Preferred Label : CBP/p300 Bromodomain Inhibitor AUR-107;
NCIt synonyms : CBP/p300 Inhibitor AUR-107; p300/CBP Bromodomain Inhibitor AUR107;
NCIt definition : An orally bioavailable 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 AUR-107 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 : AUR-107; AUR 107;
NCI Metathesaurus CUI : CL1915078;
Origin ID : C200814;
UMLS CUI : C5854600;
Semantic type(s)
concept_is_in_subset