Targeting Reversible Lysine Acetylation with Designed Small Molecules

Event Details

Type

Friday Lecture Series

Speaker(s)

Philip Cole, M.D., Ph.D., professor, Brigham and Women's Hospital, Harvard Medical School

Speaker bio(s)

Reversible Lys acetylation by acetyltransferases and deacetylases is critical to the regulation of gene expression and cell growth in normal physiology and disease processes. Two major enzymes that catalyze these reactions are p300 acetyltransferase and HDAC1 deacetylase. Dr. Cole's lab has used rational design approaches to develop synthetic compounds that target p300 acetyltransferase activity. Their latest generation compounds have been used to provide new insights into the role of p300/CBP in cancer. They have also developed synthetic agents that selectively target HDAC1-containing CoREST complex by dually inhibiting HDAC1 and CoREST subunit LSD1 histone demethylase. They show that one of our dual action inhibitors, corin, shows enhanced pharmacologic properties in melanoma and cutaneous squamous cell carcinoma based on its combined HDAC1- and LSD1-targeting warheads.

Dr. Cole received his B.S. in chemistry in 1984 from Yale University and then spent a year as a Churchill Scholar at the University of Cambridge. He received M.D. and Ph.D. degrees from Johns Hopkins University where he pursued research in bioorganic chemistry. He then entered post-doctoral training at Harvard Medical School prior to joining The Rockefeller University in 1996 as an assistant professor and head of lab. In 1999, Dr. Cole returned to Johns Hopkins as professor and director of pharmacology until 2017, when he moved to Harvard Medical School and Brigham and Women's Hospital as professor of medicine and biological chemistry and molecular pharmacology. With Tom Muir, his group developed the method of expressed protein ligation while at Rockefeller. In work also begun at Rockefeller with Robert G. Roeder, Dr. Cole reported the first potent and selective histone acetyltransferase inhibitors which ultimately led to the founding of Acylin Therapeutics, Inc. His honors include election as an AAAS fellow and receipt of an NIH MERIT Award.

Open to

Public

Host

Tarun Kapoor, Ph.D.

Reception

Refreshments, 3:15 p.m. - 3:45 p.m., Abby Lounge

Contact

Justin Sloboda

Phone

(212) 327-7785

Sponsor

Justin Sloboda
(212) 327-7785
jsloboda@rockefeller.edu

Readings

http://librarynews.rockefeller.edu/?p=4921