Fedotcheva T A, Shimanovsky N L
Pirogov Russian National Research Medical University, Moscow, 1 Ostrovityanova St., 117997 Russia.
Pharm Chem J. 2023;56(10):1307-1313. doi: 10.1007/s11094-023-02790-8. Epub 2023 Jan 12.
Actual mechanisms of multidrug resistance (MDR) to chemotherapy in oncology are considered. ABC-transporters such as P-glycoprotein, BCRP protein, and MRP proteins take part in the development of resistance. The review presents the main classes of chemosensitizers, i.e., inhibitors of ABC transporters of the 1-4 generations. Plant polyphenols, i.e., flavonoids, are commonly referred to as the last (4) generation of MDR inhibitors. Chemosensitizers of different classes should be chosen with allowance for the patient mutation-expression profile and the receptor status of a particular tumor. The appropriate dosage of the chemosensitizer and the administration schedule can enhance the process of counteracting MDR.
本文探讨了肿瘤化疗中多药耐药(MDR)的实际机制。ABC转运蛋白如P-糖蛋白、BCRP蛋白和MRP蛋白参与了耐药性的产生。综述介绍了主要类型的化学增敏剂,即1-4代ABC转运蛋白抑制剂。植物多酚,即类黄酮,通常被认为是第4代MDR抑制剂。应根据患者的突变表达谱和特定肿瘤的受体状态来选择不同类型的化学增敏剂。合适的化学增敏剂剂量和给药方案可以增强对抗MDR的过程。