Cambridge Healthtech Institute’s 8th Annual

Macrocyclics & Constrained Peptides

Discovery and Design of Cell-Penetrating, Middle-Sized Molecules for Oral-Based Medicines

April 14-15, 2020

In the drug discovery industry, synthetic macrocyclic compounds theoretically fit the bill for new chemical entities that have good drug potential yet can access newer drug targets such as protein-protein interactions (PPIs) that are intracellular and more complex than traditional enzymatic targets. Indeed, there are examples of naturally occurring macrocyclics, such as cyclosporin, that have become successful drug compounds. Synthetic macrocyclics' 'idealness' however is still being optimized. Please join us to stay abreast and discuss challenges that remain in the discovery, design and optimization of macrocyclic compounds or constrained peptides with good oral bioavailability and cell penetration.

Preliminary Agenda

NEW APPROACHES FOR CONSTRUCTING MACROCYCLIC SCAFFOLDS

Encoded Library Approaches for Macrocyclic Peptide-Based Drug Discovery

Christoph Dumelin, PhD, Investigator III, Chemical Biology & Therapeutics (CBT), Novartis Pharma AG

Macrocycles to Control Peptide Conformation and Activity

Paramjit Arora, PhD, Professor, Chemistry, New York University

New Chemistries for Macrocyclic Scaffolds

Laura Itzhaki, PhD, Professor, Pharmacology, University of Cambridge

Selection Methodology for Macrocyclics from DEL Campaigns

Chris Phelps, PhD, Manager, R&D Platform Technology & Science, GlaxoSmithKline Boston

CONSTRAINED PEPTIDES

Cyclotides as Scaffolds for Intracellular Targets

David Craik, PhD, ARC Laureate Fellow – Group Leader, Institute for Molecular Bioscience, Queensland University, Australia

Constrained Peptides for Drug Discovery

Rami Hannoush, PhD, Principal Scientist, Group Leader, Early Drug Biochemistry, Genentech

MACROCYCLIC-BASED DRUG LEADS

Type IV Macrocyclic Inhibitors of BRAF Kinase Block Paradoxical Signaling in Resistant Melanomas

Campbell McInnes, PhD, Professor, Drug Discovery and Biomedical Sciences, University of South Carolina

Cell-Based Production and Selection of PPI-Modulating Compounds

Maria Soloveychik, PhD, CEO, SnyntheX

Syrbactin Proteasome Inhibitors for Oncology and Immune Disorders

Michael Pirrung, PhD, Distinguished Professor of Chemistry, University of California Riverside

* The program is subject to change without notice, due to unforeseen reason.