克服顺铂耐药性的新型Pt(Ⅳ)前药研究进展  

Research progress in new Pt(Ⅳ)prodrugs to overcome cisplatin resistance

作　　者：孙蒙琪 陈西敬 赵娣 SUN Meng-qi;CHEN Xi-jing;ZHAO Di(School of Basic Medicine and Clinical Pharmacy,China Pharmaceutical University,Nanjing 210009)

机构地区：[1]中国药科大学基础医学与临床药学学院,南京210009

出　　处：《中南药学》2022年第4期863-870,共8页Central South Pharmacy

摘　　要：顺铂在各种恶性肿瘤的治疗中发挥着关键作用,但其使用常因耐药受到限制。Pt(Ⅳ)前药是将活性或非活性配体与Pt(Ⅱ)化合物通过化学键合而成,其在一定程度上表现出更佳的药效、更低的毒性、较低的耐药性以及更好的代谢稳定性,是一类有望规避顺铂耐药性的新型铂类抗肿瘤药物。本文围绕靶向细胞凋亡逃逸、DNA损伤修复以及提高Pt(Ⅳ)前药的脂溶性和靶向性等方面,对目前研究中出现的能够克服顺铂耐药的新型Pt(Ⅳ)前药进行了分析探讨,以期能为克服顺铂耐药的Pt(Ⅳ)前药开发提供借鉴。Cisplatin plays a key role in the treatment of various malignant tumors,but its use is usually limited due to drug resistance.Pt(Ⅳ)prodrugs are formed by the chemical bonding of active or inactive ligands with Pt(Ⅱ)compounds.To a certain extent,they show better efficacy,lower toxicity,lower drug resistance and better metabolic stability.They are a new type of platinum anticancer drugs expected to reduce drug resistance of cisplatin.This paper focused on targeting apoptosis escape,DNA damage repair,and improving fat solubility and targeting of Pt(Ⅳ)prodrugs,and summarized Pt(Ⅳ)prodrugs that can overcome cisplatin resistance to provide reference for the development of Pt(Ⅳ)prodrugs.

关 键 词：顺铂 多药耐药 Pt(Ⅳ)前药 逆转耐药 

分 类 号：R914.2[医药卫生—药物化学]