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细胞周期蛋白依赖性激酶 7 抑制剂在癌症治疗中的应用。

Cyclin-dependent kinase 7 inhibitors in cancer therapy.

机构信息

State Key Laboratory of Natural Medicines & Development of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.

出版信息

Future Med Chem. 2020 May;12(9):813-833. doi: 10.4155/fmc-2019-0334. Epub 2020 Mar 25.

Abstract

Cyclin-dependent kinase 7 (CDK7) plays crucial roles in the regulation of cell cycle and transcription that are tightly associated with cancer development and metastasis. The recent identification of the first covalent inhibitor which possesses high specificity against CDK7 prompts intense studies on designing highly selective CDK7 inhibitors and exploring their applications in cancer treatments. This review summarizes the latest biological studies on CDK7 and reviews the development of CDK7 inhibitors in preclinical and clinical evaluations, along with the prospects and potential challenges in this research area. CDK7 is an attractive anticancer target, and the discovery and development of CDK7 inhibitors has received much attention.

摘要

细胞周期蛋白依赖性激酶 7(CDK7)在细胞周期和转录的调节中发挥着关键作用,与癌症的发生和转移密切相关。最近发现了第一个对 CDK7 具有高特异性的共价抑制剂,这促使人们对设计高度选择性的 CDK7 抑制剂进行了深入研究,并探索了它们在癌症治疗中的应用。本文综述了 CDK7 的最新生物学研究,并回顾了 CDK7 抑制剂在临床前和临床评估中的发展,以及该研究领域的前景和潜在挑战。CDK7 是一个有吸引力的抗癌靶点,CDK7 抑制剂的发现和开发受到了广泛关注。

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