2nd Annual

Epigenetic Inhibitor Discovery

Chemically Modulating Gene Expression

April 21-22, 2015 


Epigenetic drug discovery is one of the fastest growing and potentially groundbreaking target spaces for developers. Over the past few years, a significant increase in small molecule inhibitors chemically modulating enzymatic activity of Histone Methyltransferases (HMTs), Histone Demethylases (HDMs), and disrupting interactions of the BET family bromodomains have rapidly translated into clinical investigation. Now, with apparent safety and efficacy being demonstrated in clinical trials, the opportunity to develop novel chemical tools and inhibitors against the wealth of epigenetic modifiers is ever present. Cambridge Healthtech Institute will once again convene leaders in Epigenetic Inhibitor Discovery to bring forth novel and emerging strategies for inhibition, new bioactive tools and inhibitors, as well as strategies for lead optimization to obtain clinically relevant small molecules. 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.


Great opportunity to share and discuss cutting-edge approaches/aspects in drug discovery.

Fabrizio G., Principal Scientist, AstraZeneca

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


Advances in Developing Novel BET Bromodomain Inhibitors 

Featured Presentation: A Bump-and-Hole Approach to Engineer Controlled Selectivity of BET Bromodomain Chemical Probes

Alessio Ciulli, Ph.D., Reader, Chemical & Structural Biology, BBSRC David Phillips Fellow, College of Life Sciences, University of Dundee

Discovery of Dual PI3K/BRD4 Inhibitors

Donald Durden, M.D., Ph.D., Professor, Vice Chair, Pediatrics, UCSD School of Medicine; CEO and President, SignalRx Pharmaceuticals

Discovery and Development of a Potent Dual TRIM24/BRPF1 Inhibitor, IACS-9571, Using Structure-Based Drug Design

Wylie Palmer, Ph.D., Institute Research Scientist, Institute of Applied Cancer Science, MD Anderson Cancer Center

Discovery and Development of Novel BET Bromodomain Inhibitors

Brian Albrecht, Ph.D., Senior Director, Medicinal Chemistry, Constellation Pharmaceuticals


Discovery and Development of Novel Lysine and Arginine Methyltransferase Inhibitors 

Discovery and Development of Novel Arginine Methyltransferase Inhibitors

Richard Chesworth, Ph.D., Epizyme

Discovery of a Potent and Specific Drug to Inhibit PRMT5 in Hematologic and Solid Tumors

Chenglong Li, Ph.D., Associate Professor, Division of Medicinal Chemistry and Pharmacognosy College of Pharmacy, The Ohio State University Comprehensive Cancer Center

The Discovery and Characterization of A-366, a Potent and Selective Inhibitor of Histone Methyltransferase G9a

Ramzi Sweis, Ph.D., Research Investigator, Discovery Chemistry, AbbVie, Inc.

Epigenetic Inhibitors are Potentially Useful Therapeutics for Acute Leukemia

Yongcheng Song, Ph.D., Associate Professor, Pharmacology, Baylor College of Medicine


Emerging Tools and Strategies for Epigenetic Inhibitor Discovery 

Discovery of Novel Small Molecules and Small Cyclic Peptides as Chemical Tools and Inhibitors, Using DNA Encoded Peptide Libraries for HDMs and HMTs

Brian Lohse, Ph.D., Associate Professor, Drug Design and Pharmacology, University of Copenhagen

In silico Discovery and Experimental Validation of Selective Bromodomain Inhibitors

Amedeo Caflisch, Ph.D., Professor and Chair, Computational Structural Biology, Department of Biochemistry, University of Zurich



For more details on the conference, please contact:
Kip Harry
Conference Producer
Cambridge Healthtech Institute
Phone: (+1) 781-972-5454
Email: kharry@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