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摘要
多药耐药(MDR)表型是胆管癌对当前的抗肿瘤药反应不良的一个因素。当手术摘除无效时,无论是作为辅助治疗还是用于治疗晚期的CCA这在很大程度上限制了药理学方法的使用。MDR是机体抵御存在与胆管癌中的毒性化合物的复杂组合的结果,这在通过灌注该组织的血液使胆汁上皮免受到达胆道毒素的影响中起作用,或由肝细胞分泌到胆汁中,胆管细胞暴露于胆汁中。上述的化学抗性(MOC)的这些机制在来源于胆管细胞的肿瘤中通常具有增强的功效。本综述文章是关于CCA对肿瘤药物不良反应的MOC的最新情况。这些MOC被分类为以下:由于吸收减少(MOC-1a)或增强的外排(MOC-1b),细胞中药物的量的变化;前药,活性药物和非活性代谢物(MOC-2)之间改变的比例;抗肿瘤药物(MOC-3)分子靶标的变化;增强肿瘤细胞修复药物诱导的DNA损伤(MOC-4)的能力和细胞凋亡/存活平衡(MOC-5)受损。
关键词: 化疗、药物代谢、药物转运、肝癌、药理学、治疗、肿瘤
Current Drug Targets
Title:Molecular Bases of Chemoresistance in Cholangiocarcinoma
Volume: 18 Issue: 8
关键词: 化疗、药物代谢、药物转运、肝癌、药理学、治疗、肿瘤
摘要: The multidrug resistance (MDR) phenotype accounts for the poor response of cholangiocarcinoma to available antitumor drugs. This is an important limitation to the use of pharmacological approaches, both as adjuvant therapies and for treating advanced CCA when surgical removal is not possible. MDR is the result of a complex combination of defense mechanisms against toxic compounds already present in cholangiocytes, which play a role in the physiology of these cells by protecting the biliary epithelium from the toxins reaching the biliary tree with the blood that perfuses this tissue, or that are secreted by hepatocytes into bile, to which cholangiocytes are exposed. These mechanisms of chemoresistance (MOC) are also present, usually with enhanced efficacy, in tumors derived from cholangiolar cells. The present review article is an update of the state-of-the-art regarding the MOC involved in the poor response of CCA to antitumor drugs. These MOC have been classified as: changes in the amount of drug in the cells due to decreased uptake (MOC-1a) or enhanced efflux (MOC-1b); altered proportions between prodrug, active drug and inactive metabolites (MOC-2); changes in the molecular targets of antitumor drugs (MOC-3); an enhanced ability of tumor cells to repair drug-induced DNA damage (MOC-4), and an impaired apoptosis/survival balance (MOC-5).
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Cite this article as:
Molecular Bases of Chemoresistance in Cholangiocarcinoma, Current Drug Targets 2017; 18 (8) . https://dx.doi.org/10.2174/1389450116666150223121508
DOI https://dx.doi.org/10.2174/1389450116666150223121508 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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