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
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 https://repositoriouba.sisbi.uba.ar/gsdl/cgi-bin/library.cgi?a=d&c=artiaex&d=paper_00664804_v56_n8_p4483_RodriguesPoveda_oai
Aporte de:	Repositorio Digital de la Universidad de Buenos Aires (UBA) de Universidad de Buenos Aires

id	I28-R145-paper_00664804_v56_n8_p4483_RodriguesPoveda_oai
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spelling	I28-R145-paper_00664804_v56_n8_p4483_RodriguesPoveda_oai2024-08-16 Rodrígues-Poveda, C.A. González-Pacanowska, D. Szajnman, S.H. Rodríguez, J.B. 2012 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. application/pdf http://hdl.handle.net/20.500.12110/paper_00664804_v56_n8_p4483_RodriguesPoveda info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar Antimicrob. Agents Chemother. 2012;56(8):4483-4486 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 2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase info:eu-repo/semantics/article info:ar-repo/semantics/artículo info:eu-repo/semantics/publishedVersion https://repositoriouba.sisbi.uba.ar/gsdl/cgi-bin/library.cgi?a=d&c=artiaex&d=paper_00664804_v56_n8_p4483_RodriguesPoveda_oai
institution	Universidad de Buenos Aires
institution_str	I-28
repository_str	R-145
collection	Repositorio Digital de la Universidad de Buenos Aires (UBA)
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 https://repositoriouba.sisbi.uba.ar/gsdl/cgi-bin/library.cgi?a=d&c=artiaex&d=paper_00664804_v56_n8_p4483_RodriguesPoveda_oai
work_keys_str_mv	AT rodriguespovedaca 2alkylaminoethyl11bisphosphonicacidsarepotentinhibitorsoftheenzymaticactivityoftrypanosomacruzisqualenesynthase AT gonzalezpacanowskad 2alkylaminoethyl11bisphosphonicacidsarepotentinhibitorsoftheenzymaticactivityoftrypanosomacruzisqualenesynthase AT szajnmansh 2alkylaminoethyl11bisphosphonicacidsarepotentinhibitorsoftheenzymaticactivityoftrypanosomacruzisqualenesynthase AT rodriguezjb 2alkylaminoethyl11bisphosphonicacidsarepotentinhibitorsoftheenzymaticactivityoftrypanosomacruzisqualenesynthase
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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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