Immunology and Pharmacology; Assistant Director, Center of Drug Discovery, Baylor College of Medicine


Dr. Damian Young is Assistant Director of the Center for Drug Discovery (CDD) at Baylor College of Medicine.He is also a Scholar of the Cancer Prevention and Research Institute of Texas (CPRIT). Prior to this, he was Group Leader within the Chemical Biology Program at the Broad Institute of Harvard and MIT. Dr. Young’s research program focuses on developing modern synthetic methodologies to assemble small molecule–screening collections for therapeutic discovery. He has utilized diversity-oriented synthesis (DOS) to produce screening collections that have led to a variety of chemical probes using high-throughput screening. More recently, his group was the first to apply the principles of DOS to fragment-based drug discovery (FBDD). At Baylor, Dr. Young is applying these DOS-based fragment strategies to important targets in cancer. Dr. Young received a BS degree in chemistry from Howard University in Washington DC and a PhD in organic chemistry from the North Carolina State University in Raleigh, NC, under the direction of Prof. Daniel L. Comins. He  conducted postdoctoral studies at Harvard University and the Broad Institute of Harvard and MIT in the laboratory of Prof. Stuart L. Schreiber.

 

Kinase Inhibitor Chemistry (April 24-25) 

Dean Richard Artis, Ph.D., Senior Vice President, Molecular Discovery, Elan


Valerio Berdini, Associate Director, Computational Chemistry, Astex Pharmaceutical

Valerio received his degree in chemistry at Rome University in Italy in 1995 which he followed with two years on a fully funded research project on drug design and computational chemistry. He then worked for three years as a research scientist at Dompè S.p.A., in Italy. Valerio moved to Astex in Cambridge in September 2001 as a full time molecular modeler where he progressed to the role of Associate Director. In the years Valerio has been working on several structure-based projects focusing primarily, but not exclusively, on Kinases inhibitors design. Using Astex state-of-the-art Fragment Based approach he is co-author of many patents, medicinal Chemistry papers and has been involved in the design of several of Astex clinical candidates.

Rogier C. Buijsman, Ph.D., Head, Chemistry, Netherlands Translational Research Center B.V. (NTRC)

Rogier Buijsman is Head of Chemistry and Co-Founder of the Netherlands Translational Research Center BV. Rogier is trained as a medicinal chemist working in pharmaceutical industry for more than 15 years. Rogier started its carreer at MSD/Organon, where he worked on nuclear receptor, GPCR and kinase programmes within Oncology, Immunology and Fertility.

Bruce Dorsey, Ph.D., Senior Director, Medicinal Chemistry, Teva Pharmaceuticals

Dr. Bruce Dorsey is currently a Senior Director of Medicinal Chemistry at Teva Pharmaceuticals, where he is responsible for all medicinal chemistry small molecule programs to deliver drug candidates in the therapeutic areas of oncology, inflammation and CNS. He began a career in medicinal chemistry at Merck and Co., Inc. contributing to medicinal chemistry teams in virology, anticoagulants, and neuroscience. After twelve years at Merck he left to join an emerging biotech discovery company, Locus Pharmaceuticals. As a principle investigator at Locus Pharmaceuticals and head of the medicinal chemistry department, Bruce wrote for and received a Small Business Innovation Research Award for the design and synthesis of gp-41 inhibitors (HIV). In 2004, Bruce joined the Department of Medicinal Chemistry at Cephalon, Inc. During this time he has supervised a proteasome project (CEP-18770 reached phase II clinical trials), kinase inhibitor programs including ALK (CEP-37440 phase I), B-Raf (CEP-32496 phase I), FAK, JAK2, and AXL (CEP-40783 IND ready). He has been with Teva Pharmaceuticals since the acquisition of Cephalon in the fall of 2011. Bruce earned a Ph.D. degree from the University of Pennsylvania under the guidance of Amos B. Smith III, after which he joined the laboratory of Professor Stuart L. Schreiber and completed a National Institutes of Health postdoctoral fellowship spending time at Yale and Harvard University. He has co-authored 59 publications in chemistry and drug discovery, and is a co-inventor on 38 patents and patent applications.

