摘要
目前,癌症激酶作为新抗癌药物的重要靶点。激酶有500种,其中有些已经得到临床研究,而其余的因其潜在的治疗应用而亟待研究。磷酸化是激酶的主要功能,它是一个最重要的信号转导机制,其中细胞间信号传导调节细胞内如离子转运、激素反应和细胞增殖过程。激酶功能的紊乱可能会导致肿瘤进展和其他如免疫、神经系统、代谢和感染性疾病的发生。这使得有必要将激酶抑制剂发展成为治疗试剂。本文讨论不同类型的癌症中不同类型的激酶及其抑制剂,并对激酶的起源、发现、在癌症治疗中的激酶抑制剂的特性和作用方式进行了全面的概述。
关键词: 激酶,激酶抑制剂,癌症,小分子,激酶家族,抗癌治疗。
Current Drug Targets
Title:Cancer Kinases and its Novel Inhibitors: Past, Present and Future Challenges
Volume: 16 Issue: 11
Author(s): Prathesha Pillai, R.S. Surenya, Shantikumar V. Nair and Vinoth-Kumar Lakshmanan
Affiliation:
关键词: 激酶,激酶抑制剂,癌症,小分子,激酶家族,抗癌治疗。
摘要: Cancer kinome is now well organized as an important target for a new class of cancer drugs. There are more than 500 members in the kinase family in which some of them are clinically analysed, while the rest are under investigation for potential therapeutic applications. Phosphorylation, major function of kinases is one of the most significant signal transduction mechanism in which intercellular signals regulate intracellular processes like ion transport, hormone responses and cellular proliferation. Any deregulation of kinase function may lead to tumor progression and other disorders such as immunological, neurological , metabolic including also infectious diseases. This led to the necessity in the development of kinase inhibitors as therapeutic agent. Herein we discuss about different types of kinases and their inhibitors in various types of cancers. This review portrays a broad overview of the origin of kinases, discovery, the characterization and mode of action of kinase inhibitors in cancer therapy.
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Prathesha Pillai, R.S. Surenya, Shantikumar V. Nair and Vinoth-Kumar Lakshmanan , Cancer Kinases and its Novel Inhibitors: Past, Present and Future Challenges, Current Drug Targets 2015; 16 (11) . https://dx.doi.org/10.2174/1389450116666150416120108
DOI https://dx.doi.org/10.2174/1389450116666150416120108 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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