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Am J Nucl Med Mol Imaging. 2014 Aug 15;4(5):385-405. eCollection 2014.

Recent advances in diagnosis and treatment of gliomas using chlorotoxin-based bioconjugates.

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Department of Nuclear Medicine, The First People's Hospital, Shanghai Jiaotong University Shanghai 200080, P.R. China.
Molecular Imaging Center, Department of Radiology, Keck School of Medicine, University of Southern California Los Angeles, CA 90033, USA.


Malignant gliomas, especially glioblastoma multiforme, are the most widely distributed and deadliest brain tumors because of their resistance to surgical and medical treatment. Research of glioma-specific bioconjugates for diagnosis and therapy developed rapidly during the past several years. Many studies have demonstrated that chlorotoxin (CTX) and Buthus martensii Karsch chlorotoxin (BmK CT) specifically inhibited glioma cells growth and metastasis, and accelerated tumor apoptosis. The bioconjugates of CTX or BmK CT with other molecules have played an increasing role in diagnostic imaging and treatment of gliomas. To date, CTX-based bioconjugates have achieved great success in phase I/II clinical trials about safety profiles. Here, we will provide a review on the important role of ion channels in the underlying mechanisms of gliomas invasive growth and how CTX suppresses gliomas proliferation and migration. We will summarize the recent advances in the applications of CTX bioconjugates for gliomas diagnosis and treatment. In addition, we will review recent studies on BmK CT bioconjugates and compare their efficacies with CTX derivatives. Finally, we will address advantages and challenges in the use of CTX or BmK CT bioconjugates as specific agents for theranostic applications in gliomas.


Buthus martensii Karsch chlorotoxin (BmK CT); Chlorotoxin (CTX); glioma; imaging; therapy


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