Abstract
Cell cycle deregulation is one of the first steps that transform normal cells into tumor cells. CDKs are a family of proteins devoted to controlling cell cycle entry, progression and exit. Studies from animal models show a tissuespecific essentiality of the single CDKs. In cancer cells, mis-regulation of CDK function is a common event. For this reason the pioneer compound Flavopiridol was developed and many new drugs are currently under development. ATP and the last generation of non-ATP competitive inhibitors are now emerging as one of the most potentially powerful target therapies. Many clinical trials are ongoing, as either a single agent or in combination with the classical cytotoxic agents. In this review, we discuss new strategies and methods to design more potent, selective and specific CDK inhibitors, starting from evidence emerging from animal and cancer cell models.
Keywords: CDK, kinase inhibitors, CDK clinical trials
Current Drug Targets
Title: CDK Inhibitors: From the Bench to Clinical Trials
Volume: 11 Issue: 3
Author(s): Flavio Rizzolio, Tiziano Tuccinardi, Isabella Caligiuri, Chiara Lucchetti and Antonio Giordano
Affiliation:
Keywords: CDK, kinase inhibitors, CDK clinical trials
Abstract: Cell cycle deregulation is one of the first steps that transform normal cells into tumor cells. CDKs are a family of proteins devoted to controlling cell cycle entry, progression and exit. Studies from animal models show a tissuespecific essentiality of the single CDKs. In cancer cells, mis-regulation of CDK function is a common event. For this reason the pioneer compound Flavopiridol was developed and many new drugs are currently under development. ATP and the last generation of non-ATP competitive inhibitors are now emerging as one of the most potentially powerful target therapies. Many clinical trials are ongoing, as either a single agent or in combination with the classical cytotoxic agents. In this review, we discuss new strategies and methods to design more potent, selective and specific CDK inhibitors, starting from evidence emerging from animal and cancer cell models.
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Rizzolio Flavio, Tuccinardi Tiziano, Caligiuri Isabella, Lucchetti Chiara and Giordano Antonio, CDK Inhibitors: From the Bench to Clinical Trials, Current Drug Targets 2010; 11 (3) . https://dx.doi.org/10.2174/138945010790711978
DOI https://dx.doi.org/10.2174/138945010790711978 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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