The relevance of membrane transporters gained momentum in recent years and it is now widely recognized that transporters are key players in drug disposition and chemoresistance. As such, the kidneys harbor a variety of drug transporters and are one of the main routes for xenobiotic excretion. The breast cancer resistance protein (BCRP/ABCG2) is widely accepted as a key mediator of anticancer drug resistance and is a prominent renal drug transporter. Here, we review the role of BCRP in both processes and present a multitude of variables that can influence its activity. An increasing number of renally cleared chemotherapeutics, including tyrosine kinase inhibitors, described as BCRP substrates can modulate its activity via transcription factors and cellular signaling pathways, such as the phosphoinositide 3-kinase (PI3K) pathway. In addition to pharmacological actions, genetic variations, as well as differences between species and gender can affect BCRP function, which are also discussed. Furthermore, the role of BCRP in light of cancer treatments and the implications for novel therapeutic interventions that take into account renal function are discussed.

膜转运蛋白的相关性近年来发展势头强劲，现在人们普遍认为，膜转运蛋白是药物处置和化学抗药性的关键参与者。因此，肾脏具有多种药物转运蛋白，是异种生物排泄的主要途径之一。乳腺癌抗性蛋白（BCRP / ABCG2）被广泛认为是抗癌药物耐药性的关键介质，并且是重要的肾脏药物转运蛋白。在这里，我们回顾了BCRP在这两个过程中的作用，并提出了许多可能影响其活性的变量。被称为BCRP底物的越来越多的肾脏清除化学疗法（包括酪氨酸激酶抑制剂）可以通过转录因子和细胞信号途径（如磷酸肌醇3-激酶（PI3K）途径）调节其活性。除了药理作用外，遗传变异以及物种和性别之间的差异也会影响BCRP功能，这也将进行讨论。此外，还讨论了BCRP在癌症治疗中的作用以及考虑到肾功能的新型治疗干预的意义。