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Molecules 2018, 23(11), 2918; https://doi.org/10.3390/molecules23112918

A Novel Venom-Derived Peptide for Brachytherapy of Glioblastoma: Preclinical Studies in Mice

1
Department of Biochemistry and Molecular Medicine, University of Southern California, Los Angeles, CA 90089, USA
2
Department of Neurological Surgery, University of Southern California, Los Angeles, CA 90089, USA
3
Faculty of Pharmacy, Haiphong University of Medicine and Pharmacy, Haiphong, Vietnam
*
Author to whom correspondence should be addressed.
Academic Editor: Jean-Marc Sabatier
Received: 1 October 2018 / Revised: 1 November 2018 / Accepted: 3 November 2018 / Published: 8 November 2018
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Abstract

We developed a bacterial expression system to produce a recombinant disintegrin, vicrostatin (VCN), whose structure is based on a natural disintegrin isolated from southern copperhead snake venom. Our goal is to develop VCN for potential clinical translation as an anti-cancer agent. VCN is a peptide of 69 amino acids with a single tyrosine residue. We have employed VCN as integrin-targeted radionuclide therapy (brachytherapy) for treatment of glioblastoma (GBM, glioma). GBM is a deadly brain cancer that doesn’t discriminate between sexes and knows no age limit. We established that the tyrosine residue in VCN can be radioiodinated with full retention of bioactivity. 131I-VCN was utilized for integrin-targeted radionuclide therapy using mouse models of glioma. The combination of radioiodinated VCN plus temozolomide (a DNA alkylating agent) significantly prolonged survival of glioma-bearing mice. We also obtained similar results using an immunocompetent mouse model and a murine glioma cell line. In summary, as demonstrated in studies reported here we have shown that VCN as targeted radionuclide therapy for GBM has significant translational potential for therapy of this deadly disease. View Full-Text
Keywords: disintegrin; glioblastoma; integrin; brachytherapy; radioiodine; vicrostatin; cancer therapy disintegrin; glioblastoma; integrin; brachytherapy; radioiodine; vicrostatin; cancer therapy
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Swenson, S.; Minea, R.O.; Tuan, C.D.; Thein, T.-Z.; Chen, T.C.; Markland, F.S. A Novel Venom-Derived Peptide for Brachytherapy of Glioblastoma: Preclinical Studies in Mice. Molecules 2018, 23, 2918.

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