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Abstract:

As part of our efforts aimed at searching for new antiparasitic agents, the effect of representative 2-alkylaminoethyl-1,1-bisphosphonic acids on Trypanosoma cruzi squalene synthase (TcSQS) was investigated. These compounds had proven to be potent inhibitors of T. cruzi. This cellular activity had been associated with an inhibition of the enzymatic activity of T. cruzi farnesyl diphosphate synthase. 2-Alkylaminoethyl-1,1-bisphosphonic acids appear to have a dual action, since they also inhibit TcSQS at the nanomolar range. Copyright © 2012, American Society for Microbiology. All Rights Reserved.

Registro:

Documento: Artículo
Título:2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase
Autor:Rodrígues-Poveda, C.A.; González-Pacanowska, D.; Szajnman, S.H.; Rodríguez, J.B.
Filiación:Instituto de Parasitología Y Biomedicina López-Neyra, Consejo Superior de Investigaciones Científicas, Parque Tecnológico de Ciencias de la Salud, Granada, Spain
Departamento de Química Orgánica and UMYMFOR (CONICET-FCEyN), Facultad de Ciencias Exactas Y Naturales, Universidad de Buenos Aires, Buenos Aires, Argentina
Palabras clave:1,1 bisphosphonic acid derivative; bisphosphonic acid derivative; geranyltransferase; squalene synthase; squalene synthase inhibitor; unclassified drug; article; drug effect; drug mechanism; drug potency; enzyme activity; enzyme inhibition; IC 50; nonhuman; priority journal; Trypanosoma cruzi; Antiparasitic Agents; Chagas Disease; Diphosphonates; Farnesyl-Diphosphate Farnesyltransferase; Geranyltranstransferase; Parasitic Sensitivity Tests; Structure-Activity Relationship; Trypanocidal Agents; Trypanosoma cruzi
Año:2012
Volumen:56
Número:8
Página de inicio:4483
Página de fin:4486
DOI: http://dx.doi.org/10.1128/AAC.00796-12
Título revista:Antimicrobial Agents and Chemotherapy
Título revista abreviado:Antimicrob. Agents Chemother.
ISSN:00664804
CODEN:AMACC
CAS:geranyltransferase, 37277-79-5, 50812-36-7; squalene synthase, 9077-14-9; Antiparasitic Agents; Diphosphonates; Farnesyl-Diphosphate Farnesyltransferase, 2.5.1.21; Geranyltranstransferase, 2.5.1.10; Trypanocidal Agents
PDF:https://bibliotecadigital.exactas.uba.ar/download/paper/paper_00664804_v56_n8_p4483_RodriguesPoveda.pdf
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00664804_v56_n8_p4483_RodriguesPoveda

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Citas:

---------- APA ----------
Rodrígues-Poveda, C.A., González-Pacanowska, D., Szajnman, S.H. & Rodríguez, J.B. (2012) . 2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase. Antimicrobial Agents and Chemotherapy, 56(8), 4483-4486.
http://dx.doi.org/10.1128/AAC.00796-12
---------- CHICAGO ----------
Rodrígues-Poveda, C.A., González-Pacanowska, D., Szajnman, S.H., Rodríguez, J.B. "2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase" . Antimicrobial Agents and Chemotherapy 56, no. 8 (2012) : 4483-4486.
http://dx.doi.org/10.1128/AAC.00796-12
---------- MLA ----------
Rodrígues-Poveda, C.A., González-Pacanowska, D., Szajnman, S.H., Rodríguez, J.B. "2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase" . Antimicrobial Agents and Chemotherapy, vol. 56, no. 8, 2012, pp. 4483-4486.
http://dx.doi.org/10.1128/AAC.00796-12
---------- VANCOUVER ----------
Rodrígues-Poveda, C.A., González-Pacanowska, D., Szajnman, S.H., Rodríguez, J.B. 2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase. Antimicrob. Agents Chemother. 2012;56(8):4483-4486.
http://dx.doi.org/10.1128/AAC.00796-12