氯毒素-A 多模态成像平台靶向脑胶质瘤肿瘤。
Chlorotoxin-A Multimodal Imaging Platform for Targeting Glioma Tumors.
机构信息
Frank Laboratory, Radiology and Imaging Sciences, Clinical Center, National Institutes of Health, Bethesda, MD 20892, USA.
National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, MD 20892, USA.
出版信息
Toxins (Basel). 2018 Nov 26;10(12):496. doi: 10.3390/toxins10120496.
Chlorotoxin (CTX) is a 36-amino-acid disulfide-containing peptide derived from the venom of the scorpion . CTX alters physiology in numerous ways. It interacts with voltage gated chloride channels, Annexin-2, and matrix metalloproteinase-2 (MMP-2). CTX-based bioconjugates have been widely subjected to phase I/II clinical trials and have shown substantial promise. Many studies have demonstrated that CTX preferentially binds to neuroectodermal tumors, such as glioblastoma, without cross-reactivity to normal brain cells. With its ability to penetrate the blood-brain-barrier (BBB) and its tyrosine residue allows covalent conjugation with functional moieties, CTX is an attractive platform to explore development of diagnostic and therapeutic agents for gliomas. In this review, we outline CTX structure and its molecular targets, summarize molecular variations of CTX developed for glioma imaging, and discuss future trends and perspectives for CTX conjugates as a theranostic agent.
氯毒素 (CTX) 是一种 36 个氨基酸组成的二硫键肽，来源于蝎子毒液。CTX 以多种方式改变生理机能。它与电压门控氯离子通道、膜联蛋白-2 和基质金属蛋白酶-2（MMP-2）相互作用。基于 CTX 的生物缀合物已广泛进行 I/II 期临床试验，并显示出很大的前景。许多研究表明，CTX 优先与神经外胚层肿瘤（如胶质母细胞瘤）结合，而与正常脑细胞无交叉反应。CTX 具有穿透血脑屏障 (BBB) 的能力，其酪氨酸残基允许与功能部分进行共价结合，因此是探索开发用于治疗神经胶质瘤的诊断和治疗剂的有吸引力的平台。在这篇综述中，我们概述了 CTX 的结构及其分子靶标，总结了用于神经胶质瘤成像的 CTX 的分子变化，并讨论了 CTX 缀合物作为治疗药物的未来趋势和前景。
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