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Open AccessArticle

Drug Conjugates for Targeting Eph Receptors in Glioblastoma

1
Brain Tumor Center of Excellence, Wake Forest Baptist Medical Center Comprehensive Cancer Center, Winston-Salem, NC 27157, USA
2
Department of Experimental Therapeutics, Division of Cancer Medicine, MD Anderson Cancer Center, Houston, TX 77054, USA
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(4), 77; https://doi.org/10.3390/ph13040077
Received: 2 March 2020 / Revised: 14 April 2020 / Accepted: 15 April 2020 / Published: 23 April 2020
(This article belongs to the Special Issue Targeting the Eph–ephrin System)
Glioblastoma (GBM) is a complex and heterogeneous tumor that warrants a comprehensive therapeutic approach for treatment. Tumor-associated antigens offer an opportunity to selectively target various components of the GBM microenvironment while sparing the normal cells within the central nervous system. In this study, we conjugated a multivalent vector protein, QUAD 3.0, that can target four receptors: EphA3, EphA2, EphB2, and also IL-13RA2, spanning virtually 100% of the GBM microenvironment, to doxorubicin derivatives. The conjugates effectively bound to all four receptors, although to varying degrees, and delivered cytotoxic loads to both established and patient-derived GBM cell lines, with IC50 values in the low nM range. The conjugates were also non-toxic to animals. We anticipate that the QUAD 3.0 Dox conjugates will be further used in preclinical models and possibly clinics in the foreseeable future. View Full-Text
Keywords: Eph receptors; multiple-receptor targeting; glioblastoma; ligand–drug conjugates; doxorubicin Eph receptors; multiple-receptor targeting; glioblastoma; ligand–drug conjugates; doxorubicin
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Sharma, P.; Roberts, C.; Herpai, D.; Fokt, I.D.; Priebe, W.; Debinski, W. Drug Conjugates for Targeting Eph Receptors in Glioblastoma. Pharmaceuticals 2020, 13, 77.

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