Targeting Histone Methyltransferases and Demethylases header

Suggested Event Package:

October 7

*Short Course: Biologically-Relevant Chemical Diversity 

*Short Course: Heat Shock Protein Inhibitor Discovery 

October 8-9: Targeting Epigenetic Readers and Chromatin Remodelers Conference 

October 9-10: Targeting Histone Methyltransferases and Demethylases Conference 

*Separate registration is required

About This Conference:

Epigenetic drug development has quickly gained widespread interest due to the apparent therapeutic efficacy now being demonstrated in preclinical and clinical studies. Drugging the histone methylome remains at the center of discovery with new findings of somatic mutations and deregulation of genes coding for Histone Methyltransferase and Demethylase enzymes. This, in combination with the chemically tractable nature of these enzymes, is providing a strong impetus for therapeutic intervention via pharmacological modulation. Notably, over the past year a rapid expansion of novel demethylase targets, particularly in the Jumonji C domain-containing demethylase family, has substantially deepened the possibilities of regulating chromatin environments via histone methylation. Histone demethylases are now joining the more-established histone methyltransferase targets for clinical development.

As the suite of inhibitors targeting methylation-controlling enzymes expands, challenges can be seen in designing new compounds with higher affinity and specificity; elucidating mechanisms of action of these drugs to shed light on target function in disease; and an overall rigorous approach to target validation in preclinical studies to assess efficacy and toxicity.

Cambridge Healthtech Institute will once again convene leaders in epigenetic drug development to provide updates on preclinical and clinical programs, introduce novel targets and chemical matter, and discuss strategies for targeting and validating histone methyltransferases and demethylases.

Mechanisms Regulating Gene Expression and Tumorigenesis

Disorders of Histone Methylation in Hematological Malignancy

Jonathan D. Licht, M.D., Johanna Dobe Professor & Chief, Division of Hematology/Oncology, Feinberg School of Medicine, Northwestern University

Epigenetic Reprogramming by Tumor-Derived EZH2 Gain-of-Function Mutations Promotes Aggressive 3D Cell Morphologies and Enhances Melanoma Tumor Growth

Robert Rollins, Ph.D., Principal Scientist, Oncology, Pfizer

JARID1/KDM5 Demethylases as Cancer Targets

Qin Yan, Ph.D., Assistant Professor, Pathology, School of Medicine, Yale University

Pharmacological Modulation: Mechanisms of Action, Efficacy and Toxicity Studies

Targeting Histone Methyltransferases in Cancer Therapy

Jesse Smith, Ph.D., Executive Director, Biological Sciences, Epizyme

Talk Title to be Announced

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

Development of Histone Demethylase Inhibitors for Oncological and Neurodegenerative Disease

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

Therapeutic Inhibitors of the KDM5 Histone Demethylases

Peter Staller, Ph.D., Director, Oncology Research, EpiTherapeutics ApS

Discovery and Development of Novel Bioactive Chemical Matter


Christopher Schofield, Ph.D., Professor, Organic Chemistry, Department of Chemistry, University of Oxford

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

A Dual Approach to Develop Inhibitors of Protein Methyltransferases

Minkui Luo, Ph.D., Assistant Member & Assistant Professor, Molecular Pharmacology and Chemistry, Memorial Sloan-Kettering Cancer Center





green arrow VIEW ALL SPONSORS 



The exhibit hall was sold out in 2013, so please contact us early to reserve your place. To customize your sponsorship or exhibit package for 2014, contact:

Jon Stroup
Business Development Manager