Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity

Junko Ohkanda, Jeffrey W. Lockman, Kohei Yokoyama, Michael H. Gelb, Simon L. Croft, Howard Kendrick, Maria Isabel Harrell, Jean E. Feagin, Michelle A. Blaskovich, Said M. Sebti, Andrew D. Hamilton

Research output: Contribution to journalArticle

Abstract

Malaria continues to represent a very serious health problem in the tropics. The current methods of clinical treatment are showing deficiencies due to the increased incidence of resistance in the parasite. In the present paper we report the design, synthesis, and evaluation of potential antimalarial agents against a novel target, protein farnesyltransferase. We show that the most potent compounds are active against Plasmodium falciparum in vitro at submicromolar concentrations.

Original languageEnglish (US)
Pages (from-to)761-764
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number6
DOIs
StatePublished - Mar 26 2001

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Ohkanda, J., Lockman, J. W., Yokoyama, K., Gelb, M. H., Croft, S. L., Kendrick, H., Harrell, M. I., Feagin, J. E., Blaskovich, M. A., Sebti, S. M., & Hamilton, A. D. (2001). Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity. Bioorganic and Medicinal Chemistry Letters, 11(6), 761-764. https://doi.org/10.1016/S0960-894X(01)00055-5