Preferred Label : CBP/p300 Bromodomain Inhibitor TT125-802;
NCIt definition : 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.;
Molecule name : TT-125-802; TT 125-802;
Origin ID : C215085;
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