8th Annual

Protein-Protein Interactions

Targeting PPIs for Therapeutic Interventions

April 21-22, 2015 


Many biologically important processes are regulated by protein complexes. Such protein-protein interactions (PPIs) or protein-DNA interactions were considered ‘undruggable’ until recently. The main driver of recent PPI successes has been biophysical techniques such as surface plasma resonance (SPR) and nuclear magnetic resonance (NMR), sometimes using fragment-based approaches, that have resulted in inhibitors against even difficult PPIs. Computational approaches based on crystal structures of the PPIs being targeted have also accelerated drug design against PPIs. This conference will cover ‘success stories’ highlighting application of biophysical approaches, as well as the challenges that still exist in PPI-targeted drug design: should we inhibit the PPI directly or allosterically? Which interface should be targeted and how much of it? How strongly does the inhibitor need to bind? Join fellow drug discovery scientists for this day-and-a-half meeting that is in the first half of CHI's larger Drug Discovery Chemistry event


The Drug Discovery Chemistry conference offers a compact, dynamic event over
three days that allows the scientific community an excellent opportunity to stay aware of current trends.

Kenneth D., Director, FLAMMA

Preliminary Agenda

Plenary Keynote

Chemotype Coverage in Fragment, Phenotypic, & Deorphanization Screens

Brian K. Shoichet, Ph.D., Professor, Department of Pharmaceutical Chemistry, University of California, San Francisco

BCL Proteins and Partners 

Targeting MCL1 for the Treatment of Cancer

Michael H. Serrano-Wu, Ph.D., Director, Medicinal Chemistry, Center for the Development of Therapeutics, Broad Institute

Discovery and Structure-Based Optimization of Novel Small Molecule Mcl-1 Inhibitors

Zaneta Nikolovska-Coleska, Ph.D., Assistant Professor, Pathology, University of Michigan Medical School

Modulators of PUMA: BCL2 Interactions Discovered Using High-Throughput BRET2 and Mammalian-2-Hybrid Assays

Mary Ellen Digan, Ph.D., Senior Research Investigator I, Center for Proteomic Chemistry, Novartis Institutes for Biomedical Research, Inc.

More PPIs Involved in Cancer 

Allosteric Modulation of the AAA ATPase p97: Role in Cancer and Neurodegeneration

Michelle Arkin, Ph.D., Associate Professor, Pharmaceutical Chemistry, University of California, San Francisco

Targeting the NPM1 and FOXM1 Interaction as a Novel Anticancer Therapy

Andrei Gartel, Ph.D., Associate Professor, Medicine, University of Illinois Chicago

Macrocycles that Modulate the C-Terminus of HSP90: A New Mechanism for Inhibiting Protein Folding

Shelli Mcalpine, Ph.D., Professor, Chemistry, University of New South Wales

Structural and Biophysical Studies of Novel, Potent HDM2-p53 Antagonists

Mark McCoy, Ph.D., Principal Scientist, Structural Chemistry, Merck

Case Study: Fragment Approach for a PPI Cancer Target

Ben Davis, Ph.D., Research Fellow, Vernalis


Non-Cancer PPI Targets 

Case Study: Optimization of a Low Affinity Fragment for a PPI Drug Target

Doug Beshore, Ph.D., Associate Director, Medicinal Chemistry, Merck

Homology Models of the HIV-1 Attachment Inhibitor BMS-626529 Bound to GP120 Suggest a Unique Mechanism of Action

David Langley, Ph.D., Senior Scientist, Computational Chemistry, Bristol-Myers Squibb Co. 

Assessing Flexibility and Druggability of PPIs Using Molecular Dynamics

Woody Sherman, Ph.D., Vice President, Applications Science, Schrödinger

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