Targeting Histone Methyltransferases  

 

ABOUT THIS CONFERENCE 

 

To date, several widespread and promising second-generation epigenetic drug development campaigns have been dedicated to the modulation of histone methylation. In this post-genomic era of drug development, the identification of genetic mutations and overexpression of histone methyltransferases (HMTs) across a variety of cancer types provide unique validation for selective and tumor-specific targeting of methyltransferase enzymes. Significant progress has been seen in the development of potent, selective and tolerable inhibitors against several HMTs, including the first inhibitor to enter human clinical trials. Yet, with several HMT targets and inhibitors poised for further development, there is great need for advanced tools to perturb methylation environments in normal and disease states. Building on the success of last year, Cambridge Healthtech Institute's Second Annual Targeting Histone Methyltransferases conference is the preeminent event for HMTi development, gathering a diverse cross-section of academic and industry leaders actively working on advancing second-generation epigenetic therapies.

SUGGESTED EVENT PACKAGE:

 

 

September 23: Biochemical and Structure-Based Approaches to Epigenetic Drug Discovery Short Course 

September 23: Characterization and Quantification of Histone Modifications Short Course 

September 24 - 25: Targeting Histone Methyltransferases Conference 

September 25 - 26: Targeting Histone Demethylases Conference Conference 


FEATURED OPENING SESSION: LEADERS IN EPIGENETIC DRUG DISCOVERY 

Featured Presentation

Peter J. Tummino, Ph.D., Head, Biology, Cancer Epigenetics Discovery Performance Unit, Oncology R&D, GlaxoSmithKline Pharmaceuticals

 

Featured Presentation

Cheryl H. Arrowsmith, Ph.D., Chief Scientist, Structural Genomics Consortium; Professor, Medical Biophysics; Canada Research Chair, Structural Proteomics, University of Toronto

 

 

 

State of the Art in lysine Methyltransferase Inhibitors

A First-in-Class Chemical Probe for SETD7

Dafydd Owen, Ph.D., Associate Research Fellow, Medicinal Chemistry, Pfizer Worldwide R&D

 

Targeting Histone Methyltransferases in Cancer Therapy

Sarah Knutson, Ph.D., Senior Scientist, Biological Sciences, Epizyme

 

Therapeutic Applications of EZH2 Small Molecule Inhibitors

Patrick Trojer, Ph.D., Senior Director&Head, Biology, Constellation Pharmaceuticals

 

 

 

mechanistic insights into oncogenesis and Targeted Therapy

Targeting H3K4 Methylation by the MLL1 Complex for the Treatment of Mixed Lineage Leukemia

Yali Dou, Ph.D., Associate Professor, Pathology, University of Michigan

 

Small Molecule Epigenetic Intervention of Disease via Histone Lysine Methyltransferases

Matthew Fuchter, Ph.D., Senior Lecturer, Synthetic and Medicinal Chemistry, Department of Chemistry, Imperial College London 

 

Harnessing EZH2 Enzymatic Activities by Targeting PRC2 Associated Cofactors

Gang "Greg" Wang, Ph.D., Assistant Professor, Department of Biochemistry & Biophysics, UNC Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill

 

Targeting the Histone Methyltransferase MMSET in Cancer

Irfan Asangani, Ph.D., Research Investigator, Pathology, Michigan Center for Translational Pathology

 

 

 

Approaches for HMT Inhibitor Development

 

Chemical Tractability of Protein Methyltransferases: Lessons Learned from Protein Structures and Screening Campaigns

Matthieu Schapira, Ph.D., Principal Investigator, Computational Chemistry, Structural Genomics Consortium; Associate Professor, Department of Pharmacology & Toxicology, University of Toronto

 

Targeting the MLL1-WDR5 Protein-Protein Interaction as a Novel Therapeutic Strategy for Acute Leukemia Harboring MLL1 Fusion Protein

Shaomeng Wang, Ph.D., Warner-Lambert/Parke-Davis Professor in Medicine, Pharmacology and Medicinal Chemistry; Director, Cancer Drug Discovery Program; Co-Director, Molecular Therapeutics Program; University of Michigan Comprehensive Cancer Center

 

Histone Methyltransferase Inhibitors Targeting Cancer

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

 

Talk Title to be Announced

Stephen Antonysamy, Ph.D., Principal Research Scientist, Structural Biology, Eli Lilly

 

Global Analysis of Methylation and Functional Annotation of Methyltransferases: Chemo-Enzymatic Approaches

Zhaohui Sunny Zhou, Ph.D., Faculty Fellow, Barnett Institute of Chemical and Biological Analysis;

Associate Professor, Department of Chemistry and Chemical Biology, Northeastern University