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.
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
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Cambridge Healthtech Institute
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