Abstract
With the advent of the Type II kinase inhibitor imatinib (Gleevec) for treatment against cancer, rational design of tailored molecules has brought a revolution in medicinal chemistry for treating tumours caused by kinase malfunctioning. Among different types of kinase inhibitors, the design of Type II inhibitors has been rationalized for maximizing the benefits and reducing drawbacks. Here we highlight the development made in Type II inhibitors, discussing the advantages and disadvantages of these types of molecules. Furthermore, we present the strategies for designing druggable molecules that either selectively inhibit target kinases or overcome drug resistance.
Keywords: Allosteric inhibitors, cancer, covalent inhibitors, DFG-in, DFG-out, kinase inhibitors, Type I inhibitors, Type II inhibitors, Type III inhibitors, Type IV inhibitors.
Anti-Cancer Agents in Medicinal Chemistry
Title:Type II Kinase Inhibitors: An Opportunity in Cancer for Rational Design
Volume: 13 Issue: 5
Author(s): Javier Blanc, Raphael Geney and Christel Menet
Affiliation:
Keywords: Allosteric inhibitors, cancer, covalent inhibitors, DFG-in, DFG-out, kinase inhibitors, Type I inhibitors, Type II inhibitors, Type III inhibitors, Type IV inhibitors.
Abstract: With the advent of the Type II kinase inhibitor imatinib (Gleevec) for treatment against cancer, rational design of tailored molecules has brought a revolution in medicinal chemistry for treating tumours caused by kinase malfunctioning. Among different types of kinase inhibitors, the design of Type II inhibitors has been rationalized for maximizing the benefits and reducing drawbacks. Here we highlight the development made in Type II inhibitors, discussing the advantages and disadvantages of these types of molecules. Furthermore, we present the strategies for designing druggable molecules that either selectively inhibit target kinases or overcome drug resistance.
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Cite this article as:
Blanc Javier, Geney Raphael and Menet Christel, Type II Kinase Inhibitors: An Opportunity in Cancer for Rational Design, Anti-Cancer Agents in Medicinal Chemistry 2013; 13 (5) . https://dx.doi.org/10.2174/1871520611313050008
DOI https://dx.doi.org/10.2174/1871520611313050008 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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