Platinum(IV)-chlorotoxin (CTX) conjugates for targeting cancer cells
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Author(s) • • •
Graf, Nora
Mokhtari, Tara E.
Papayannopoulos, Ioannis A.
Lippard, Stephen J.
Date Issued
February 2012
Journal
Journal of Inorganic Biochemistry
Publisher
Elsevier
Citation
Graf, Nora, Tara E. Mokhtari, Ioannis A. Papayannopoulos, and Stephen J. Lippard. “Platinum(IV)-Chlorotoxin (CTX) Conjugates for Targeting Cancer Cells.” Journal of Inorganic Biochemistry 110 (May 2012): 58–63.
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Author's final manuscript
Abstract
Cisplatin is one of the most widely used anticancer drugs. Its side effects, however, have motivated researchers to search for equally effective analogs that are better tolerated. Selectively targeting cancer tissue is one promising strategy. For this purpose, a platinum(IV) complex was conjugated to the cancer-targeting peptide chlorotoxin (CTX, TM601) in order to deliver cisplatin selectively to cancer cells. The 1:1 Pt-CTX conjugate was characterized by mass spectrometry and gel electrophoresis. Like most platinum(IV) derivatives, the cytotoxicity of the conjugate was lower in cell culture than that of cisplatin, but greater than those of its Pt(IV) precursor and CTX in several cancer cell lines.
MIT Department
Massachusetts Institute of Technology. Department of Chemistry
Koch Institute for Integrative Cancer Research at MIT
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DOI of Published Version
https://doi.org/10.1016/j.jinorgbio.2012.02.012