Multidrug resistance (MDR) in cancer cells is the development of resistance to a variety of structurally and functionally nonrelated anticancer drugs. This phenomenon has become a major obstacle to cancer chemotherapy seriously affecting the clinical outcome. MDR is associated with increased drug efflux from cells mediated by an energy‐dependent mechanism involving the ATP‐binding cassette (ABC) transporters, mainly P‐glycoprotein (ABCB1), the MDR‐associated protein‐1 (ABCC1), and the breast cancer resistance protein (ABCG2). The first two transporters have been widely studied already and reviews summarized the results. The ABCG2 protein has been a subject of intense study since its discovery as its overexpression has been detected in resistant cell lines in numerous types of human cancers. To date, a long list of modulators of ABCG2 exists and continues to increase. However, little is known about the clinical consequences of ABCG2 modulation. This makes the design of novel, potent, and nontoxic inhibitors of this efflux protein a major challenge to reverse MDR and thereby increase the success of chemotherapy. The aim of the present review is to describe and highlight specific and nonspecific modulators of ABCG2 reported to date based on the selectivity of the compounds, as many of them are effective against one or more ABC transport proteins.

中文翻译：

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ABCG2 / BCRP：特定和非特定调节剂

癌细胞中的多药耐药性（MDR）是对多种结构上和功能上不相关的抗癌药的耐药性的发展。这种现象已成为严重影响临床结果的癌症化疗的主要障碍。MDR与能量依赖性机制介导的细胞的药物外排增加有关，该机制涉及ATP结合盒（ABC）转运蛋白，主要是P-糖蛋白（ABCB1），MDR相关蛋白-1（ABCC1）和乳腺癌。抗性蛋白（ABCG2）。前两个转运蛋白已被广泛研究，并综述了结果。自从发现ABCG2蛋白以来，就一直在对其进行深入研究，因为已经在许多类型的人类癌症的耐药细胞系中检测到了它的过表达。迄今为止，存在并且持续增加的一长串ABCG2调节剂。但是，关于ABCG2调节的临床后果知之甚少。这使得设计这种外排蛋白的新型，有效且无毒的抑制剂成为逆转MDR并因此增加化疗成功的主要挑战。本综述的目的是基于化合物的选择性描述和强调迄今为止报道的ABCG2的特异性和非特异性调节剂，因为它们中的许多对一种或多种ABC转运蛋白有效。