Type II Kinase Inhibitors: An Opportunity in Cancer for Rational Design

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 16, 12 Issues, 2016

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex

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Type II Kinase Inhibitors: An Opportunity in Cancer for Rational Design

Anti-Cancer Agents in Medicinal Chemistry, 13(5): 731-747.

Author(s): Javier Blanc, Raphael Geney and Christel Menet.

Affiliation: Galapagos NV., Industriepark Mechelen Noord; Generaal De Wittelaan L11 A3; B-2800 Mechelen, Belgium.


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.


Allosteric inhibitors, cancer, covalent inhibitors, DFG-in, DFG-out, kinase inhibitors, Type I inhibitors, Type II inhibitors, Type III inhibitors, Type IV inhibitors.

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Article Details

Volume: 13
Issue Number: 5
First Page: 731
Last Page: 747
Page Count: 17
DOI: 10.2174/1871520611313050008
Price: $58

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