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Allosteric kinase inhibitors:a new paradigm for effective and selective modulation of kinase activities
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作者 杨洪亮 陈婷 +1 位作者 柏旭 裴亚中 《Journal of Chinese Pharmaceutical Sciences》 CAS 2012年第6期531-543,共13页
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 ... 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. 展开更多
关键词 Protein kinase Allosteric conformation DFG-out atp non-competitive Kinase inhibitor
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