Platinum(IV)-chlorotoxin (CTX) conjugates for targeting cancer cells
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 t...
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Elsevier
2015
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Online Access: | http://hdl.handle.net/1721.1/98866 https://orcid.org/0000-0002-2693-4982 |
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author | Graf, Nora Mokhtari, Tara E. Papayannopoulos, Ioannis A. Lippard, Stephen J. |
author2 | Massachusetts Institute of Technology. Department of Chemistry |
author_facet | Massachusetts Institute of Technology. Department of Chemistry Graf, Nora Mokhtari, Tara E. Papayannopoulos, Ioannis A. Lippard, Stephen J. |
author_sort | Graf, Nora |
collection | MIT |
description | 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. |
first_indexed | 2024-09-23T09:42:45Z |
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institution | Massachusetts Institute of Technology |
language | en_US |
last_indexed | 2024-09-23T09:42:45Z |
publishDate | 2015 |
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spelling | mit-1721.1/988662022-09-26T13:17:32Z Platinum(IV)-chlorotoxin (CTX) conjugates for targeting cancer cells Graf, Nora Mokhtari, Tara E. Papayannopoulos, Ioannis A. Lippard, Stephen J. Massachusetts Institute of Technology. Department of Chemistry Koch Institute for Integrative Cancer Research at MIT Graf, Nora Mokhtari, Tara E. Papayannopoulos, Ioannis A. Lippard, Stephen J. 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. National Cancer Institute (U.S.) (Grant CA034992) German Academic Exchange Service (Fellowship) 2015-09-22T17:34:07Z 2015-09-22T17:34:07Z 2012-02 2012-02 Article http://purl.org/eprint/type/JournalArticle 01620134 http://hdl.handle.net/1721.1/98866 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. https://orcid.org/0000-0002-2693-4982 en_US http://dx.doi.org/10.1016/j.jinorgbio.2012.02.012 Journal of Inorganic Biochemistry Creative Commons Attribution-Noncommercial-NoDerivatives http://creativecommons.org/licenses/by-nc-nd/4.0/ application/pdf Elsevier PMC |
spellingShingle | Graf, Nora Mokhtari, Tara E. Papayannopoulos, Ioannis A. Lippard, Stephen J. Platinum(IV)-chlorotoxin (CTX) conjugates for targeting cancer cells |
title | Platinum(IV)-chlorotoxin (CTX) conjugates for targeting cancer cells |
title_full | Platinum(IV)-chlorotoxin (CTX) conjugates for targeting cancer cells |
title_fullStr | Platinum(IV)-chlorotoxin (CTX) conjugates for targeting cancer cells |
title_full_unstemmed | Platinum(IV)-chlorotoxin (CTX) conjugates for targeting cancer cells |
title_short | Platinum(IV)-chlorotoxin (CTX) conjugates for targeting cancer cells |
title_sort | platinum iv chlorotoxin ctx conjugates for targeting cancer cells |
url | http://hdl.handle.net/1721.1/98866 https://orcid.org/0000-0002-2693-4982 |
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