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Creatine and phosphocreatine analogs: anticancer activity and enzymatic analysis.

Publication ,  Journal Article
Bergnes, G; Yuan, W; Khandekar, VS; O'Keefe, MM; Martin, KJ; Teicher, BA; Kaddurah-Daouk, R
Published in: Oncol Res
1996

The brain isoform of creatine kinase has been implicated in cellular transformation processes. Cyclocreatine, a creatine kinase substrate analog, was previously shown to be cytotoxic to a broad spectrum of solid tumors. We have synthesized, enzymatically characterized, and evaluated the antitumor activity of a series of substrate analogs of creatine kinase. Using in vitro assays, we demonstrate that several of these analogs are cytotoxic to the human ME-180 cervical carcinoma, the MCF-7 breast adenocarcinoma and the HT-29 colon adenocarcinoma cell lines at low mM concentrations. Analogs that were active in vitro delayed the growth of a subcutaneously implanted rat 13,762 mammary adenocarcinoma. Tumor growth delays of 6-8 days were achieved, which is comparable to effects seen with standard regimens of currently used anticancer drugs. These studies further establish the creatine kinase system as a promising and novel target for anticancer chemotherapy drug design.

Duke Scholars

Published In

Oncol Res

ISSN

0965-0407

Publication Date

1996

Volume

8

Issue

3

Start / End Page

121 / 130

Location

United States

Related Subject Headings

  • Uterine Cervical Neoplasms
  • Tumor Cells, Cultured
  • Rats
  • Phosphocreatine
  • Oncology & Carcinogenesis
  • Neoplasms, Experimental
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Female
  • Creatinine
 

Citation

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MLA
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Bergnes, G., Yuan, W., Khandekar, V. S., O’Keefe, M. M., Martin, K. J., Teicher, B. A., & Kaddurah-Daouk, R. (1996). Creatine and phosphocreatine analogs: anticancer activity and enzymatic analysis. Oncol Res, 8(3), 121–130.
Bergnes, G., W. Yuan, V. S. Khandekar, M. M. O’Keefe, K. J. Martin, B. A. Teicher, and R. Kaddurah-Daouk. “Creatine and phosphocreatine analogs: anticancer activity and enzymatic analysis.Oncol Res 8, no. 3 (1996): 121–30.
Bergnes G, Yuan W, Khandekar VS, O’Keefe MM, Martin KJ, Teicher BA, et al. Creatine and phosphocreatine analogs: anticancer activity and enzymatic analysis. Oncol Res. 1996;8(3):121–30.
Bergnes, G., et al. “Creatine and phosphocreatine analogs: anticancer activity and enzymatic analysis.Oncol Res, vol. 8, no. 3, 1996, pp. 121–30.
Bergnes G, Yuan W, Khandekar VS, O’Keefe MM, Martin KJ, Teicher BA, Kaddurah-Daouk R. Creatine and phosphocreatine analogs: anticancer activity and enzymatic analysis. Oncol Res. 1996;8(3):121–130.
Journal cover image

Published In

Oncol Res

ISSN

0965-0407

Publication Date

1996

Volume

8

Issue

3

Start / End Page

121 / 130

Location

United States

Related Subject Headings

  • Uterine Cervical Neoplasms
  • Tumor Cells, Cultured
  • Rats
  • Phosphocreatine
  • Oncology & Carcinogenesis
  • Neoplasms, Experimental
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Female
  • Creatinine