Journal of medicinal chemistryHumansAnimalsAntineoplastic AgentsMethionine AdenosyltransferaseStructure-Activity Relationship
Furo[2,3-f]quinazolin-7(6H)-one Derivatives as Potent, Selective, and Orally Bioavailable MAT2A Inhibitors for MTAP-Deficient Cancer Therapy.
Zihan Shi, Kexin Lin, Lijie Lin, Zhiyi Chen, Zhiyin Xie, Yaoliang Sun, Rongrong Cui, Sulin Zhang, Mingyue Zheng, Shilin Xu
Published: 202510.1021/acs.jmedchem.5c02062
Abstract
Methionine adenosyltransferase 2A (MAT2A) has emerged as a synthetic lethal target in methylthioadenosine phosphorylase (MTAP)-deleted cancers, which account for approximately 15% of human tumors and currently lack effective therapies. However, exist…
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