Definition

An orally bioavailable inhibitor of the bromodomain of the histone acetyltransferase (HAT) paralogs, CREB binding protein (CBP) and p300 (E1A-associated protein p300; p300 HAT), with potential antineoplastic activity. Upon oral administration, CBP/p300 bromodomain inhibitor FT-7051 targets and binds to the bromodomain of CBP and p300. This disrupts the acetylation of histones and other proteins and prevents the co-activation of the androgen receptor (AR) including AR-v7. This may inhibit tumor cell proliferation in AR-positive tumor cells. The HAT paralogs CBP and p300 are key transcriptional co-activators that are essential for a multitude of cellular processes and are implicated in the progression and therapeutic resistance of certain cancers.