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基于微泡的血栓靶向的当前策略:激活特异性表位和小分子配体

Current Strategies for Microbubble-Based Thrombus Targeting: Activation-Specific Epitopes and Small Molecular Ligands.

作者信息

Wang Zhaojian, Huang Huaigu, Chen Yuexin, Zheng Yuehong

机构信息

Department of Vascular Surgery, Peking Union Medical College Hospital, Beijing, China.

出版信息

Front Bioeng Biotechnol. 2021 Jul 16;9:699450. doi: 10.3389/fbioe.2021.699450. eCollection 2021.

Abstract

Microbubbles with enhanced ultrasound represent a potentially potent evolution to the administration of a free drug in the treatment of thrombotic diseases. Conformational and expressional changes of several thrombotic biological components during active coagulation provide epitopes that allow site-specific delivery of microbubble-based agents to the thrombus for theranostic purpose. Through the interaction with these epitopes, emerging high-affinity small molecular ligands are able to selectively target the thrombi with tremendous advantages over traditional antibody-based strategy. In this mini-review, we summarize recent novel strategies for microbubble-based targeting of thrombus through epitopes located at activated platelets and fibrin. We also discuss the challenges of current targeting modalities and supramolecular carrier systems for their translational use in thrombotic pathologies.

摘要

具有增强超声功能的微泡代表了在血栓性疾病治疗中游离药物给药的一种潜在有效进展。在活跃凝血过程中,几种血栓形成生物成分的构象和表达变化提供了表位,使得基于微泡的药剂能够用于治疗诊断目的,实现向血栓的位点特异性递送。通过与这些表位相互作用,新出现的高亲和力小分子配体能够选择性地靶向血栓,相对于传统的基于抗体的策略具有巨大优势。在本综述中,我们总结了通过位于活化血小板和纤维蛋白上的表位实现基于微泡靶向血栓的最新新策略。我们还讨论了当前靶向模式和超分子载体系统在血栓性疾病转化应用中的挑战。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e257/8322734/3dabe18b57c6/fbioe-09-699450-g001.jpg

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