first-in-class oral MAT2A allosteric inhibitor

synthetic lethal candidate in Ph. I for MTAP-

from >2000 fragment library and SBDD

J. Med. Chem., Apr. 8, 2021

Agios Pharmaceuticals, Cambridge, MA

The Agios first-in-class oral MAT2A enzyme allosteric inhibitor, AG-270, is a Ph. I clinical candidate for tumors with MTAP gene loss. The inhibitor works on a synthetic lethality principle: the MTAP-loss which drives…

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