Structure-Based Design of Novel Inhibitors of the MCL-1’s Protein-Protein Interaction
Xin Huang, PhD, Principal Scientist, Department of Molecular Engineering, Amgen

Kip Harry, Conference Director at Cambridge Healthtech Institute discusses epigenetic drug discovery with Dr. Matthew Fuchter, Senior Lecturer of Synthetic and Medicinal Chemistry at the Imperial College London.

Questions Include:

• From an inhibitor development standpoint, what methods do you use for discovery to lead?
• Why do you choose natural products to aid in targeting epigenetic modifiers and is there limited chemical matter in this space?
• What opportunities are there for infectious disease and other indications?
• What has ignited all this interest in developing second generation epigenetic inhibitors – particularly targeting Histone Methyltransferases, Demethylases and BET Bromodomains?
• Have we learned anything from approved compounds?
• What are major challenges seen in the development of novel epigenetic inhibitors?
• What about safety and toxicity of compounds – is this a major concern?
• What talks/topics are you looking forward to during the Epigenetic Inhibitor Discovery Meeting?
• How quickly can we expect to see these novel medicines reaching patients in need?
• Is combination therapy where we will see the greatest impact in this space?
• Some compare the epigenetic enzymes to kinases, where they will provide years of fertile grounds for discovery. What do you think?

Dr. Erlanson of Carmot Therapeutics and Dr. Zartler of Tessera Consulting speak with CHI's Dr. Shah on March 14, 2014 about new strategies for fragment linking, different companies' fragment-based campaigns, and types of PPI-directed compounds advancing in the clinic.

Dr. Erlanson will be speaking at the Fragment Based Drug Discovery meeting on April 24-25, 2014 in San Diego, part of CHI's Drug Discovery Chemistry event about Fishing for Fragments to Complement Known Binders.

Dr. Zartler was the scientific advisor to Dr. Shah for the Protein-Protein Interactions meeting taking place April 23-24, 2014 in San Diego, part of CHI's Drug Discovery Chemistry event.

Drs. Erlanson and Zartler are also co-instructors of one of the dinner workshops at the event, Advancing Tools and Technologies for Fragment-Based Design on April 24, 2014.

Erlanson and Zartler are also co-editors of the Practical Fragments blog: Click Here