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PAI-PROTAC
- Development stage
- Preclinical
- Lead developer
- Protai
- 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
PAI-PROTAC is a novel, selective proteolysis-targeting chimera (PROTAC) designed to degrade the lysine acetyltransferase 6A (KAT6A) protein. Developed by Protai using its AIMS™ proteomics and AI platform, the molecule functions by recruiting the Cereblon (CRBN) E3 ubiquitin ligase to KAT6A, inducing its ubiquitination and subsequent proteasomal degradation. KAT6A is a member of the MYST family of histone acetyltransferases and plays a critical role in driving hormonal signaling in estrogen receptor-positive (ER+) breast cancer. PAI-PROTAC demonstrates high selectivity for KAT6A over the closely related KAT6B and other KAT enzymes, and it has shown efficacy in inhibiting growth in ER+ breast cancer cell lines without degrading CRBN neosubstrates.
02
Targets
KAT6A (Lysine acetyltransferase 6A)CRBN (Cereblon)
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