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Toxins 2018, 10(12), 496;

Chlorotoxin—A Multimodal Imaging Platform for Targeting Glioma Tumors

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
Authors to whom correspondence should be addressed.
Received: 18 October 2018 / Revised: 20 November 2018 / Accepted: 23 November 2018 / Published: 26 November 2018
(This article belongs to the Special Issue From Toxins to Drugs)
Full-Text   |   PDF [567 KB, uploaded 26 November 2018]   |  


Chlorotoxin (CTX) is a 36-amino-acid disulfide-containing peptide derived from the venom of the scorpion Leiurus quinquestriatus. 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. View Full-Text
Keywords: chlorotoxin; glioblastoma; imaging modalities chlorotoxin; glioblastoma; imaging modalities

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Cohen, G.; Burks, S.R.; Frank, J.A. Chlorotoxin—A Multimodal Imaging Platform for Targeting Glioma Tumors. Toxins 2018, 10, 496.

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