Allosteric kinase inhibitors: a new paradigm for effective and selective modulation of kinase activities

doi:10.5246/jcps.2012.06.068

Abstract

Abstract:

Dysregulation of kinases has been proven to be one of the main causes of abnormal growth and survival of cancer cells. Selective modulations of kinase activities have become the focus of many research programs for the development of safe and effective chemotherapy for cancers. So far, fifteen kinase inhibitors have received FDA approval for the treatment of various forms of cancers. Among them, the allosteric kinase inhibitors have been shown to have superior clinical profile in terms of safety and efficacy. In this review, we summarize the allosteric conformations of kinases, their corresponding inhibitors and the modes of their interactions.

Key words: Protein kinase, Allosteric conformation, DFG-out, ATP non-competitive, Kinase inhibitor

CLC Number:

R962.1

Supporting:

Hongliang Yang, Ting Chen, Xu Bai, Yazhong Pei^* . Allosteric kinase inhibitors: a new paradigm for effective and selective modulation of kinase activities [J]. , DOI: 10.5246/jcps.2012.06.068.

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