4th Annual

Macrocyclics and Constrained Peptides

Bigger, Better, But hopefully still Oral, Small Molecules

April 20-21, 2016

Macrocyclics and Constrained Peptides icon  

The newer, synthetic macrocyclic and constrained peptide compounds (ranging in size from .5 -2 kilodaltons) offer the promise of being the ‘ideal’ class of compounds for new drug entities. Their cyclical shape enables solubility and stability affording them the possibility to be developed into oral medications and most are small enough to cross the cell membrane to reach intracellular targets, where many of the causes and solutions to diseases reside. And because of macrocyclics’ slightly larger size than typical small molecules, they offer more specificity and have greater chances of disrupting protein-protein interactions. However, theory has yet to be fully realized. Solubility and cell permeability issues are still being addressed. This meeting will focus on the remaining challenges, cover the new targets being addressed with macrocyclics and provide updates on a few early examples of compounds advancing in drug development.

Preliminary Agenda

Design Considerations and Challenges

Passive Membrane Permeability in Cyclic Peptides: New Rules for a New Chemical Space 
Scott Lokey, Ph.D., Professor, Chemistry and Biochemistry, University of California, Santa Cruz 

How to Design Non-Peptidic Cell Permeable Macrocycycles

Jan Kihlberg, Ph.D., Professor, Organic Chemistry, Uppsala University

Computer-aided Macrocycle Design

Matthew Jacobson, Ph.D., Professor, Pharmaceutical Chemistry, University of California, San Francisco

Schrodinger logoTechnologies Enabling Macrocycle Design

Dan Sindhikara,, Ph.D., Senior Scientist, Schrödinger

Library Synthesis and Screening

Synthesis and Screening of Vast Libraries of DNA-Encoded Macrocycles

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

Macrocyclic Drug Candidates for Lung Diseases and Novel Antibiotics

Daniel Obrecht, Ph.D., CSO, Pharmaceutical Research, Polyphor Ltd.

Case Studies: Compounds in Early Development

Lorlatinib (PF-06463922), a Macrocyclic ALK/ROS1 Inhibitor for the Treatment of Resistance Mutations and Brain Metastasis

Teddy W. Johnson, Ph.D., Senior Principal Scientist, Oncology Chemistry, Pfizer San Diego

Cyclohexylgriselimycin: A Synthetic and New Anti-Tuberculosis Drug Candidate

Evelyne Fontaine, Ph.D., Laboratory Head, Infectious Diseases, Medicinal Chemistry, Sanofi

Macrocycle Design for PD1-PD1L and p53-MDM2

Alexander Dömling, Ph.D., Professor, Drug Design, University of Groningen

Targeting Ras-GTPase Oncogenic Interactions with Macrocyclics

Dehua Pei, Ph.D., Professor, Department of Chemistry and Biochemistry, The Ohio State University

Orally Stable GI-restricted Peptides for Inflammatory Bowel Diseases 

Ashok Bhandari, Ph.D., Senior Director Chemistry, Protagonist Therapeutics 

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