Cambridge Healthtech Institute’s 5th Annual
Targeting Histone Methyltransferases and Demethylases
Tools and Strategies for Modulating Histone Methylation

Part of the 14th Annual Discovery on Target Conference
September 20-21, 2016 | Westin Boston Waterfront | Boston, MA


Targeting epigenetic modifiers and readers, particularly histone methyltransferases, demethylases and bromodomain-containing proteins have recently set the foundation for a new generation of anti-cancer drugs. Over the past few years, several companies have developed and successfully moved novel compounds targeting EZH2, DOT1L, LSD1, and a collection of BET bromodomain inhibitors into clinical studies. As these compounds continue to progress, developers are now focused on the discovery of new targets and designing novel inhibitors to expand into this robust target space. Of particular interest for discovery are non-BET bromodomain proteins, chromodomain proteins, and methyl-lysine readers, arginine methyltransferases, and JmjC-domain containing demethylases.

Cambridge Healthtech Institute has extensively covered the progression of second-generation epigenetic inhibitor discovery and development by establishing the first and longest-running series of meetings specifically focused on enhancing epigenetic drug discovery. We are once again excited to host the industry’s largest drug discovery event focused on targeting the chromatin-modifying enzymes of histone methyltransferases, demethylases and bromodomain-containing proteins. The back-to-back Targeting Histone Methyltransferases and Demethylases and Targeting Epigenetic Readers and Chromatin Remodelers meetings will once again unite academic and industry researchers to discuss novel tools and strategies for targeting these proteins, share the discovery and development of novel inhibitors, as well and provide updates on preclinical and clinical findings. 

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

Part 1 - Targeting Histone Methyltransferases and Demethylases

The first part of this series focuses on targeting the histone methylome as a therapeutic strategy. Adding to the more established series of histone methyltransferase targets, histone demethylases of both JmjC and CoREST domains have also advanced into clinical development and are now showing favorable clinical outcomes. Notably, recent interest and success in developing inhibitors against arginine methyltranslferase enzymes has substantially deepened the possibilities of regulating chromatin environments via histone methylation.

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 the 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, Target Protein-Protein Interactions
  • Functional and Structural Analysis of HMTs and HDMs
  • Structure Activity Relationships
  • Optimization to Lead
  • Novel HMT and HDM Inhibitors
  • Preclinical Studies on Selective Inhibition of Readers/Remodelers

Preclinical and Clinical Development

  • Preclinical Studies on Novel Inhibitions Targeting HMTs and HDMs
  • Updates on HMT and HDM Programs in Preclinical and Clinical Stages

If you are interested in speaking, please click here.

Click here to register for a special early-bird discounted rate.

The deadline for submission is March 4, 2016.

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
E: kharry@healthtech.com

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