Toward rapamycin analog (rapalog)-based precision cancer therapy

doi:10.1038/aps.2015.68

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	Toward rapamycin analog (rapalog)-based precision cancer therapy
	Meng, Ling-hua1,2,3 ; Zheng, X. F. Steven 2,3
刊名	ACTA PHARMACOLOGICA SINICA
	2015-10
卷号	36 期号:10 页码:1163-1169
关键词	rapalog rapamycin mTOR precision cancer therapy
ISSN号	1671-4083
DOI	10.1038/aps.2015.68
文献子类	Review
英文摘要	Rapamycin and its analogs (rapalogs) are the first generation of mTOR inhibitors, which have the same molecular scaffold, but different physiochemical properties. Rapalogs are being tested in a wide spectrum of human tumors as both monotherapy and a component of combination therapy. Among them, temsirolimus and everolimus have been approved for the treatment of breast and renal cancer. However, objective response rates with rapalogs in clinical trials are modest and variable. Identification of biomarkers predicting response to rapalogs, and discovery of drug combinations with improved efficacy and tolerated toxicity are critical to moving this class of targeted therapeutics forward. This review focuses on the aberrations in the PI3K/mTOR pathway in human tumor cells or tissues as predictive biomarkers for rapalog efficacy. Recent results of combinational therapy using rapalogs and other anticancer drugs are documented. With the rapid development of next-generation genomic sequencing and precision medicine, rapalogs will provide greater benefits to cancer patients.
资助项目	NIH[CA123391] ; NIH[CA173519] ; NIH[CA166575] ; National Natural Science Foundation of China[81321092] ; National Natural Science Foundation of China[81173079] ; National Natural Science Foundation of China[81373445]
WOS关键词	RENAL-CELL CARCINOMA ; PHASE-II TRIAL ; MULTIPLE-MYELOMA CELLS ; BREAST-CANCER ; HEPATOCELLULAR-CARCINOMA ; DETERMINES SENSITIVITY ; TEMSIROLIMUS CCI-779 ; KINASE INHIBITORS ; MAMMALIAN TARGET ; INTERFERON-ALPHA
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	ACTA PHARMACOLOGICA SINICA
WOS记录号	WOS:000362459200002
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276383]
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
通讯作者	Zheng, X. F. Steven
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China 2.Rutgers State Univ, Robert Wood Johnson Med Sch, Rutgers Canc Inst New Jersey, New Brunswick, NJ 08903 USA; 3.Rutgers State Univ, Robert Wood Johnson Med Sch, Div Canc Pharmacol, New Brunswick, NJ 08903 USA;
推荐引用方式 GB/T 7714	Meng, Ling-hua,Zheng, X. F. Steven. Toward rapamycin analog (rapalog)-based precision cancer therapy[J]. ACTA PHARMACOLOGICA SINICA,2015,36(10):1163-1169.
APA	Meng, Ling-hua,&Zheng, X. F. Steven.(2015).Toward rapamycin analog (rapalog)-based precision cancer therapy.ACTA PHARMACOLOGICA SINICA,36(10),1163-1169.
MLA	Meng, Ling-hua,et al."Toward rapamycin analog (rapalog)-based precision cancer therapy".ACTA PHARMACOLOGICA SINICA 36.10(2015):1163-1169.