Targeting PPIs for Therapeutic Interventions
April 23-24, 2014
Targeting the non-catalytic site of protein-protein interactions (PPIs) with small molecules has enabled drug discovery to move beyond the typical enzyme targets such as proteases and kinases and address disease-state relevant regulatory complexes of biological processes such as intracellular signal transduction, transcription, immuno-modulation, epigenetic modifications and protein stability. However targeting PPIs pose unique challenges because the targets’ structure (an interaction site between two proteins) is often not known and is usually a larger area with different physico-chemical properties than a ‘catalytic site’. Cambridge Healthtech Institute’s seventh annual Protein-Protein Interactions meeting will highlight the different disease areas where targeting PPIs is showing promise and will bring colleagues together to discuss lead optimization challenges for the medicinal chemist. Hear case studies of PPI-targeted compounds that are progressing in drug development or not, with a focus on the kinds of roadblocks the compounds encountered.
David Fry, Ph.D., Vice President, Protein Chemistry, The Chemistry Research Solution (TCRS), LLC
Edward R. Zartler, Ph.D., President & CSO Quantum Tessera Consulting
Small Molecule Disruptors of the GK-GKRP Interaction
Kate Ashton, Ph.D., Senior Scientist, Medicinal Chemistry, Amgen, Inc.
Targeting Intracellular Protein-Protein Interactions with Engineered Cyclotides
Julio Camarero, Ph.D., Associate Professor, Pharmacology and Pharmaceutical Sciences/Chemistry, University of Southern California
A New Approach to Protein-Ligand Binding as Illustrated in Optimization of Small Molecule Drug Candidates Targeting PPIs
José Duca, Ph.D., Head, CADD in Cambridge, Novartis Institutes for BioMedical Research, Inc.
Antibody-Guided Discovery of Small Molecule Protein-Protein-Interaction Inhibitors
Wolfgang Fecke, Ph.D., Group Leader, Primary Pharmacology, UCB Pharma
Allosteric Regulators Targeting Higher-Order Proteasome Assemblies in the Treatment of Cancer
Maria Gaczynska, Ph.D., Associate Professor, Molecular Medicine, University of Texas Health Science Center at San Antonio
Allosteric Inhibitors of the Heat Shock Protein 70 (Hsp70) Complex
Jason E. Gestwicki, Ph.D., Associate Professor, Department of Pharmaceutical Chemistry, University of California at San Francisco
Direct Inhibition of β-Catenin with Small Molecules
Elmar Nurmemmedov, Ph.D., Scientist, Molecular Experimental Medicine, The Scripps Research Institute
Discovery of Potent and Selective Piperidinone Inhibitors of the MDM2-p53 Interaction
Daqing Sun, Ph.D., Principal Scientist, Medicinal Chemistry, Amgen
The Design and Synthesis of A-Helix Mimetics as PPI Inhibitors
Roman Kombarov, Ph.D., Project Manager, ASINEX