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. 2001 Mar 26;11(6):761-4.
doi: 10.1016/s0960-894x(01)00055-5.

Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity

J Ohkanda  1 , J W Lockman, K Yokoyama, M H Gelb, S L Croft, H Kendrick, M I Harrell, J E Feagin, M A Blaskovich, S M Sebti, A D Hamilton
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Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity

J Ohkanda et al. Bioorg Med Chem Lett. .

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.

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