用于硼中子俘获治疗的碳硼烷多肽衍生物

    Carborane Polypeptide Derivatives for Boron Neutron Capture Therapy

    • 摘要: 含碳硼烷多肽衍生物的设计和应用得到越来越多人们的关注,尤其是作为硼中子俘获治疗(boron neutron capture therapy, BNCT)硼携带剂用于治疗恶性肿瘤极具发展前景。BNCT利用10B与中子俘获反应,放出α粒子杀死肿瘤细胞。作为一种二元靶向疗法,其成功关键就是硼携带剂的靶向性和亲和力的效果,当前如何设计更高效的硼携带剂是BNCT发展的主要问题。多肽作为生物必需物质,增加其衍生物靶向性的同时被肿瘤特异性摄取,是含碳硼烷多肽化合物作为硼携带剂极大的优势。本文首次对已报导的含碳硼烷多肽衍生物进行分类总结,并评估作为硼携带剂应用于中子俘获治疗的发展潜力。对含碳硼烷多肽衍生物的总结,将为新一代硼携带剂设计用于中子俘获治疗发展提供研究动力。

       

      Abstract: The design and application of carborane polypeptide derivatives have attracted more and more attention, especially as boron carrier in the treatment of malignant tumors(BNCT). BNCT uses 10B to react with neutron capture, releasing alpha particles that kill tumor cells. As a binary targeted therapy, the key to its success is the targeting and affinity effect of boron carriers. At present, how to design more efficient boron carriers is the main problem in the development of BNCT. Polypeptides, as biological essential substances, can be taken up specifically by tumors while increasing the targeting of their derivatives, which is a great advantage of carbborane polypeptide compounds as boron carriers. In this paper, the reported carbborane polypeptide derivatives are classified and summarized for the first time, and the development potential as boron carriers for neutron capture therapy is evaluated. The summary of carbborane containing polypeptide derivatives will provide research impetus for the development of a new generation of boron carriers designed for neutron capture therapy.

       

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