Targeting Histone Demethylases  



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.



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


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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 Short Courses

2015 Discovery on Target Brochure  





Molecular Sensing

Rosa Drug Development Advisors






The exhibit hall was sold out in 2014, so please contact us early to reserve your place. To customize your sponsorship or exhibit package for 2015, contact:

Jon Stroup
Sr. Business Development Manager


September 21 

Next-Generation Histone Deacetylase Inhibitors Symposia 

Strategies for Rare Diseases Symposia 

September 22 

Developing CRISPR-Based Therapies Symposia 

September 22 - 23 

Targeting Epigenetic Readers and Chromatin Remodelers 

Targeting the Ubiquitin Proteasome System 

Targeting the Microbiome 

GPCR - Based Drug Discovery - Part 1 

Antibodies Against Membrane Protein Targets - Part 1 

RNAi for Functional Genomics Screening 

Gene Therapy Breakthroughs 

Targeting Ocular Disorders 

September 23 - 24 

Targeting Histone Methyltransferases and Demethylases 

Targeting the Unfolded Protein Response 

Kinase Inhibitor Discovery 

GPCR-Based Drug Discovery - Part 2 

Antibodies Against Membrane Protein Targets - Part 2 

New Frontiers in Gene Editing 

Quantitative Systems Pharmacology 

Short Courses 

SC1: Cancer Metabolism: Pathways, Targets and Clinical Updates 

SC2: Leveraging Data and Analytics for Drug DiSCovery 

SC3: Setting Up Effective Rnai SCreens: From Design to Data to Validation 

SC4: Phenotypic SCreening and Chemical Probe Development 

SC5: GPCR Structure-based Drug Discovery 

SC6: Targeting of GPCRs with Monoclonal Antibodies 

SC7: Setting Up Effective Functional SCreens Using 3D Cell Cultures 

SC8: Targeting Protein-protein Interactions: Biophysical Approaches 

SC9: Preclinical Animal Models for Ocular Indications 

SC10: Introduction to Allosteric Modulators and Biased Ligands of GPCRs 

SC11: Introduction to Targeted Covalent Inhibitors 

SC12: Assays and High-throughput SCreening for Novel Epigenetic Inhibitors 

SC13: Gamification and Drug Target Challenges 

SC14: A Primer to Gene Editing: Tools and Applications 

SC15: Using Mechanistic Physiological Models In Drug Development