Targeting Histone Methyltransferases and Demethylases header

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. 

Who should attend: Executives, Directors, Managers, Group Leaders and Senior Scientists from Pharma, Biotechs, Academia, Government and Healthcare Organizations working in fields such as Drug Discovery, Preclinical Research and Development, Molecular/Cell Biology, Biochemistry, Chemical Genomics/Biology, Structural Biology, Medicinal Chemistry, Pharmacology and Synthetic Chemistry.

If you are interested in presenting, please click here to submit a proposal.

Topics may include, but are not limited to: 


Understanding HMTs and HDMs in Disease 

  • Genetic Abnormalities of HMTs and HDMs in Disease
  • Regulatory Mechanisms Leading to Disease
  • Technological Advances for Interrogating Histone Methylation, Histone Methyltransferases and Demethylases in vivo 


 Discovery to Lead 

  • Strategies for Discovery and Development of Novel Chemical Matter, Including: High-Throughput Screening, Virtual Screening, Fragment/Structure-Based Design, Chemoinformatic Approaches
  • Functional and Structural Analysis of HMTs and HDMs
  • Structure Activity Relationships
  • Optimization to Lead
  • Novel HMT and HDM Inhibitors


Preclinical and Clinical Development 

  • Updates on HMT and HDM Programs in Preclinical and Clinical Stages
  • PK/PD - in vitro and in vivo Target Binding Kinetics 
  • Mechanism of Action 
  • Assessing Efficacy and Toxicity
  • Disease Relevant Preclinical Models and Biomarkers

If you are interested in presenting, please click here to submit a proposal.

The deadline for submission is March 28, 2014. 

All proposals are subject to review by the Scientific Advisory Committee to ensure the highest quality of the conference program.  Please note that due to limited speaking slots, preference is given to pharmaceutical and biotech companies, regulators and those from academia. Additionally, vendors/consultants who provide products and services to these biopharmaceutical companies are offered opportunities for podium presentation slots based on a variety of Corporate Sponsorships. 

For questions or suggestions about the meeting, please contact:    
Kip Harry
Conference Director
Cambridge Healthtech Institute
T: (+1) 781-972-5454

For sponsorship and exhibit sales information including sponsored podium presentations, contact:
Jon Stroup
Manager, Business Development
Cambridge Healthtech Institute
T: (+1) 781-972-5483






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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