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


Cambridge Healthtech Institute’s 4th Annual
Targeting Epigenetic Readers and Chromatin Remodelers
Targeting Protein-Protein Interactions of Epigenetic Readers

Part of the 14th Annual Discovery on Target Conference
September 21-22, 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.

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

Targeting Histone Methyltransferases and Demethylases

Targeting the histone methylome as a therapeutic strategy has quickly captured the interest of developers worldwide due to the genetic and over-expression abnormalities displayed in a variety of human cancers, as well as the chemically tractable nature of modifying enzymes. 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, a surge of interest and success in developing inhibitors against arginine methyltranslferase enzymes has substantially deepened the possibilities of regulating chromatin environments via histone methylation, and thereby expanding this already robust target space.

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, Chemoinformatic Approaches
  • Functional and Structural Analysis of HMTs and HDMs
  • Structure Activity Relationships
  • Optimization to Lead
  • Novel HMT and HDM Inhibitors

Pre-Clinical and Clinical Development

  • Updates on HMT and HDM Programs in Preclinical and Clinical Stages
  • Assessing Efficacy and Safety

Targeting Epigenetic Readers and Chromatin Remodelers

One of the most recent and exciting areas of discovery research centers around targeting chromatin modifying proteins, particularly those responsible for the recognition of the histone code written in acetyl and methyl marks. With several clinical trials underway, and countless discovery programs initiated, particular interest has been given to targeting the BET family of proteins across a diverse range of therapeutic indications. Advances in probe development now allows for individual and polypharmacological targeting of BET and non-BET proteins, thus given rise to inhibitors modulating various disease pathways, creating novel phenotypic output, and providing a better understanding as to the individual roles of chromatin-associated proteins in human physiology and disease.

Topics may include, but are not limited to:

Target Identification and Validation

  • Targeting Chromatin Remodelers, BET bromodomains, Ph.D., Tudor, Chromo, PWWP and MBT domains
  • Novel Reader Targets with Therapeutic Implications in Cancer and Inflammation
  • Novel Chromatin Remolding Targets with Therapeutic Implications in Cancer and Inflammation
  • Selective Inhibition of Readers/Remodelers and Cellular Response

Discovery to Lead

  • Structural Characterization of Reader Domains and Remodeler Subunits
  • High-Throughput Profiling and Screening for Inhibitors
  • Virtual Screening
  • Phenotypic Screening
  • Fragment/Structure-Based Design
  • Protein-Protein Interaction Strategies
  • Development of High-Quality Chemical Probes/Scaffolds
  • Discovery of Novel BET and Non-BET inhibitors
  • Lead Optimization
  • Dual Inhibitors

Pre-Clinical and Clinical Development

  • Updates on HMT and HDM Programs in Preclinical and Clinical Stages
  • Assessing Efficacy and Safety

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

Call for Speakers

 

Arrow DownCONFERENCE-AT-A-GLANCE

Arrow DownDOWNLOAD 2015 BROCHURE

Arrow Overshort courses

Arrow OverVIEW ALL SPONSORS

Arrow OverVIEW MEDIA PARTNERS


SPONSORSHIPS & EXHIBITS

The exhibit hall was sold out in 2015, so please contact us early to reserve your place. To customize your sponsorship or exhibit package for 2016, contact:

Jon Stroup
Sr. Business Development Manager
781-972-5483
jstroup@healthtech.com

 

DOT-Vid-recap