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蛋白酪氨酸激酶抑制作用:基于机制的抗肿瘤药物发现

Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents.

作者信息

Chang C J, Geahlen R L

机构信息

Department of Medicinal Chemistry and Pharmacognosy, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907.

出版信息

J Nat Prod. 1992 Nov;55(11):1529-60. doi: 10.1021/np50089a001.

DOI:10.1021/np50089a001
PMID:1479375
Abstract

Protein-tyrosine kinases (PTKs) have been shown to induce the cascade of altered cell parameters characteristic of transformed cells. This proposition provides an important rationale for the discovery of potential antitumor agents from natural sources on the basis of inhibition of PTK activity. Numerous naturally occurring and synthetic analogues of PTK inhibitors were systematically evaluated in this review based on their structure-activity relationships and potential antitumor efficacy.

摘要

蛋白酪氨酸激酶(PTKs)已被证明可诱导转化细胞所特有的一系列细胞参数改变。这一观点为基于抑制PTK活性从天然来源发现潜在抗肿瘤药物提供了重要的理论依据。在本综述中,基于其构效关系和潜在的抗肿瘤疗效,对众多天然存在的和合成的PTK抑制剂类似物进行了系统评估。

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