Targeting Histone Methyltransferases and Demethylases Header

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 1 - Targeting Histone Methyltransferases and Demethylases

The first part of this series focuses on targeting the histone methylome as a therapeutic strategy. Adding to the more established series of histone methyltransferase targets, histone demethylases of both JmjC and CoREST domains have also advanced into clinical development and are now showing favorable clinical outcomes. Notably, recent interest and success in developing inhibitors against arginine methyltransferase enzymes, JmJC domain demethylases and lysine-methyl readers have substantially deepened the possibilities of regulating chromatin environments via histone methylation.

Preliminary Agenda


Structure-Based Approaches to Identify Novel and Specific Inhibitors for Different Subfamilies of Jumonji Demethylases

Udo Oppermann, Ph.D., Professor, Molecular Biology; Director, Molecular Laboratory Sciences, Botnar Research Centre; Principal Investigator, Epigenetics and Metabolism, Structural Genomics Consortium, University of Oxford

Structure, Kinetics and Inhibition of KDM5A, a Key Drug Target in Histone H3 Lysine 4 Demethylation

Xiaodong Cheng, Ph.D., Professor, Department of Biochemistry, Emory University

Characterization of a Novel LSD1 Inhibitor in Preclinical Models of Cancer

Sang Hyun Lee, Ph.D., Principal Scientist, Pharmacology, Incyte Corporation

Targeting Histone Lysine Methylation for Cancer Therapy

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

Development of Lysine-Specific Demethylase Inhibitors for Oncological and Neurodegenerative Disease

Tamara Maes, Ph.D., Co-Founder, Vice President & CSO, Oryzon Genomics


Substrate Specificity of Histone Methyltransferases

Masoud Vedadi, Ph.D., Principal Investigator, Molecular Biophysics, Structural Genomics Consortium; Assistant Professor, Department of Pharmacology and Toxicology, University of Toronto

Targeting Protein Methyltransferases via Novel Models of Interaction

Minkui Luo, Ph.D., Associate Member & Associate Professor, Chemical Biology Program, Memorial Sloan Kettering Cancer Center

Fragment-Based Discovery of WDR5-MLL1 Disruptors

Shaun Stauffer, Ph.D., Professor, Pharmacology; Associate Director, Medicinal Chemistry, Vanderbilt University

Discovery of Selective Inhibitors for Protein Methyltransferases

Jing Liu, Ph.D., Assistant Professor, Structural and Chemical Biology, Icahn School of Medicine at Mount Sinai


Targeting Histone Lysine Methylation in Cancer

Patrick Trojer, Ph.D., Vice President, Constellation Pharmaceuticals, Inc.

Talk Title to be Announced

Jesse Smith, Ph.D., Vice President, Biological Sciences, Epizyme

For questions or suggestions about the meeting, please contact:
Kip Harry
Conference Director
Cambridge Healthtech Institute
T: (+1) 781-972-5454

For sponsorship and exhibit sales information including sponsored podium presentations, contact:
Jon Stroup
Senior Manager, Business Development
Cambridge Healthtech Institute
T: (+1) 781-972-5483