3rd Annual

Macrocyclics and Constrained Peptides

Bigger, Better, But hopefully still Oral, Small Molecules

April 22-23, 2015 

 
 

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

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 placing them in size between small molecule drug entities and larger therapeutic antibodies. Similar to small molecules, the smaller macrocyclics can pass through the cell membrane to reach intracellular targets and have the potential to be delivered orally. But their cyclic shape and slightly larger size confers advantages of bigger (but not orally bioavailable) molecules such as biologics and naturally-occurring macrocyclics which have better specificity for disrupting protein-protein interactions. Thus small macrocyclics have the promise to successfully inhibit a largely untapped but medically relevant class of drug targets –intracellular regulatory protein complexes that are dependent on protein-protein interactions.

Cambridge Healthtech Institute’s third annual Macrocyclic and Constrained Peptides meeting, part of our Drug Discovery Chemistry event, will continue to explore this emerging class of molecules and discuss the challenges they are facing as drug candidates now that several have entered clinical development. Constrained peptides, which can be considered macrocyclic because of their 3D shape but are slightly larger (between 2 and 5 kilodaltons) than macrocyclic peptides, will also be covered. 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.
 

Preliminary Agenda


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


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

Identification of High Affinity Protein Ligands from DNA-Encoded Libraries of Macrocyclic Peptidomimetic Compounds

Thomas Kodadek, Ph.D., Professor, Chemistry & Cancer Biology, The Scripps Research Institute


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

Targeting PPIs in Inflammation

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



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