3rd Annual

Macrocyclics and Constrained Peptides

Bigger, Better, But hopefully still Oral, Small Molecules

April 22-23, 2015 

 

Recent advances combining biological and chemical approaches to create libraries of small, synthetic macrocyclic molecules have created a new class of therapeutically promising compounds that exhibit desireable ‘middle ground’ characteristics – small enough to pass through the cell membrane and reach intracellular targets, with the potential to be delivered orally; but large enough to have better specificity for disrupting protein-protein interactions. This conference explores this emerging class of molecules and discusses the challenges they face as drug candidates. Join fellow drug discovery scientists for this day-and-a-half meeting that is in the second half of our larger Drug Discovery Chemistry event. 


 

This meeting was an eye-opener for me to see how collectively drug delivery scientists can work
with medicinal chemists to bring new pharmaceutical products more effectively to the market.

Hayat O., Professor, University of Illinois at Chicago

Preliminary Agenda


Plenary Keynote

Fragment-Based Drug Discovery: A Fifteen Year (Re-)Evolution

Harren Jhoti, Ph.D., President & CEO, Astex Pharmaceuticals


EXPANDING THE RULE OF FIVE

FEATURED SPEAKER: Understanding Permeability of Peptide and Peptidomimetic Macrocycles

Spiro Liras, Ph.D., Vice President, Worldwide Medicinal Chemistry, CVMED, Pfizer

Towards Design Rules for Macrocycles

Adrian Whitty, Ph.D., Department of Chemistry, Biomolecular Engineering Research Center, Boston University

Oral Druggable Space beyond the Rule of 5: Insights from Drugs and Clinical Candidates

Jan Kihlberg, Ph.D., Professor, Department of Chemistry, BMC, Uppsala University, Sweden

Constrained Cyclic Peptides: Conformation vs. Bioavailability

David P. Fairlie, Ph.D., Professor and Head, Division of Chemistry and Structural Biology, Institute for Molecular Bioscience, University of Queensland       

 

STRATEGIC TARGET SELECTION FOR SYNTHETIC MACROCYCLICS

A Novel Cyclic Peptide Drp1 Inhibitor Diminishes Aberrant Mitochondrial Fission

Nir Qvit, Ph.D., Postdoctoral Fellow, Chemical and Systems Biology, Stanford University

Structural Basis of Macrocycle-Enzyme Interaction

Markus Seeliger, Ph.D., Assistant Professor, Pharmacological Sciences, Stony Brook University


CASE STUDIES: PROGRESSING IN THE DEVELOPMENT PIPELINE

Exploring Macrocycles for Protein-Protein Interaction Targets: the Discovery of Novel Bifunctional XIAP Antagonists

Nick Terrett, Ph.D., Chief Scientific Officer, Ensemble

A Macrocyclic Peptide Inhibitor of Complement C5 as an Alternative to Monoclonal Antibody Therapy

Douglas A. Treco, Ph.D., President and CEO, Ra Pharmaceuticals, Inc.

 

PF-06463922, a Novel Small Molecule macrocyclic inhibitor of ALK/ROS1 with Pre-clinical Brain Availability and Broad Spectrum Potency against ALK-resistant Mutations   

Ted W. Johnson, Ph.D., Research Fellow, Medicinal Chemistry, Pfizer Oncology  

 

 



For more details on the conference, please contact:
Anjani Shah, Ph.D.
Conference Director
Cambridge Healthtech Institute
Phone: (914) 723-0255
Email: ashah@healthtech.com 

For partnering and sponsorship information, please contact:
Carolyn Benton
Business Development Manager
Cambridge Healthtech Institute
Phone: (+1) 781-972-5412
Email: cbenton@healthtech.com