c-MET kinase inhibitors: a patent review (2011-2013)
文献类型：期刊论文
| 作者 | Zhu, Kongkai1,2; Kong, Xiangqian2; Zhao, Dan2; Liang, Zhongjie1; Luo, Cheng1,2
|
| 刊名 | EXPERT OPINION ON THERAPEUTIC PATENTS
 |
| 出版日期 | 2014-02 |
| 卷号 | 24期号:2页码:217-230 |
| 关键词 | cancer therapy c-MET inhibitor drug discovery inhibitor selectivity patent review |
| ISSN号 | 1354-3776 |
| DOI | 10.1517/13543776.2014.864279 |
| 文献子类 | Review |
| 英文摘要 | Introduction: The receptor tyrosine kinase c-MET displays aberrant activation in the malignant phenotype of various tumors, and thus, has drawn considerable attention as drug target for cancer therapy. Many c-MET inhibitors are now under clinical investment, and one of them - Cabozantinib - has been approved by US FDA in 2012 for the treatment of medullary thyroid cancer, which further proved the feasibility of c-MET inhibition method in cancer therapy. Areas covered: This article briefly outlines the role of c-MET in oncogenesis and provides a broad overview of the assays used to characterize new inhibitors. Then, a series of representative small-molecule inhibitors of c-MET, especially from the published patent literature from 2011 to 2013, are recorded. Herein, the challenges in the kinase inhibitor design, such as the inhibitor selectivity and resistance mutations, are also discussed. Expert opinion: Up to now, at least 17 inhibitors of c-MET are under clinical evaluation, and several agents exhibit encouraging results. Thus, inhibiting c-MET signaling has major therapeutic value in cancer therapy. Focus on the selectivity of both types of inhibitors, with potent selectivity or multi-targets, have demonstrated antitumor efficacy. The network pharmacology and clinical trials integrated would provide powerful tools to further evaluate the superiority of both inhibitors in continued efficacy and toxicity. |
| WOS关键词 | CYTOREDUCTIVE ANTITUMOR-ACTIVITY ; HEPATOCYTE GROWTH-FACTOR ; SMALL-MOLECULE INHIBITOR ; ACTIVITY IN-VIVO ; SOMATIC MUTATIONS ; SIGNALING PATHWAY ; FACTOR RECEPTOR ; THYROID-CANCER ; LUNG CANCERS ; GENE |
| 资助项目 | China Postdoctoral Science Foundation[7131701713] ; Hi-Tech Research and Development Program of China[2012AA020302] ; National Natural Science Foundation of China[81230076] ; National Natural Science Foundation of China[81302700] ; National Science and Technology Major Project "Key New Drug Creation and Manufacturing Program"[2013ZX09507-004] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000329873900007 |
| 出版者 | INFORMA HEALTHCARE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277214]  |
| 专题 | 药物发现与设计中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Liang, Zhongjie |
| 作者单位 | 1.Suzhou Univ, Ctr Syst Biol, Suzhou 215006, Jiangsu, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhu, Kongkai,Kong, Xiangqian,Zhao, Dan,et al. c-MET kinase inhibitors: a patent review (2011-2013)[J]. EXPERT OPINION ON THERAPEUTIC PATENTS,2014,24(2):217-230. |
| APA | Zhu, Kongkai,Kong, Xiangqian,Zhao, Dan,Liang, Zhongjie,&Luo, Cheng.(2014).c-MET kinase inhibitors: a patent review (2011-2013).EXPERT OPINION ON THERAPEUTIC PATENTS,24(2),217-230. |
| MLA | Zhu, Kongkai,et al."c-MET kinase inhibitors: a patent review (2011-2013)".EXPERT OPINION ON THERAPEUTIC PATENTS 24.2(2014):217-230. |
入库方式： OAI收割
来源：上海药物研究所
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