Overview of Methionine Adenosyltransferase 2A (MAT2A) as an Anticancer Target: Structure, Function, and Inhibitors,Journal of Medicinal Chemistry

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Overview of Methionine Adenosyltransferase 2A (MAT2A) as an Anticancer Target: Structure, Function, and Inhibitors
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2022-07-07 , DOI: 10.1021/acs.jmedchem.2c00395
Chunzheng Li ₁ , Gang Gui ₁ , Li Zhang ₁ , Anqi Qin ₁ , Chen Zhou ₂ , Xiaoming Zha ₁

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Methionine adenosyltransferase 2A (MAT2A) is a rate-limiting enzyme in the methionine cycle that primarily catalyzes the synthesis of S-adenosylmethionine (SAM) from methionine and adenosine triphosphate (ATP). MAT2A has been recognized as a therapeutic target for the treatment of cancers. Recently, a few MAT2A inhibitors have been reported, and three entered clinical trials to treat solid tumorsor lymphoma with MTAP loss. This review aims to summarize the current understanding of the roles of MAT2A in cancer and the discovery of MAT2A inhibitors. Furthermore, a perspective on the use of MAT2A inhibitors for the treatment of cancer is also discussed. We hope to provide guidance for future drug design and optimization via analysis of the binding modes of known MAT2A inhibitors.

中文翻译：

甲硫氨酸腺苷转移酶 2A (MAT2A) 作为抗癌靶点的概述：结构、功能和抑制剂

蛋氨酸腺苷转移酶 2A (MAT2A) 是蛋氨酸循环中的一种限速酶，主要催化从蛋氨酸和三磷酸腺苷 (ATP)合成S-腺苷蛋氨酸 (SAM)。MAT2A已被公认为治疗癌症的治疗靶点。最近，已经报道了一些 MAT2A 抑制剂，其中三个进入临床试验以治疗MTAP缺失的实体瘤或淋巴瘤。本综述旨在总结目前对 MAT2A 在癌症中作用的认识以及 MAT2A 抑制剂的发现。此外，还讨论了使用 MAT2A 抑制剂治疗癌症的前景。我们希望通过分析已知 MAT2A 抑制剂的结合模式，为未来的药物设计和优化提供指导。

更新日期：2022-07-07

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