肿瘤靶向的硼携带剂在硼中子俘获治疗中的应用与发展  

Application and Development of Tumor-Targeting Boron Carriersin Boron Neutron Capture Therapy

作　　者：陈奎[1,2] 吕林雯 邢更妹 CHEN Kui;LYU Lin-wen;XING Geng-mei(Institute of High Energy Physics,Chinese Academy of Sciences,Beijing 100049,China;Spallation Neutron Source Science Center,Dongguan 523808,China)

机构地区：[1]中国科学院高能物理研究所,北京100049 [2]散裂中子源科学中心,广东东莞523808

出　　处：《核化学与放射化学》2023年第6期487-498,I0002,共13页Journal of Nuclear and Radiochemistry

基　　金：国家自然科学基金(12105312,31971294);粤莞联合基金(2021B1515120037,2021B1515140042);粤港澳中子散射科学和技术联合实验室开放课题(E1905DHT)。

摘　　要：硼中子捕获疗法(boron neutron capture therapy, BNCT)作为一种前景广阔的恶性肿瘤治疗方法已经进入临床。硼药的肿瘤靶向是实现BNCT的二元细胞级精准靶向治疗的前提。基于肿瘤细胞表面特异性/差异性表达受体介导的选择性识别、靶向和富集是目前硼药靶向递送研究的焦点,同时还衍生出了一些精准靶向细胞器的其他靶向递送策略。本文在此分别从小分子硼药和纳米硼药的研发过程,解析了BNCT硼药靶向和递送方法的选择、挑战及其改进方案。新技术、新方法和新思路为未来分子靶向硼药、多靶向硼药的发展提供巨大的便利,包括:依赖组学技术的靶点寻找,依赖机器学习的靶向分子设计和优化,以及基于这些靶点库和靶向分子库搭建的模块化硼核的建立。Boron neutron capture therapy(BNCT)is a promising therapeutic method for malignant tumors and has entered the clinical trials.As a binary cellular accurate therapy,BNCT relies on tumor-targeting boron delivery.It is intriguing for boron delivery design that selective recognization,target,and accumulation are based on specific or differential expression receptors on the tumor cell surface.Several delivery strategies targeting other subcellular organelles have also emerged.Here,we summarized the selection,challenges,and improvement of boron targeting delivery methods in small molecule boron drugs and boron-containing nanoparticles.In the future,new technologies,new methods,and new ideas include target receptors finding via omics,ligands optimization via machine learning,and establishment of modular boron cores based on receptors and ligands libraries,thereby provide great convenience for the development of molecular-targeted boron drugs and multi-targeted boron drugs.

关 键 词：BNCT 肿瘤靶向 硼药 硼携带剂 纳米 

分 类 号：TL923[核科学技术—核燃料循环与材料] R817.5[医药卫生—影像医学与核医学]