Targeting Histone Demethylases  

 

ABOUT THIS CONFERENCE 

Once thought to be an irreversible mechanism, our view of histone methylation has changed with the discovery of a new class of druggable enzymes responsible for the removal and maintenance of methyl groups. The past few years have seen much excitement elucidating the functional and therapeutic benefit of modulating genetically aberrant or overexpressed histone demethylase (HDM) enzymes across a selection of diseases. In addition, robust high-throughput screening and hit-finding approaches have progressed, enabling the development of inhibitors, with high activity and potency. Continued efforts require a deepened understanding of the biological consequences of modulation, heightened specificity of screens and hit finding, and ultimately, increased production of small molecule inhibitors for lead development and optimization. The Targeting Histone Demethylases conference will join pharmaceutical, biotech and academic researchers to network, collaborate and discuss practical solutions to challenges, while exploring the expanding arena of HDM therapeutics.

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 Coursee 

September 24 - 25: Targeting Histone Methyltransferases Conference 

September 25 - 26: Targeting Histone Demethylases Conference 


Perturbing the Histone Demethylome: Novel Modulators & Insights into INHIBITION

Targeting the Histone Demethylome

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

 

Targeting Histone Demethylation in Cancer

Ryan Kruger, Ph.D., Manager, Cancer Epigenetics Discovery Performance Unit, Oncology R&D, GlaxoSmithKline Pharmaceuticals

 

Targeting Lysine-Specific Demethylase 1 with Polyamine Analogues to Induce Expression of Aberrantly Silenced Genes

Robert A. Casero, Jr., Ph.D., Professor of Oncology, The Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University School of Medicine

 

Reactivation of Repressed Epigenetic Mechanisms with Small Molecule Inhibitors

Michael McCabe, Ph.D., Investigator, Biology, Cancer Epigenetics Discovery Performance Unit, Oncology R&D, GlaxoSmithKline Pharmaceuticals

 

JARID1 Demethylases as Cancer Targets

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

 

The Therapeutic Potential of Jumonji Histone Demethylase Inhibitors

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

 

 

 

CLINICAL INSIGHTS INTO targeted Therapy

Chromatin Regulators as Therapeutic Targets in Breast Cancer

Kornelia Polyak, M.D., Ph.D., Associate Professor, Department of Medicine, Harvard Medical School; Associate Professor of Medicine, Medical Oncology, Dana-Farber Cancer Institute

 

Chromatin Modification in Reversible Tolerance to Anti-Cancer Drug

Jeffrey Settleman, Ph.D., Senior Director, Discovery Oncology, Genentech

 

Epigenetic Therapy for Cancer Treatment

Lorraine Gudas, Ph.D., Chairman & Revlon Pharmaceutical Professor, Pharmacology and Toxicology, Pharmacology Department, Weill Cornell Medical College

 

Talk Title to be Announced

Igor P. Pogribny, M.D., Ph.D., Principal Research Investigator, Division of Biochemical Toxicology, National Center for Toxicological Research, FDA

 

Epigenetic Reprogramming in Pancreatic Cancer: The Emerging Role of Histone Demethylases

Alexandros Tzatsos, M.D., Ph.D., Instructor, Medicine, Harvard Medical School; Assistant Geneticist, Massachusetts General Hospital Cancer Center

 

 

 

Towards Discovery of High-Quality Demethylase Probes

Targeting H3K9me2 Writers and Erasers

Xiaodong Cheng, Ph.D., Professor of Biochemistry & Georgia Research Alliance Emminent Scholar, Emory University School of Medicine

 

Strategies for Identifying New Chemical Probes for Histone Lysine Demethylases

Brian Lohse, Ph.D., Associate Professor, Drug Design and Pharmacology, University of Copenhagen

 

Structure and Specificity of JMJD2 Histone Demethylases

Raymond C. Trievel, Ph.D., Associate Professor of Biological Chemistry, University of Michigan Medical School

 

Nitric Oxide is an Endogenously Produced Epigenetic Regulatory Molecule

Douglas Thomas, Ph.D., Associate Professor, Medicinal Chemistry, University of Illinois at Chicago