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

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


Volume 16, 12 Issues, 2016


Download PDF Flyer




Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

Aims & ScopeAbstracted/Indexed in

Ranking and Category:
  • 27th of 59 in Chemistry, Medicinal

Submit Abstracts Online Submit Manuscripts Online

Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 2.722
5 - Year: 2.849

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.

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.



Purchase Online Order Reprints Order Eprints Rights and Permissions




Article Details

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

Related Journals




Webmaster Contact: urooj@benthamscience.org Copyright © 2016 Bentham Science