3rd Annual

Epigenetic Inhibitor Discovery

Targeting Histone Methyltransferases, Demethylases and Bromodomains

April 19-20, 2016

Epigenetic Inhibitor Discovery icon  

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 and methyl lysine readers; arginine methyltransferases; and JmjC-domain containing demethylases.

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.

Preliminary Agenda

Design and Development of Bromodomain Inhibitors

New Synthetic Routes to Triazolo-Benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition

Alessio Ciulli, Ph.D., Associate Professor & Principal Investigator, Chemical & Structural Biology, College of Life Sciences, University of Dundee

Design and Development of Novel BET Bromodomain Inhibitors

Eric Campeau, Ph.D., PMP, Director of Biology, Zenith Epigenetics

In silico Design of Dual PI-3 Kinase/BET Bromodomain Inhibitors; Structural Details for Binding BD1

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

Discovery of Novel Histone Demethylase Inhibitors

Novel Dual Inhibitors of LSD1-HDAC for Treatment of Multiple Myeloma and Other Cancers

Dhanalakshmi Sivanandhan, Ph.D., Principal Scientist & Assistant Director, Jubilant Biosys

Small Molecule Epigenetic Modulators for the Treatment of Cardiovascular Disorders

Patrick M Woster, Ph.D., Endowed Chair, Drug Discovery; Professor, Pharmaceutical and Biomedical Sciences, College of Pharmacy, Medical University of South Carolina

Discovery of Histone Lysine Demethylase Inhibitors

Takayoshi Suzuki, Ph.D., Professor, Graduate School of Medical Science, Kyoto Prefectural University of Medicine

Targeting Histone and DNA Methylation

Profiling the ‘Methylome’ Targets of the Histone Lysine Methyltransferases: DOT1L

Matthew Fuchter, Ph.D., Reader, Chemistry, Department of Chemistry, Imperial College London

A Rational Approach for the Discovery of Inhibitors of NSD2 for the Treatment of Cancer

Christian A. G. N. Montalbetti, Ph.D., Head, Chemistry, Inventiva‬

Chemical Tools to Modulate Gene Expression by Targeting DNA Methylation

Paola B. Arimondo, Ph.D., Director, Research, ETaC - Epigenetic Targeting of Cancer, CNRS

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

For partnering & sponsorship information, please contact:
Carolyn Benton
Business Development Manager
Cambridge Healthtech Institute
Phone: (+1) 781-972-5412
Email: cbenton@healthtech.com