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 |
DOI | 10.1021/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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