Inventors:
Philip A. Cole - Baltimore MD, US
Ling Wang - Seattle WA, US
Erin M. Bowers - Baltimore MD, US
David J. Meyers - Towson MD, US
Chandrani Mukherjee - Baltimore MD, US
International Classification:
C07D 405/06
US Classification:
514369, 435184, 514404, 514375, 435 74, 506 8, 5483657, 506 9, 548183, 548224
Abstract:
The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.