美国 FDA 批准用于癌症治疗的小分子激酶抑制剂（2001-2015 年）：医疗适应症、结构优化和结合模式，第一部分。

IF 3.3 3区医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Bioorganic & Medicinal Chemistry Pub Date : 2024-08-08 DOI:10.1016/j.bmc.2024.117870

Ying Wang , Xiang Nan , Yanping Duan , Qiuxu Wang , Zhigang Liang , Hanrong Yin

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引用次数: 0

摘要

鉴于激酶在恶性肿瘤的病因、进展、侵袭和转移中的节点作用，激酶失调已成为抗癌药物发现的一类主要靶点，美国食品及药物管理局（FDA）于 2015 年底批准了 28 种用于癌症治疗的小分子激酶抑制剂（SMKI）药物，就验证了这一点。虽然这些药物的临床前和临床数据已被广泛介绍，但对美国食品药品管理局批准的这些抗肿瘤小分子激酶抑制剂的医疗适应症、设计原理和结合模式进行最新综述，为今后开发具有特定疗效和安全性的小分子激酶抑制剂提供启示，是非常必要的。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

FDA-approved small molecule kinase inhibitors for cancer treatment (2001–2015): Medical indication, structural optimization, and binding mode Part I

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FDA-approved small molecule kinase inhibitors for cancer treatment (2001–2015): Medical indication, structural optimization, and binding mode Part I

The dysregulation of kinases has emerged as a major class of targets for anticancer drug discovery given its node roles in the etiology of tumorigenesis, progression, invasion, and metastasis of malignancies, which is validated by the FDA approval of 28 small molecule kinase inhibitor (SMKI) drugs for cancer treatment at the end of 2015. While the preclinical and clinical data of these drugs are widely presented, it is highly essential to give an updated review on the medical indications, design principles and binding modes of these anti-tumor SMKIs approved by the FDA to offer insights for the future development of SMKIs with specific efficacy and safety.

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来源期刊

Bioorganic & Medicinal Chemistry 医学-生化与分子生物学

CiteScore

6.80

自引率

2.90%

发文量

413

审稿时长

17 days

期刊介绍： Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.