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 3 

September 23: Characterization and Quantification of Histone Modifications Short Course 8 

September 24 - 25: Targeting Histone Methyltransferases Conference 

September 25 - 26: Targeting Histone Demethylases Conference 


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Wednesday, September 25

11:50 am Registration

1:30 pm Chairperson’s Opening Remarks

 

1:40 Plenary Keynote Speakers

Stuart L. Schreiber
Towards a Patient-Based Drug Discovery
   

Stuart L. Schreiber, Ph.D., Director, Chemical Biology, Founding Member, Broad Institute of Harvard and MIT; Howard Hughes Medical Institute Investigator; Morris Loeb Professor of Chemistry and Chemical Biology, Harvard University

 Paul L. Feldman
Enteroendocrine Drug Discovery for Treatment of Metabolic Diseases
 

Paul L. Feldman, Ph.D., Senior Vice President, GlaxoSmithKline



For complete Keynote details, click here
 

 

3:10 Coffee Break in the Exhibit Hall with Poster Viewing


TOWARDS DISCOVERY OF HIGH-QUALITY DEMETHYLASE PROBES

3:50 pm Chairperson’s Opening Remarks

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

4:00 Targeting H3K9me2 Writers and Erasers

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

I will discuss the design of potent inhibitors of H3K9me2 writers (G9a/GLP) and erasers (PHF8/KIAA1718) by adding a lysine or methyl-lysine mimic.

 

4:30 Selected Poster Presentation: Identification and Characterization of Histone Demethylase Inhibitors with Diverse Mechanisms

Amy Gustafson, Senior Research Associate, Genentech

4:45 Selected Poster Presentation: Understanding LSD1/CoREST Dynamics Using Enhanced Sampling Simulation

Nadeem A. Vellore, Ph.D., Fellow, Medicine Chemistry, College of Pharmacy, University of Utah

5:00 Structure and Specificity of JMJD2 Histone Demethylases

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

The human JMJD2 family of lysine demethylases displays dual site selectivity toward trimethylatedLys9 and Lys36 in histone H3 (H3K9me3 and H3K36me3), with the exception of JMJD2D that is specific for H3K9me3. To elucidate the molecular basis for the differences in methylation site specificity within the JMJD2 family, we determined the crystal structure of a JMJD2D:H3K9me3 peptide complex and compared it to structures of JMJD2A bound H3K9me3 and H3K36me3 peptides. These structural comparisons coupled with kinetics analysis of JMJD2A and JMJD2D demonstrated that subtle variations in the histone binding clefts of the JMJD2 demethylases impart substantial differences in their respective methylation site specificities.These studies will inform the design of inhibitors that selectively target specific JMJD2 homologs to treat JMJD2-linked cancers and other diseases.

5:30 Strategies for Identifying New Chemical Probes for Histone Lysine Demethylases

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

Here we present past, present and future work in our group, with focus on discovery and synthesis of new chemical probes and inhibitors for the histone lysine demethylases KDM4 and LSD. The work includes small molecules, substrate-based inhibitors and DNA-encoded peptide libraries, to obtain selective inhibitors.We are presenting three strategies in one presentation. Evidence how, through these strategies, sub-type selective probes and inhibitors can be found. Two methods (H/D-Exchange and DNA-encoded peptide libraries) that to our knowledge have not been published on epigenetic targets yet, will be covered, showing that these techniques should be incorporated into labs, worldwide.

6:00 Nitric Oxide is an Endogenously Produced Epigenetic Regulatory Molecule

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

We have recently demonstrated 3 novel and distinct mechanisms whereby the free radical nitric oxide (NO) can affect histone methylation patterns: direct inhibition of JMJC-demethylase activity, reduction in iron cofactor availability, and regulation methyl-modifying enzyme gene expression. This model is the first description of NO as an endogenously produced epigenetic regulatory modulator and provides a novel explanation for non-classical gene regulation by NO.

6:30 Close of Day

 

 

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2014 Discovery on Target Brochure  

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PREMIER SPONSORS 

Cellecta 

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SPONSORSHIPS & EXHIBITS 

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
781-972-5483
jstroup@healthtech.com 

2014 Discovery On Target CAG 

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CONFERENCES


October 8 – 9

Targeting Epigenetic Readers and
Chromatin Remodelers
 

Targeting the Ubiquitin Proteasome System  

Big Data Analytics and Solutions  

GPCR-Based Drug Discovery  

RNAi for Functional Genomics Screening
– Part 1
 

Protein-Protein Interactions as Drug Targets  

Antibodies Against Membrane Protein Targets
– Part 1
 


October 9 – 10

Targeting Histone Methyltransferases and Demethylases  

Screening Drug Transporter Proteins  

Maximizing Efficiency in Discovery  

GPCR-Targeted Therapeutics  

Genome Editing for Functional Genomics
Screens – Part 2
 

Cancer Metabolism  

Antibodies Against Membrane Protein Targets
– Part 2
 


SYMPOSIUM


October 7

Next Generation Histone Deacetylase Inhibitors  


SHORT COURSES


October 7

SC1: Designing Scalable Software Systems for Big Data Analytics  

SC2: Approaches for Biologically-Relevant Chemical Diversity  

SC3: Setting Up Effective RNAi Screens: From Design to Data to Validation  

SC4: Targeting Protein-Protein Interactions  

SC5: GPCR Structure-Based Drug Discovery  

SC6: Advances in Metagenomic Drug Discovery for New Anti-Infective Agents  

SC7: Targeting of GPCRs with Monoclonal Antibodies  

SC8: A Primer to Gene Editing: Tools and Applications  

SC9: Introduction to Targeted Covalent Inhibitors  


October 9

SC10: Setting Up Effective Functional Screens Using 3D Cell Cultures  

SC11: Integration of BDDCS and Extended Clearance Principles  

SC12: Introduction to Allosteric Modulators and Biased Ligands of GPCRs  

SC13: Introduction to Drug Metabolism