Istvan Enyedy, Ph.D., Senior Scientist, Chemistry, Biogen Idec

In the past 15 years Istvan J. Enyedy has been involved in new target evaluation, hit finding, and hit-to-lead optimization projects for several types of target classes using both ligand and structure-based methods. He is coauthor on more than 30 publications and 9 patents/applications. He received his Ph.D. in 1998 at Catholic University of America, Washington DC, and did postdoctoral training in Dr. Shaomeng Wang’s group at Georgetown University Medical Center, Washington DC. Between 2001 and 2008 he worked at Bayer Pharmaceuticals, West Haven, CT and Novartis Institutes for Biomedical Research in Cambridge, MA. Since August 2008 he has been working at Biogen Idec in Cambridge, MA.

Jan Hoflack, Ph.D., CSO, Oncodesign Biotechnology

Before joining Oncodesign, Dr. Hoflack, was Vice-President Medicinal Chemistry and Biosciences at Johnson & Johnson Pharmaceutical R&D in Beerse, Belgium. Prior to this assignment, he held senior management positions at AstraZeneca in Gothenburg (Sweden), at Novartis in Basel (Switzerland), and at Marion Merrell Dow in Strasbourg (France). Dr Hoflack holds a Ph.D. in Organic Chemistry from the State University of Ghent in Belgium.

Stefan Laufer, Ph.D., Chairman, Pharmaceutical & Medicinal Chemistry, Pharmacy & Biochemistry, University of Tuebingen

Dr. Stefan Laufer is Professor for Pharmaceutical and Medicinal Chemistry at Tuebingen University. He received his degrees from Regensburg University. After 10 years in pharmaceutical industry (Head Drug Research, R&D Director) he joined in 1999 Tuebingen University as Chairman Pharm./Med. Chemistry. His research interests are anti-inflammatory drug discovery with various eicosanoid (COX-1,2,3, LOXs, mPGES1, cPLA2) and protein kinase targets (p38, JAKs, JNKs, CK1d, . Two compounds from his lab entered clinical development phases. Dr. Laufer chairs the ICEPHA (Interfaculty Center for Pharmacogenomics and Drug Research), an academic drug discovery platform at Tuebingen University and Robert Bosch Hospital Stuttgart. He has authored more than 300 publications and is inventor in 40 patent families.

Jun Liang, Ph.D., Scientist, Discovery Chemistry, Genentech, Inc.


Christel Menet, Ph.D., Senior Therapeutic Area Lead & Project Director, Galapagos NV

Dr. Christel Menet joined Galapagos in 2005, and over the past 8 yrs has taken on roles of increasing leadership and responsibility. Prior to Galapagos, she worked at Faust Pharmaceutical (French Biotech) and Evotec (UK) developing GLPG0555 – Phase 1; GLPG0778 – Jak1 selective, Phase II; GLPG0634 – Jak1, with positive results in Phase IIb; and others in preclinical development.

Pierre-Yves Michellys, Ph.D., Director, Medicinal Chemistry, The Genomics Institute of the Novartis Research Foundation (GNF)

Pierre-Yves Michellys received his Ph.D in 1995 from the laboratory of Professor Maurice Santelli at the University of Science and Techniques of Saint Jerome in Marseille (France) where he was studying expedited synthesis of novel estrane derivatives. In October 1995 he joined the laboratory of Professor Barry Trost at Stanford University for his post-doctoral studies where he contributed to the optimization of a methodology of macrocycle synthesis using a novel cycloisomerization of allene. In December 1997, he began his career as a medicinal chemist at Ligand Pharmaceuticals where he was involved in research associated with nuclear hormone receptors. In May 2003, he joined the Genomics Institute of the Novartis Research Foundation (GNF) where is now a Director of Medicinal Chemistry. He is currently involved in the discovery of novel innovative medicines for unmet medical needs in several disease areas.

