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CBP/p300 bromodomain inhibitor TT125-802

An orally bioavailable small molecule inhibitor of the bromodomain of the histone acetyltransferase (HAT) paralogs, CREB binding protein (CBP; CREBBP) and p300 (E1A-associated protein p300; p300 HAT), with potential immunomodulating and antineoplastic activities. Upon oral administration, CBP/p300 bromodomain inhibitor TT125-802 targets and binds to the bromodomains of CBP and p300. This disrupts the acetylation of histones and other proteins and decreases regulatory T cells (Tregs) generation, inhibits its suppressive function and causes Tregs apoptosis. This modulates T-helper cells, induces an anti-tumor immune response and decreases tumor growth. The HAT paralogs CBP and p300 are key transcriptional co-activators that are essential for a multitude of cellular processes and play a key role in the regulation of gene expression in both tumor and immune cells.
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Code name:TT 125-802
TT-125-802
TT125-802
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