2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase

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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 b...

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Autores principales:	Rodrígues-Poveda, C.A., González-Pacanowska, D., Szajnman, S.H., Rodríguez, J.B.
Formato:	Artículo publishedVersion
Lenguaje:	Inglés
Publicado:	2012
Materias:	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
Acceso en línea:	http://hdl.handle.net/20.500.12110/paper_00664804_v56_n8_p4483_RodriguesPoveda
Aporte de:	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

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spelling	paperaa:paper_00664804_v56_n8_p4483_RodriguesPoveda2023-06-12T16:45:42Z 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 Rodrígues-Poveda, C.A. González-Pacanowska, D. Szajnman, S.H. Rodríguez, J.B. 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 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. Fil:Szajnman, S.H. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Rodríguez, J.B. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. 2012 info:eu-repo/semantics/article info:ar-repo/semantics/artículo info:eu-repo/semantics/publishedVersion application/pdf eng info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_00664804_v56_n8_p4483_RodriguesPoveda
institution	Universidad de Buenos Aires
institution_str	I-28
repository_str	R-134
collection	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA)
language	Inglés
orig_language_str_mv	eng
topic	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
spellingShingle	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 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
topic_facet	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
description	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.
format	Artículo Artículo publishedVersion
author	Rodrígues-Poveda, C.A. González-Pacanowska, D. Szajnman, S.H. Rodríguez, J.B.
author_facet	Rodrígues-Poveda, C.A. González-Pacanowska, D. Szajnman, S.H. Rodríguez, J.B.
author_sort	Rodrígues-Poveda, C.A.
title	2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase
title_short	2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase
title_full	2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase
title_fullStr	2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase
title_full_unstemmed	2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase
title_sort	2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of trypanosoma cruzi squalene synthase
publishDate	2012
url	http://hdl.handle.net/20.500.12110/paper_00664804_v56_n8_p4483_RodriguesPoveda
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2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase

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