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...

Full description

Bibliographic Details
Main Authors: Graf, Nora, Mokhtari, Tara E., Papayannopoulos, Ioannis A., Lippard, Stephen J.
Other Authors: Massachusetts Institute of Technology. Department of Chemistry
Format: Article
Language:en_US
Published: Elsevier 2015
Online Access:http://hdl.handle.net/1721.1/98866
https://orcid.org/0000-0002-2693-4982
_version_ 1826193665441136640
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
format Article
id mit-1721.1/98866
institution Massachusetts Institute of Technology
language en_US
last_indexed 2024-09-23T09:42:45Z
publishDate 2015
publisher Elsevier
record_format dspace
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
work_keys_str_mv AT grafnora platinumivchlorotoxinctxconjugatesfortargetingcancercells
AT mokhtaritarae platinumivchlorotoxinctxconjugatesfortargetingcancercells
AT papayannopoulosioannisa platinumivchlorotoxinctxconjugatesfortargetingcancercells
AT lippardstephenj platinumivchlorotoxinctxconjugatesfortargetingcancercells