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靶向去甲基化酶的小分子抑制剂的结构特征。

Structural characteristics of small-molecule inhibitors targeting demethylase.

机构信息

Green Catalysis Center, College of Chemistry, Zhengzhou University, Zhengzhou, China.

出版信息

Future Med Chem. 2021 Sep;13(17):1475-1489. doi: 10.4155/fmc-2021-0132. Epub 2021 Jul 9.

Abstract

Studies have shown that the gene is closely related to obesity and weight gain in humans. is an N-methyladenosine demethylase and is linked to an increased risk of obesity and a variety of diseases, such as acute myeloid leukemia, type 2 diabetes, breast cancer, glioblastoma and cervical squamous cell carcinoma. In light of the significant role of , the development of small-molecule inhibitors targeting the protein provides not only a powerful tool for grasping the active site of but also a theoretical basis for the design and synthesis of drugs targeting the protein. This review focuses on the structural characteristics of inhibitors and discusses the occurrence of obesity and cancer caused by gene overexpression.

摘要

研究表明,该基因与人的肥胖和体重增加密切相关。是一种 N6-甲基腺苷去甲基酶,与肥胖风险增加以及多种疾病相关,如急性髓系白血病、2 型糖尿病、乳腺癌、胶质母细胞瘤和宫颈鳞状细胞癌。鉴于的重要作用,针对 蛋白的小分子抑制剂的开发不仅为掌握 的活性位点提供了有力工具,也为针对 蛋白的药物设计和合成提供了理论基础。本综述重点讨论了 抑制剂的结构特征,并探讨了 基因过表达导致肥胖和癌症的发生。

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