双环肽靶向核药研究进展  

Research progress in bicyclic peptide-based radiopharmaceuticals

作　　者：高新 苗源 张思琪 王钝[2] 王锐 胡宽 GAO Xin;MIAO Yuan;ZHANG Si-qi;WANG Dun;WANG Rui;HU Kuan(State Key Laboratory of Bioactive Substance and Function of Natural Medicines,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China;School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]中国医学科学院、北京协和医学院药物研究所,天然药物及核药基础与新药创制全国重点实验室,北京100050 [2]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《药学学报》2025年第4期864-874,共11页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金面上项目(82372002);中国医学科学院中央级公益性科研院所基本科研业务费(2022-RC350-04);中国医学科学院医学与健康科技创新工程项目(2021-I2M-1-026,2022-I2M-2-002,2021-I2M-3-001,2023-I2M-2-006,2023-I2M-QJ-010);北京市科技新星创新新星和北京市科技新星计划交叉合作课题;北京市自然科学基金-昌平创新联合基金(L234044);北京市自然科学基金-北京经济技术开发区创新联合基金(L248087);北京协和医学院中央高校基本科研业务费青年学者项目(3332023044);中国国家原子能机构核技术研究发展中心(放射性药物非临床评价)开放基金(ZHYLYB2021005)。

摘　　要：核药是核医学的灵魂,靶向配体发现是核药研创的核心。多肽核药在临床实践中展示出了显著的优势,在已获批靶向核药中占据重要地位。作为核药配体的新锐力量,双环肽开发技术近年来发展迅速,其相较于传统多肽配体优势明显,具有重要的临床转化潜力。该文总结了双环肽配体的获取方式,概述了双环肽核药的主要临床和临床前研究进展,对双环肽靶向核药的未来发展方向做出展望。以期为药学和核医学从业者了解多肽核药前沿提供参考。Radiopharmaceuticals play a crucial role in nuclear medicine,with the development of radioligands being a key focus in this field.Peptide-based radiopharmaceuticals have shown significant advantages in clinical applications,with the majority of FDA-approved targeting radiopharmaceuticals since 2018 being derived from peptides or peptidomimetics.Bicyclic peptides have emerged as a promising targeting moiety in radioligands,offering improved biophysical properties compared to linear or monocyclic peptide ligands.This article provides an overview of the methods for obtaining bicyclic peptide ligands,as well as highlighting the major clinical and preclinical advancements in bicyclic peptide-based radiopharmaceuticals.The review also discusses the future prospects of bicyclic peptide-based radiopharmaceuticals,offering insights for practitioners in the field of pharmaceutical science and nuclear medicine to keep up with the latest developments in radiopharmaceutical innovation.

关 键 词：靶向核药 双环肽 PET显像 高通量筛选 天然产物活性肽 

分 类 号：R943[医药卫生—药剂学]