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Ornithine Aminotransferase versus GABA Aminotransferase: Implications for the Design of New Anticancer Drugs

机译:鸟氨酸氨基转移酶与GABA氨基转移酶:对新型抗癌药物设计的启示

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摘要

Ornithine aminotransferase (OAT) and -aminobutyric acid aminotransferase (GABA-AT) are classified under the same evolutionary subgroup and share a large portion of structural, functional, and mechanistic features. Therefore, it is not surprising that many molecules that bind to GABA-AT also bind well to OAT. Unlike GABA-AT, OAT had not been viewed as a potential therapeutic target until recently; consequently, the number of therapeutically viable molecules that target OAT is very limited. In this review the two enzymes are compared with respect to their active-site structures, catalytic and inactivation mechanisms, and selective inhibitors. Insight is offered that could aid in the design and development of new selective inhibitors of OAT for the treatment of cancer.
机译:鸟氨酸氨基转移酶(OAT)和-氨基丁酸氨基转移酶(GABA-AT)被归为同一进化亚组,并具有很大的结构,功能和机制特征。因此,许多与GABA-AT结合的分子也与OAT结合也就不足为奇了。与GABA-AT不同,直到最近,OAT才被视为潜在的治疗目标。因此,靶向OAT的治疗上可行的分子数量非常有限。在这篇综述中,对两种酶的活性位点结构,催化和失活机理以及选择性抑制剂进行了比较。提供的见解可以帮助设计和开发用于治疗癌症的新型OAT选择性抑制剂。

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