Breast Cancer Resistant Protein Inhibitors: A Review

The breast cancer resistance protein (BCRP), an ATP-binding cassette (ABC) transporter superfamily member, has therapeutic importance in cancer owing to its multidrug resistance capabilities. BCRP has really been tied to the clinical treatment of cancer tolerance, Acute myelogenous or acute lymphocytic leukemias are the most common. Because of the way its ATP-dependent drug efflux pump works, the FDA has previously recognized BCRP as one of the potentially critically significant drug transports and its apparent role in drug resistance diminishes the therapeutic effectiveness of numerous chemotherapy drugs. The objective of this review paper is to compile the many study results on natural compounds that have BCRP inhibitory effects. Increased consumption of these flavonoids in cancer patients taking chemotherapy may have unfavourable effects. The current study offers the first information on the rotenoid derivatives' ability to inhibit BCRP, Boravinones appears to be a novel class of fascinating BCRP inhibitors.

乳腺癌耐药蛋白（breast cancer resistance protein, BCRP）属于ATP结合盒（ATP-binding cassette, ABC）转运蛋白超家族，因其具备多药耐药特性，在癌症治疗领域具有重要的研究与临床价值。BCRP与癌症治疗耐受密切相关，其中以急性髓系白血病和急性淋巴细胞白血病最为多见。由于其ATP依赖性药物外排泵的作用机制，美国食品药品监督管理局（Food and Drug Administration, FDA）此前已将BCRP列为极具关键意义的药物转运蛋白之一；其在耐药性形成中的明确作用，会削弱多种化疗药物的治疗效果。本综述旨在汇总各类具有BCRP抑制活性的天然化合物的相关研究成果。化疗期间的癌症患者若过量摄入这类黄酮类化合物（flavonoids），可能会产生不利影响。本研究首次披露了鱼藤酮类衍生物的BCRP抑制活性，其中布拉维诺酮类（Boravinones）似乎是一类极具研究价值的新型BCRP抑制剂。