Title : Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion.

Pub. Date : 2021 Apr 22

PMID : 33829783






2 Functional Relationships(s)
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1 Fragment screening followed by iterative structure-guided design enabled >10 000-fold improvement in potency of a family of allosteric MAT2A inhibitors that are substrate noncompetitive and inhibit release of the product, S-adenosyl methionine (SAM), from the enzyme"s active site. S-Adenosylmethionine methionine adenosyltransferase 2A Homo sapiens
2 Fragment screening followed by iterative structure-guided design enabled >10 000-fold improvement in potency of a family of allosteric MAT2A inhibitors that are substrate noncompetitive and inhibit release of the product, S-adenosyl methionine (SAM), from the enzyme"s active site. S-Adenosylmethionine methionine adenosyltransferase 2A Homo sapiens