Type II kinase inhibitors: an opportunity in cancer for rational design

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


Volume 14, 10 Issues, 2014


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Ranking and Category:
  • 26th of 59 in Chemistry, Medicinal
  • 99th of 197 in Oncology

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


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Type II kinase inhibitors: an opportunity in cancer for rational design

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


Abstract

Since the introduction of the Type II kinase inhibitor imatinib (Gleevec) for treatment against cancer, rational design of tailored molecules has increased the opportunities in medicinal chemistry to tackle tumours related to kinase dysfunctionalities. Among the different types of kinase inhibitors, the design of Type II inhibitors has been rationalized to exploit the benefits and reduce the drawbacks. Here we present the advances with Type II inhibitors, discussing the advantages and disadvantages of these type of molecules. Moreover, we expose the strategies in designing druggable molecules that either selectively inhibit target kinases or overcome drug resistance.


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Article Details

Volume: 13
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DOI: 10.2174/1871520613666131125130835
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