期刊
FUTURE MEDICINAL CHEMISTRY
卷 13, 期 17, 页码 1475-1489出版社
Newlands Press Ltd
DOI: 10.4155/fmc-2021-0132
关键词
demethylase; FTO; inhibitor; structure
资金
- National Natural Science Foundation of China [U1804283]
- Natural Science Foundation of Henan Province [202300410478]
Studies have shown a close relationship between the FTO gene and obesity and various diseases. Developing small-molecule inhibitors targeting the FTO protein not only provides a powerful tool for grasping the active site of FTO, but also lays a theoretical basis for drug design and synthesis targeting FTO protein. This review focuses on the structural characteristics of FTO inhibitors and discusses obesity and cancer caused by overexpression of the FTO gene.
Studies have shown that the FTO gene is closely related to obesity and weight gain in humans. FTO is an N-6-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 FTO, the development of small-molecule inhibitors targeting the FTO protein provides not only a powerful tool for grasping the active site of FTO but also a theoretical basis for the design and synthesis of drugs targeting the FTO protein. This review focuses on the structural characteristics of FTO inhibitors and discusses the occurrence of obesity and cancer caused by FTO gene overexpression.
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