Epigenetic Inhibitor Discovery
A New Frontier in Drug Development
April 23-24, 2014
Within the past few years, an expanding collection of epigenetic modulators - spanning multiple classes and disease implications - have been positioned as promising targets for therapeutic development. Since the approval of first-generation epigenetic therapies, an increasing amount of chemically tractable epigenetic targets, such as Histone Deacetylases (HDACs), Histone Methyltransferases (HMTs), Histone Demethylases (HDMs), and a distinct set of chromatin readers - the BET family bromodomains - have given rise to novel inhibitors that are now in preclinical and clinical development. However, obtaining potent, highly-selective and cell-active inhibitors requires skillful utilization of varied assays and screening methods, such as high-throughput screening (HTS), focused screening, knowledge/fragment-based approaches, and phenotypic assays to efficiently navigate lead discovery of epigenetic targets. Cambridge Healthtech Institute is proud to announce the inaugural Epigenetic Inhibitor Discovery conference, gathering a diverse cross-section of academic and industry leaders actively working on developing epigenetic inhibitors.
Discovery and Optimization of BET Bromodomain Inhibitors
Brian Albrecht, Ph.D., Senior Director, Medicinal Chemistry, Constellation Pharmaceuticals
Screening for Inhibitors of Bromodomain 4 … Have We Learned Something? … You BET!
Paul Bonin, Principal Scientist, Assay Development and Pharmacology, Primary Pharmacology Group, Pfizer, Inc.
Cracking the Histone Code: Development of Inhibitors of the Bromodomain-Histone Interaction
Stuart Conway, Ph.D., Associate Professor, Chemistry, University of Oxford
Targeting Bromodomains - The Validity of High-Throughput Virtual Screening in Epigenetic Drug Discovery
Stefan Günther, Ph.D., Professor, Pharmaceutical Bioinformatics, Institute of Pharmaceutical Sciences, University Freiburg
Defining the Functional Consequences of Isoform Specific Inhibition of the Class I HDACs Using a Chemical Genetics Approach
Edward Holson, Ph.D., Director, Medicinal Chemistry, Stanley Center for Psychiatric Research, The Broad Institute of MIT and Harvard
A Multifaceted Strategy for Discovering Chemical Probes of Histone Methyltransferases
Jian Jin, Ph.D., Associate Professor and Director, Medicinal Chemistry, Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill
Chemical Probes to Explore Epigenetic Pathways
Susanne Muller-Knapp, Ph.D., Epigenetic Project Manager, Structural Genomics Consortium (SGC), Oxford
Targeting Epigenetic Readers for Cancer Therapy
Jun Qi, Ph.D., Senior Research Scientist, Medical Oncology, Dana-Farber Cancer Institute
Chemical Probes for Histone Demethylases
Xiang Wang, Ph.D., Assistant Professor, Chemistry and Biochemistry, University of Colorado at Boulder
Discovery of Histone Lysine Demethylase Inhibitors
Takayoshi Suzuki, Ph.D., Professor, Graduate School of Medical Science, Kyoto Prefectural University of Medicine