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Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions

文献类型：期刊论文

作者Wang, Meining2; Shen, Aijun; Zhang, Chi3; Song, Zilan2; Ai, Jing1; Liu, Hongchun1; Sun, Liping3; Ding, Jian1; Geng, Meiyu1; Zhang, Ao2
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2016-06-23
卷号59期号:12页码:5563-5586
ISSN号0022-2623
DOI10.1021/acs.jmedchem.5b01106
文献子类Article
英文摘要Heat shock protein 90 (Hsp90) is a ubiquitous chaperone of all of the oncogenic tyrosine kinases. Many Hsp90 inhibitors, alone or in combination, have shown significant antitumor efficacy against the kinase-positive naive and mutant models. However, clinical trials of these inhibitors are unsuccessful due to insufficient clinical benefits and nonoptimal safety profiles. Recently, much progress has been reported on the Hsp90-cochaperone-client complex, which will undoubtedly assist in the understanding of the interactions between Hsp90 and its clients. Meanwhile, Hsp90 inhibitors have shown promise against patients' resistance caused by early generation tyrosine kinase inhibitors (TKIs), and at least 13 Hsp90 inhibitors are being reevaluated in the clinic. In this regard, the objectives of the current perspective are to summarize the structure and function of the Hsp90-cochaperone-client complex, to analyze the structural and functional insights into the Hsp90-client interactions to address several existing unresolved problems with Hsp90 inhibitors, and to highlight the preclinical and clinical studies of Hsp90 inhibitors as an effective treatment against resistance to tyrosine kinase inhibitors.
WOS关键词CELL LUNG-CANCER ; ADVANCED SOLID TUMORS ; I DOSE-ESCALATION ; GASTROINTESTINAL STROMAL TUMOR ; REFRACTORY MULTIPLE-MYELOMA ; RETASPIMYCIN HYDROCHLORIDE IPI-504 ; MOLECULAR CHAPERONE HSP90 ; POTENT ANTITUMOR-ACTIVITY ; METASTATIC BREAST-CANCER ; MULTICENTER PHASE-II
资助项目Chinese NSF[81430080] ; Chinese NSF[81125021] ; Chinese NSF[81373277] ; Chinese NSF[81473243] ; Chinese NSF[81321092] ; Major State Basic Research Development Program[2015CB910603] ; SIMM[CA-SIMM0120154002/2002]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000378662900001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/275989]  
专题药理学第一研究室
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
药物化学研究室
通讯作者Zhang, Ao
作者单位1.Chinese Acad Sci, SIMM, State Key Lab Drug Res, Div Antitumor Pharmacol, 555 Zuchongzhi Lu,Bldg 3,Room 426, Shanghai 201203, Peoples R China;
2.Chinese Acad Sci, SIMM, Synthet Organ & Med Chem Lab, CAS Key Lab Receptor Res, 555 Zuchongzhi Lu,Bldg 3,Room 426, Shanghai 201203, Peoples R China;
3.China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China
推荐引用方式
GB/T 7714		 Wang, Meining,Shen, Aijun,Zhang, Chi,et al. Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions[J]. JOURNAL OF MEDICINAL CHEMISTRY,2016,59(12):5563-5586.
APA Wang, Meining.,Shen, Aijun.,Zhang, Chi.,Song, Zilan.,Ai, Jing.,...&Zhang, Ao.(2016).Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.JOURNAL OF MEDICINAL CHEMISTRY,59(12),5563-5586.
MLA Wang, Meining,et al."Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions".JOURNAL OF MEDICINAL CHEMISTRY 59.12(2016):5563-5586.

入库方式： OAI收割

来源：上海药物研究所

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