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ATP结合盒转运蛋白介导的MDR逆转剂的实验研究现况
引用本文:华英,胡人杰.ATP结合盒转运蛋白介导的MDR逆转剂的实验研究现况[J].天津药学,2006,18(6):55-59.
作者姓名:华英  胡人杰
作者单位:天津市医药科学研究所,天津,300020
摘    要:多药耐药性(mu ltidrug resistance,MDR)是指人肿瘤细胞对结构各异的化疗药物产生交叉耐药,是肿瘤化疗失败的主要原因之一。为了增强肿瘤细胞对化疗药物的敏感性,积极寻求有效逆转MDR的药物已成为研究重点。体外被证实具有逆转耐药活性的化合物很多,但由于体内要达到体外逆转试验的有效浓度所需剂量过大,毒副作用大,因此限制了临床应用。ATP结合盒转运蛋白家族(ATP-b ind ing cassette,ABC)介导的药物外排机制是目前MDR的主要机制,ABC转运蛋白家族中与多药耐药性相关的转运蛋有P-糖蛋白(P-gp)、多药耐药相关蛋白(MRP)和乳腺癌耐药蛋白(BCRP)。本文对ABC转运蛋白介导的MDR逆转剂的研究进展做一综述。

关 键 词:ATP结合盒转运蛋白  肿瘤多药耐药  逆转剂
文章编号:1006-5687(2006)06-0055-05
收稿时间:2006-04-04
修稿时间:2006年4月4日

The development of chemosensitizers for MDR mediated by ABC transporters
Hua Ying,Hu Renjie.The development of chemosensitizers for MDR mediated by ABC transporters[J].Tianjin Pharmacy,2006,18(6):55-59.
Authors:Hua Ying  Hu Renjie
Institution:Tianjin Institute of Medical and Pharmaceutical Science, Tianjin 300020
Abstract:Multidrug resistance(MDR) describes the cross-resistance to various structurally unrelated cytotoxic agents in human neoplasms.Resistance to chemotherapy remains an obstacle to the successful treatment of human cancer.To enhance the response of tumours to chemotherapy,attention has been focused on agents to reverse multidrug resistance and on the sensitivity of tumour cells to chemical drugs.Hundreds of reversal drugs have been found in vitro,but their clinical application has been limited because of their toxicity.Prominent among possible mechanisms of this MDR are the broad specificity drug efflux pumps of the ATPbinding cassette(ABC) family.In this review,the development of chemosensitizers are described focusing on well-known proteins including P-glycoprotein,multidrug resistance associated protein and breast cancer resistance protein.
Keywords:ABC transporter  MDR  chemosensitizer
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