Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity

Ohkanda, J; Lockman, JW; Yokoyama, K; Gelb, MH; Croft, SL; Kendrick, H; Harrell, MI; Feagin, JE; Blaskovich, MA; Sebti, SM; Hamilton, AD; (2001) Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity. Bioorganic & medicinal chemistry letters, 11 (6). pp. 761-764. ISSN 0960-894X DOI:

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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. (C) 2001 Elsevier Science Ltd. All rights reserved.

Item Type: Article
Keywords: Discovery, targets, enzyme, Alkyl and Aryl Transferases, antagonists & inhibitors, metabolism, Animal, Antimalarials, chemical synthesis, chemistry, pharmacology, Drug Design, Drug Resistance, Enzyme Inhibitors, chemical synthesis, chemistry, pharmacology, Imidazoles, chemical synthesis, chemistry, pharmacology, Inhibitory Concentration 50, Parasitic Sensitivity Tests, Plasmodium falciparum, drug effects, Structure-Activity Relationship, Support, Non-U.S. Gov't, Support, U.S. Gov't, P.H.S.
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
Research Centre: Malaria Centre
PubMed ID: 11277514
Web of Science ID: 167571100003


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