AUR115

AUR115 is a potent, orally bioavailable, and highly selective small molecule proteolysis-targeting chimera (PROTAC) designed to degrade the p300 (EP300) protein. Developed by Aurigene Discovery Technologies (a subsidiary of Dr. Reddy's Laboratories) using their proprietary A-PROX platform, AUR115 utilizes a cereblon (CRBN)-based E3 ligase recruitment mechanism to selectively target p300 for proteasomal degradation while sparing its closely related paralog, CBP (CREB-binding protein). This paralog-selective approach is intended to exploit synthetic lethality in cancers harboring CBP mutations or deletions, such as specific subsets of breast and prostate cancers. In these CBP-deficient tumor cells, the loss of p300 leads to the collapse of oncogenic transcriptional programs and induces apoptosis, whereas cells with intact CBP remain viable. AUR115 is currently in the preclinical stage of development.

Other names

p300 selective degraderp-300 selective degraderp 300 selective degraderp300 selective PROTACp-300 selective PROTACp 300 selective PROTACp300 degraderp-300 degraderp 300 degrader