周期蛋白依赖性激酶抑制剂。

Progress in cell cycle research Pub Date : 2003-01-01
Peter M Fischer, Jane Endicott, Laurent Meijer
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引用次数: 0

摘要

周期蛋白依赖性激酶参与多种细胞过程,包括细胞周期控制、细胞凋亡、神经元生理、分化和转录。基于CDK/抑制剂共晶结构和SAR研究的密集筛选和药物设计导致了大量CDK化学抑制剂的鉴定和表征。虽然它们都是通过与ATP竞争在激酶的催化位点结合而起作用,但它们的激酶选择性差异很大,在大多数情况下仍有待研究。许多生理过程对CDKs的需求证明了它们作为潜在治疗靶点的评价比最初预期的要大得多。
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Cyclin-dependent kinase inhibitors.

Cyclin-dependent kinases are involved in diverse cellular processes that include cell cycle control, apoptosis, neuronal physiology, differentiation, and transcription. Intensive screening and drug design based on CDK/inhibitor co-crystal structures and on SAR studies have led to the identification and characterization of a large variety of chemical inhibitors of CDKs. Although they all act by competing with ATP for binding at the catalytic site of the kinase, their kinase selectivity varies greatly and remains to be studied in most cases. The requirement for CDKs in many physiological processes justifies their evaluation as potential therapeutic targets against a much larger scope of diseases than initially anticipated.

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