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Enhancing therapeutic efficacy of cisplatin by blocking dna damage repair
Cong, Yuwei1,2; Wang, Liangyan3; Wang, Zigui1,2; He, Shasha1,2; Zhou, Dongfang1; Jing, Xiabin1; Huang, Yubin1
刊名Acs medicinal chemistry letters
2016-10-01
卷号7期号:10页码:924-928
关键词Protein phosphatase 2a Cisplatin Dna repair Combination treatment
ISSN号1948-5875
DOI10.1021/acsmedchemlett.6b00236
通讯作者Zhou, dongfang(east@ciac.ac.cn)
英文摘要Self-repair of nuclear dna damage is the most known reason that leads to drug resistance of cancer tissue and limited therapeutic efficacy of anticancer drugs. inhibition of protein phosphatase 2a (pp2a) would block dna damage-induced defense of cancer cells to suppress dna repair for enhanced cancer treatment. here, we combined a pp2a inhibitor lb (4-(3-carboxy-7-oxa-bicyclo[2.2.1]heptane-2-carbonyl) piperazine-1-carboxylic acid tert-butyl ester) and the dna damage chemotherapeutic drug cisplatin through a simple physical superposition. the two drugs administrated at a ratio of 1:1 exhibited an optional synergistic antitumor efficacy in vitro and in vivo. lb was demonstrated to specifically activate the protein kinase b (akt) and mitogen-activated protein kinases (mapk) signaling pathways by pp2a inhibition to overcome cell cycle arrest caused by cisplatin-induced dna damage.
WOS关键词PROTEIN PHOSPHATASE 2A ; COMBINATION THERAPY ; CANCER-CHEMOTHERAPY ; PLATINUM COMPLEXES ; TUMOR RESISTANCE ; DRUG-RESISTANCE ; CO-DELIVERY ; CELLS ; NANOPARTICLES ; INHIBITION
WOS研究方向Pharmacology & Pharmacy
WOS类目Chemistry, Medicinal
语种英语
出版者AMER CHEMICAL SOC
WOS记录号WOS:000385689300012
内容类型期刊论文
URI标识http://www.corc.org.cn/handle/1471x/2374892
专题中国科学院大学
通讯作者Zhou, Dongfang
作者单位1.Chinese Acad Sci, Changchun Inst Appl Chem, State Key Lab Polymer Phys & Chem, Changchun 130022, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
3.Nanjing Orientleader Technol Co Ltd, Nanjing 210028, Jiangsu, Peoples R China
推荐引用方式
GB/T 7714
Cong, Yuwei,Wang, Liangyan,Wang, Zigui,et al. Enhancing therapeutic efficacy of cisplatin by blocking dna damage repair[J]. Acs medicinal chemistry letters,2016,7(10):924-928.
APA Cong, Yuwei.,Wang, Liangyan.,Wang, Zigui.,He, Shasha.,Zhou, Dongfang.,...&Huang, Yubin.(2016).Enhancing therapeutic efficacy of cisplatin by blocking dna damage repair.Acs medicinal chemistry letters,7(10),924-928.
MLA Cong, Yuwei,et al."Enhancing therapeutic efficacy of cisplatin by blocking dna damage repair".Acs medicinal chemistry letters 7.10(2016):924-928.
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