Cambridge Healthtech Institute’s 13th Annual

Protein-Protein Interactions

Targeting PPIs and Nucleic Acid Complexes for Therapeutic Interventions

April 15-16, 2020

More examples in medical research are now arising about diseases that can be addressed by disrupting or modifying complexes of proteins that aberrantly interact with one another. Such protein-protein interaction (PPI) complexes can be considered a type of drug target. PPI targets are different from traditional drug targets that comprise of a single protein, more specifically an enzyme, whose function is targeted for reduction by a chemical inhibitor. For the medicinal chemist whose role is to discover, design or optimize compounds with therapeutic potential, PPIs are expanding what can be ‘drugged or targeted’ by them. However the ‘flat and large’ interacting surfaces of PPIs make them less amenable to the typical ‘groove and ball’ inhibitor design strategy for enzymes. Luckily, advances in biophysical techniques such as nuclear magnetic resonance (NMR), surface plasmon resonance (SPR) that enable rapid detection of bi-molecular interactions without an enzymatic readout, have aided progress in finding new drug leads against PPIs. At CHI’s 13th Annual Protein-Protein Interactions conference, join fellow discovery chemists to share stories and discuss best practices in this new area of disease-relevant space that is rapidly becoming more accessible.

Preliminary Agenda


Covalent Fragment-based Drug Discovery: KRAS and Beyond

Dan Erlanson, PhD, Vice President, Chemistry, Frontier Medicines

Discovery and Early Development of MRTX849, a Selective, Covalent Inhibitor of KRAS G12C

Matt Marx, Vice President, Drug Discovery, Mirati Therapeutics

Targeting KRAS Directly with Novel Drug Discovery Efforts at the NCI RAS Initiative

Dominic Esposito, PhD, Director, Protein Expression Laboratory, Frederick National Laboratory for Cancer Research (FNLCR)

Translating Frontier Oncology Targets to Outsmart Cancer

Adrian Gill, PhD, Vice President, Medicinal Chemistry & CMC, Revolution Medicines

Targeting Mutant KRAS by Direct and Indirect Approaches

Michael Gmachl, PhD, Principal Scientist, New Therapeutic Concepts, Boehringer-Ingelheim


Structure and Biophysical Characterization of Parkinson’s Disease Target, Neurturin-GFRa2

Jenny Sandmark, PhD, Associate Principal Scientist, Drug Discovery, AstraZeneca R&D


Fragment-Based Discovery of an Apolipoprotein E4 (apoE4) Stabilizer

Andrew Petros, PhD, Senior Principal Research Scientist, Protein & Assay Sciences, AbbVie

Inhibitors of Sec61 as Novel Anti-Cancer Therapeutics

Dustin McMinn, Ph.D., Senior Director, Head of Chemistry, Kezar Life Sciences

Identification of a New Class of HBV Capsid Assembly Modulator

Scott Kuduk, PhD, Scientific Director, Discovery Chemistry, Novira/J&J

Leveraging Viral Protein-Protein Interactions to Generate Inhibitors of BK and JC Polyomavirus in Early-stage Drug Discovery

Charles Warthchow, PhD, Senior Investigator, Global Discovery Chemistry, Novartis Institutes for Biomedical Research

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

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