9th Annual

Protein-Protein Interactions

Targeting PPIs for Therapeutic Interventions

April 19-20, 2016

Protein-Protein Interactions icon  

Many important biological processes are controlled by protein complexes comprised of protein-protein interactions (PPIs). Thus PPI sites represent potential targets for compounds to be developed against for modulation of specific disease processes. Such modulator compounds however are difficult to discover and design because unlike typical drug compounds, they are not easily screened for because they are not  designed to inhibit the catalytic site of an enzyme. However advances in adapting biophysical approaches to higher-throughput formats for detecting protein-protein interactions have enabled progress. An increase in the types of easily screenable compounds (such as macrocyclic peptides from DNA-encoded libraries) that can cross the cell membrane and reach intracellular PPI targets has also spurred the field forward. This meeting covers progress in the PPI area with a focus on how scientists have dealt with the challenging questions in PPI-targeted drug design such as: should we inhibit the PPI directly or allosterically? Which interface should be targeted and how much of it? Should the inhibitor bind transiently or longer?

Preliminary Agenda

Modulating Protein-Protein Interactions in the Ubiquitin Pathway

A New Paradigm in Drug Action:  Differentiated Gain of Function amongst IMiD® Analogues Binding the E3 Ubiquitin Ligase, CRL4CRBN

Philip Chamberlain, Ph.D., Principal Scientist, Biochemistry and Structural Biology, Celgene

The Discovery of CB-5083: A 1st in Class Inhibitor of p97 for the Treatment of Cancer

David Wustrow, Ph.D., Executive Vice President, Chemistry, Cleave Biosciences

Conformation-Selective Inhibitors of the AAA ATPase p97

Stacie Bulfer, Ph.D., Post-Doctoral Scholar, Michelle Arkin Laboratory, Pharmaceutical Chemistry, University of California, San Francisco

Discovery and Characterization of Small Molecule Fragments that Bind and Inhibit the Ubiquitin Specific Protease 7 (USP7)

Paola Di Lello, Ph.D., Scientist, Biophysical and Structural Chemistry, Genentech

PPI Inhibitors in Development

BCL-2 Inhibitors for Cancer

George Doherty, Ph.D., Principal Research Scientist, Oncology Discovery, Abbvie

From Fragment to in vivo Activity for a Challenging PPI Target

Tom Davies, Ph.D., Associate Director, Molecular Sciences, Astex Pharmaceuticals

Efficient Small Molecule Inhibitors of the HDM2-p53 Protein-Protein Interaction

Michael H. Reutershan, Senior Scientist, Medicinal Chemistry, Merck Research Laboratories

Inhibitors of MAP Kinases Targeting a Novel Allosteric Site

Juan Jesus Perez, Ph.D., Professor, Department of Chemical Engineering, Technical University of Catalonia and Director, Molecular Modeling, Allinky Biopharma

Identifying and Optimizing Modulators of Protein-Protein Interaction Sites

Triage of HTS Hits for Protein-Protein Interactions

Kevin Lumb, Ph.D., Scientific Director, Discovery Technologies, Janssen R&D 

How to Facilitate the Identification of Protein-Protein Interactions Inhibitors

Oliver Sperandio, Ph.D., Senior Research Associate, Inserm

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