Targeting epigenetic modifiers and readers, particularly histone methyltransferases, demethylases and bromodomain-containing proteins have recently set the foundation for a new generation of anti-cancer drugs. Over the past few years, several companies have developed and successfully moved novel compounds targeting EZH2, DOT1L, LSD1, and a collection of BET bromodomain inhibitors into clinical studies. As these compounds continue to progress, developers are now focused on the discovery of new targets and designing novel inhibitors to expand into this robust target space. Of particular interest for discovery are non-BET bromodomain proteins, methyl-lysine readers, arginine methyltransferases, and JmjC-domain containing demethylases.
Cambridge Healthtech Institute has extensively covered the progression of second-generation epigenetic inhibitor discovery and development by establishing the first and longest-running series of meetings specifically focused on enhancing epigenetic drug discovery. We are once again excited to host the industry’s largest drug discovery event focused on targeting the chromatin-modifying enzymes of histone methyltransferases, demethylases and bromodomain-containing proteins. The back-to-back Targeting Histone Methyltransferases and Demethylases and Targeting Epigenetic Readers and Chromatin Remodelers meetings will once again unite academic and industry researchers to discuss novel tools and strategies for targeting these proteins, share the discovery and development of novel inhibitors, and provide updates on preclinical and clinical findings.
Part 2 - Targeting Epigenetic Readers and Chromatin Remodelers
The second part of this series focuses on one of the most exciting areas of discovery research, focused on targeting chromatin modifying proteins, particularly those responsible for the recognition of the histone code written in acetyl and methyl marks. With several clinical trials underway, and many discovery programs initiated, particular interest has been given to targeting the BET family of proteins across a diverse range of therapeutic indications. Widespread efforts have also begun to develop novel chemical matter targeting non-BET bromodomain proteins to assess their therapeutic potential. Most recently, interest and success in developing chemical tools targeting methyl-lysine readers have substantially expanded the possibilities of modulating chromatin states by disrupting epigenetic reading.
Bromodomain Chemical Probes to Explore Epigenetic Pathways
Oleg Fedorov, Ph.D., Group Leader, Biophysics and Biochemical Screening, Structural Genomics Consortium and Target Discovery Institute, University of Oxford
Structure-Based Design of an in vivo BRD9 Probe
Laetitia Martin, Ph.D., Research Laboratory Head & Project Leader, Medicinal Chemistry, Boehringer Ingelheim
Inducible Binding Conformations that Enabled the Identification of Selective in vitro Bromodomain Inhibitors from a Common Scaffold
Terry Crawford, Senior Scientific Researcher, Medicinal Chemistry, Genentech, Inc.
Novel Bromodomain Inhibitors with Broad Activities
Claes Wahlestedt, M.D., Ph.D., Leonard M. Miller Professor & Associate Dean, Therapeutic Innovation, Miller School of Medicine, University of Miami
PHD and YEATS Domains and Their Roles in Epigenetic Mechanisms
Tatiana Kutateladze, Ph.D., Professor, Department of Pharmacology, Anschutz Medical Campus, University of Colorado
Targeting Chromatin Regulation via Methyl-Lysine Reader Chemical Probes
Lindsey Ingerman James, Ph.D., Research Assistant Professor, Center for Integrative Chemical Biology and Drug Discovery, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill
Identification and Validation of CBX2 as a Therapeutic Target
Cheryl D. Helgason, Ph.D., Senior Scientist, Experimental Therapeutics, British Columbia Cancer Agency Research Centre
FEATURED PRESENTATION: CBP/EP300 Bromodomain Inhibition
Robert J. Sims III, Ph.D., Vice President, Biology, Constellation Pharmaceuticals, Inc.
BET Bromodomain Inhibitors in Prostate Cancer
Irfan A. Asangani, Ph.D., Assistant Professor, Cancer Biology, Perelman School of Medicine, University of Pennsylvania
Response and Resistance to BET Bromodomain Inhibitors in Breast Cancer
Kornelia Polyak, M.D., Ph.D., Professor of Medicine, Department of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School
New BET Inhibitor Combination Strategies and Lessons Learned from Clinical Trials Conducted 25 Years Ago
Jonas Nilsson, Ph.D., Professor, Experimental Cancer Surgery, Surgery, Sahlgrenska Cancer Center, University of Gothenburg
For questions or suggestions about the meeting, please contact:
Cambridge Healthtech Institute
T: (+1) 781-972-5454
For sponsorship and exhibit sales information including sponsored podium presentations, contact:
Senior Manager, Business Development
Cambridge Healthtech Institute
T: (+1) 781-972-5483