Abstract:
We investigated the molecular basis of the activity of 4-phenoxyphenoxyethyl thiocyanate (WC-9) against Trypanosoma cruzi, the etiological agent of Chagas' disease. We found that growth inhibition of T. cruzi epimastigotes induced by this compound was associated with a reduction in the content of the parasite's endogenous sterols due to a specific blockade of their de novo synthesis at the level of squalene synthase.
Registro:
Documento: |
Artículo
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Título: | Mechanism of action of 4-phenoxyphenoxyethyl thiocyanate (WC-9) against Trypanosoma cruzi, the causative agent of Chagas' disease |
Autor: | Urbina, J.A.; Concepcion, J.L.; Montalvetti, A.; Rodriguez, J.B.; Docampo, R. |
Filiación: | Laboratorio de Quimica Biologica, Centro de Bioquimica y Biofisica, Inst. Venezolano de Invest. Cie., Km. 11, Carretera Panamericana, Caracas 1020, Venezuela Lab. de Enzimologia de Parasitos, Departamento de Biologia, Universidad de Los Andes, La Hechicera, Merida, Venezuela Department of Pathobiology, College of Veterinary Medicine, University of Illinois, Urbana, IL 61802, United States Departamento de Quimica Organica, Fac. de Ciencias Exactas y Naturales, Universidad de Buenos Aires, RA-1428 Buenos Aires, Argentina
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Palabras clave: | 4 phenoxyphenoxyethyl thiocyanate; antiprotozoal agent; squalene synthase; sterol; unclassified drug; wc 9; antiprotozoal activity; article; Chagas disease; controlled study; drug activity; drug mechanism; epimastigote; growth inhibition; nonhuman; priority journal; sterol synthesis; Trypanosoma cruzi; Alkyl and Aryl Transferases; Animals; Dose-Response Relationship, Drug; Ergosterol; Farnesyl-Diphosphate Farnesyltransferase; Geranyltranstransferase; Humans; Microbial Sensitivity Tests; Phenyl Ethers; Thiocyanates; Trypanocidal Agents; Trypanosoma cruzi |
Año: | 2003
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Volumen: | 47
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Número: | 6
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Página de inicio: | 2047
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Página de fin: | 2050
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DOI: |
http://dx.doi.org/10.1128/AAC.47.6.2047-2050.2003 |
Título revista: | Antimicrobial Agents and Chemotherapy
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Título revista abreviado: | Antimicrob. Agents Chemother.
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ISSN: | 00664804
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CODEN: | AMACC
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CAS: | squalene synthase, 9077-14-9; 4-phenoxyphenoxyethyl thiocyanate; Alkyl and Aryl Transferases, EC 2.5.-; Ergosterol, 57-87-4; Farnesyl-Diphosphate Farnesyltransferase, EC 2.5.1.21; Geranyltranstransferase, EC 2.5.1.10; Phenyl Ethers; Thiocyanates; Trypanocidal Agents
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PDF: | https://bibliotecadigital.exactas.uba.ar/download/paper/paper_00664804_v47_n6_p2047_Urbina.pdf |
Registro: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00664804_v47_n6_p2047_Urbina |
Referencias:
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Citas:
---------- APA ----------
Urbina, J.A., Concepcion, J.L., Montalvetti, A., Rodriguez, J.B. & Docampo, R.
(2003)
. Mechanism of action of 4-phenoxyphenoxyethyl thiocyanate (WC-9) against Trypanosoma cruzi, the causative agent of Chagas' disease. Antimicrobial Agents and Chemotherapy, 47(6), 2047-2050.
http://dx.doi.org/10.1128/AAC.47.6.2047-2050.2003---------- CHICAGO ----------
Urbina, J.A., Concepcion, J.L., Montalvetti, A., Rodriguez, J.B., Docampo, R.
"Mechanism of action of 4-phenoxyphenoxyethyl thiocyanate (WC-9) against Trypanosoma cruzi, the causative agent of Chagas' disease"
. Antimicrobial Agents and Chemotherapy 47, no. 6
(2003) : 2047-2050.
http://dx.doi.org/10.1128/AAC.47.6.2047-2050.2003---------- MLA ----------
Urbina, J.A., Concepcion, J.L., Montalvetti, A., Rodriguez, J.B., Docampo, R.
"Mechanism of action of 4-phenoxyphenoxyethyl thiocyanate (WC-9) against Trypanosoma cruzi, the causative agent of Chagas' disease"
. Antimicrobial Agents and Chemotherapy, vol. 47, no. 6, 2003, pp. 2047-2050.
http://dx.doi.org/10.1128/AAC.47.6.2047-2050.2003---------- VANCOUVER ----------
Urbina, J.A., Concepcion, J.L., Montalvetti, A., Rodriguez, J.B., Docampo, R. Mechanism of action of 4-phenoxyphenoxyethyl thiocyanate (WC-9) against Trypanosoma cruzi, the causative agent of Chagas' disease. Antimicrob. Agents Chemother. 2003;47(6):2047-2050.
http://dx.doi.org/10.1128/AAC.47.6.2047-2050.2003