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

doi:10.1016/S0960-894X(01)00055-5

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

Chemistry

Research output: Contribution to journal › Article › peer-review

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 language	English (US)
Pages (from-to)	761-764
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	6
DOIs	https://doi.org/10.1016/S0960-894X(01)00055-5
State	Published - Mar 26 2001

ASJC Scopus subject areas

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

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10.1016/S0960-894X(01)00055-5

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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

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title = "Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity",

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.",

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

note = "Funding Information: This work was supported by grants from the National Institutes of Health (CA67771 to SMS and ADH, and CA53874 to MHG) and UNDP/World Bank/WHO Special Programme for Research and Training in Tropical Diseases to SLC. ",

year = "2001",

month = mar,

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doi = "10.1016/S0960-894X(01)00055-5",

language = "English (US)",

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T1 - Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity

AU - Ohkanda, Junko

AU - Lockman, Jeffrey W.

AU - Yokoyama, Kohei

AU - Gelb, Michael H.

AU - Croft, Simon L.

AU - Kendrick, Howard

AU - Harrell, Maria Isabel

AU - Feagin, Jean E.

AU - Blaskovich, Michelle A.

AU - Sebti, Said M.

AU - Hamilton, Andrew D.

N1 - Funding Information: This work was supported by grants from the National Institutes of Health (CA67771 to SMS and ADH, and CA53874 to MHG) and UNDP/World Bank/WHO Special Programme for Research and Training in Tropical Diseases to SLC.

PY - 2001/3/26

Y1 - 2001/3/26

N2 - 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.

AB - 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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ER -

Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity

Abstract

ASJC Scopus subject areas

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