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Journal: Discovery of novel MAT2A inhibitors by an allosteric site-compatible fragment growing approach. (Pubmed Central) - Feb 19, 2024
X-ray co-crystal structure revealed that compound 7 fully occupies the allosteric pocket of MAT2A as a single molecule mimicking MAT2B. By introducing additional backbone interactions and rigidifying the requisite linker extensions, we generated compound 8, which exhibited single digit nanomolar enzymatic and sub-micromolar cellular inhibitory potency for MAT2A.
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ISM3412, a novel and selective MAT2A inhibitor for the treatment of cancer (Section 18; Poster Board #3) - Mar 14, 2023 - Abstract #AACR2023AACR_2561;
Further, it was well tolerated with no significant hepatobiliary toxicity. In conclusion, ISM3412 is a novel and highly selective MAT2A inhibitor for MTAP-deficient cancers, and merits clinical evaluation.
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