Article
Discovery of novel MAT2A inhibitors by an allosteric site-compatible fragment growing approach.
Bioorganic & medicinal chemistry - 15 Feb 2024
Gao Feng, Ding Xiaoyu, Cao Zhongying, Zhu Wei, Fan Yaya, Steurer Barbara, Wang Hailong, Cai Xin, Zhang Man, Aliper Alex, Ren Feng, Ding Xiao, Zhavoronkov Alex
Abstract excerpt
The methionine adenosyltransferase MAT2A catalyzes the synthesis ofthe methyl donor S-adenosylmethionine (SAM) and thereby regulates critical aspects of metabolism and transcription. Aberrant MAT2A function can lead to metabolic and transcriptional reprogramming of cancer cells, and MAT2A has been shown to promote survival of MTAP-deficient tumors, a genetic alteration that occurs in ∼ 13 % of all tumors. Thus,...
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