An Update on Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy

doi:10.1021/acs.jmedchem.6b00055

	An Update on Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy
	Wang, Ying-Qing1 ; Wang, Ping-Yuan 2,3,4; Wang, Yu-Ting 1; Yang, Guang-Fu 4; Zhang, Ao2,3 ; Miao, Ze-Hong 1
刊名	JOURNAL OF MEDICINAL CHEMISTRY
	2016-11-10
卷号	59 期号:21 页码:9575-9598
ISSN号	0022-2623
DOI	10.1021/acs.jmedchem.6b00055
文献子类	Article
英文摘要	Poly(ADP-ribose)polymerase-1 (PARP-1) is a critical DNA repair enzyme in the base excision repair pathway. Inhibitors of this enzyme comprise a new type of anticancer drug that selectively kills cancer cells by targeting, homologous recombination repair defects. Since 2010, important advances have been achieved in PARP-1 inhibitors. Specifically, the approval of olaparib in 2014 for the treatment of ovarian cancer with BRCA mutations validated PARP-1 as an anticancer target and established its clinical importance in cancer therapy. Here, we provide an update on PARP-1 inhibitors, focusing on breakthroughs in their clinical applications and investigations into relevant mechanisms of action, biomarkers, and drug resistance. We also provide an update on the design strategies and the structural types of PARP-1 inhibitors. Opportunities and challenges in PARP-1 inhibitors for cancer therapy will be discussed based on, the above advances.
资助项目	National Basic Research Program of China[2012CB932502] ; National Basic Research Program of China[2015CB910603] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program" of China[2016ZX09101009] ; National Natural Science Foundation of China[81573450] ; National Natural Science Foundation of China[81321092] ; National Natural Science Foundation of China[81430080] ; Chinese Academy of Sciences[XDA12020104] ; Chinese Academy of Sciences[CASIMM0120152003] ; Chinese Academy of Sciences[CASIMM0120153005] ; Chinese Academy of Sciences (Hundred Talents Project)[00000000] ; Science and Technology Commission of Shanghai Municipality[16JC1406300] ; Science and Technology Commission of Shanghai Municipality[14431905300] ; State Key Laboratory of Drug Research[SIMM1601ZZ-03]
WOS关键词	NEGATIVE BREAST-CANCER ; ADVANCED SOLID TUMORS ; SEROUS OVARIAN-CANCER ; DNA-DAMAGE RESPONSE ; CELL LUNG-CANCER ; OLAPARIB MAINTENANCE THERAPY ; RIBOSE POLYMERASE INHIBITOR ; CYCLIN-DEPENDENT KINASE-5 ; BRCA MUTATION CARRIERS ; PHASE-I TRIAL
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000387737600001
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275814]
专题	药物化学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理学第一研究室
通讯作者	Zhang, Ao; Miao, Ze-Hong
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.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zuchongzhi Lu,Bldg 3,Room 426, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Synthet Organ & Med Chem Lab, 555 Zuchongzhi Lu,Bldg 3,Room 426, Shanghai 201203, Peoples R China; 4.Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China
推荐引用方式 GB/T 7714	Wang, Ying-Qing,Wang, Ping-Yuan,Wang, Yu-Ting,et al. An Update on Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy[J]. JOURNAL OF MEDICINAL CHEMISTRY,2016,59(21):9575-9598.
APA	Wang, Ying-Qing,Wang, Ping-Yuan,Wang, Yu-Ting,Yang, Guang-Fu,Zhang, Ao,&Miao, Ze-Hong.(2016).An Update on Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy.JOURNAL OF MEDICINAL CHEMISTRY,59(21),9575-9598.
MLA	Wang, Ying-Qing,et al."An Update on Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy".JOURNAL OF MEDICINAL CHEMISTRY 59.21(2016):9575-9598.