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CBP/p300 bromodomain inhibitor AUR-107

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.
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Synonym:CBP/p300 inhibitor AUR-107
p300/CBP bromodomain inhibitor AUR107
Code name:AUR 107
AUR-107
AUR107
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