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p300 degrader

Development stage
Preclinical
Lead developer
SK Life Science
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Oral
01

Overview

SK Biopharmaceuticals, through its subsidiary SK Life Science Labs (formerly Proteovant Therapeutics), is developing an orally bioavailable, small-molecule heterobifunctional degrader targeting the epigenetic protein p300 for oncology indications. This therapeutic candidate utilizes the ubiquitin-proteasome system (UPS) to selectively eliminate p300 while maintaining minimal activity against the closely related CREB-binding protein (CBP). Preclinical data indicates that the p300 degrader effectively suppresses androgen receptor (AR) signaling and inhibits tumor growth in models of AR-positive prostate cancer and cancers characterized by CBP loss-of-function mutations. The program leverages the company's MOPED™ molecular glue and AI-enabled target identification platforms to achieve potent anti-tumor activity by protein elimination rather than simple enzymatic inhibition.

Other names
p300-selective targeted protein degraderp-300-selective targeted protein degraderp 300-selective targeted protein degrader
02

Targets

CRBN (Cereblon)EP300 (Histone acetyltransferase p300)

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