Gerhard Mueller, Ph.D., Senior Vice President, Medicinal Chemistry, MercaChem BV

Dr. Gerhard Müller is the Senior Vice President of Medicinal Chemistry at MercaChem BV. Prior to joining MercaChem, Gerhard worked at Proteros fragments GmbH as Managing Director and Chief Scientific Officer and was instrumental in establishing the integrated lead discovery business. Before his step into the contract services industry, Gerhard had the position of Vice President Drug Discovery at GPC Biotech AG, a Munich-based oncology company. Additionally, Gerhard has built a successful track record in lead finding and optimization campaigns at Glaxo, Bayer AG and N.V. Organon, yielding several small molecule development candidates. He gained valuable managerial expertise running entire pre-clinical research departments and having project portfolio management responsibilities. Furthermore, Gerhard developed impressive entrepreneurial skills during the time when he held the position of Chief Scientific Officer at Axxima Pharmceuticals AG in Munich, a company dedicated to protein kinase inhibitor research. Gerhard received his Ph.D. in Organic Chemistry in 1992 from the Technical University of Munich, working with Prof. Dr. Horst Kessler on anti-adhesive integrin antagonists.

Stuart Onions, Ph.D., Director, Research Management, Sygnature Discovery Ltd.

Stuart obtained his M.Chem. in chemistry in 2001 from Nottingham Trent University and a Ph.D. from the same university in synthetic supramolecular chemistry in 2004. Following this Stuart joined what was then Sygnature Chemical Services, now Sygnature Discovery, as a bench chemist. During his career Stuart has progressed from Senior Scientistto his current post of Director of Research Management as the Company has grown from fewer than ten individuals to a headcount of over 90 people (as of Nov 2013). He has enjoyed a very successful career at Sygnature Discovery with three compounds discovered during medicinal chemistry projects under his leadership entering human clinical trials. His publication record includes over thirty papers and patents.

Susanta Samajdar, Ph.D., Research Director, Medicinal Chemistry, Aurigene Discovery Technologies Limited

Susanta Samajdar received his Ph.D. in Synthetic Organic Chemistry from Indian Association for the Cultivation of Science (IACS), Kolkata and subsequently moved to MD Anderson Cancer Center for a Post-Doctoral training on anti-cancer drug discovery. He has over 12 years of synthetic and Medicinal Chemistry research experience in Indian Industries. Susanta has experience in leading multi-disciplinary drug discovery teams that successfully delivered several preclinical development candidates. He has elaborate experience in working with Kinases and other target classes like GPCRs, Ion channels, Proteases and NHRs, across different therapeutic areas like Oncology, Pain and Inflammation and Neurosciences.

Laurent Schio, Ph.D., Director, Medicinal Chemistry, Oncology, Sanofi

Dr. Laurent Schio received his Ph.D., in Organic chemistry from the University of Rennes in1990, then joined Roussel-Uclaf in 1991 following a postdoctoral fellowship at the Florida Institute of Technology. Until 2001, he led a lab of medicinal chemists in the anti-infective disease area (antibacterial projects) and an anti-fungal project which delivered a clinical candidate. For a period of 3 years, he then joined the Lead Generation platform of Aventis to coordinate the anti-infective portfolio of discovery projects and contributed to develop a new methodology for hit validation. In 2004, he moved back to the global organization of Medicinal Chemistry as a section head and supported Oncology and CNS projects. In 2005, in Sanofi, he joined Oncology Medicinal Chemistry as a section head. His group identified a development candidate for HSP90 and a pre-candidate for Aurora. In 2009, he became global head of Oncology medicinal chemistry and contributed to identify a clinical candidate for Met. Since 2010, he lead the Oncology medicinal chemistry group of Vitry and contributed to the discovery of the PI3Kβ clinical candidate and two other selective kinase inhibitors for development.

Erik Verner, Ph.D., Director, Chemistry, Principia Biopharma


Anthony D. William, Ph.D., Senior Scientist, The Agency for Science, Technology and Research (A*STAR)-ICES

 

Anti-Inflammatories | Protein-Protein Interactions | Epigenetic Inhibitor Discovery 
Macrocyclics and Constrained Peptides | Fragment Based Drug Discovery | Kinase Inhibitor Chemistry