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

Autores
Rodrígues-Poveda, C.A.; González-Pacanowska, D.; Szajnman, S.H.; Rodríguez, J.B.
Año de publicación
2012
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
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.
Fuente
Antimicrob. Agents Chemother. 2012;56(8):4483-4486
Materia
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
Nivel de accesibilidad
acceso abierto
Condiciones de uso
http://creativecommons.org/licenses/by/2.5/ar
Repositorio
Biblioteca Digital (UBA-FCEN)
Institución
Universidad Nacional de Buenos Aires. Facultad de Ciencias Exactas y Naturales
OAI Identificador
paperaa:paper_00664804_v56_n8_p4483_RodriguesPoveda
Acceder
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oai_identifier_str paperaa:paper_00664804_v56_n8_p4483_RodriguesPoveda
network_acronym_str BDUBAFCEN
repository_id_str 1896
network_name_str Biblioteca Digital (UBA-FCEN)
spelling 2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthaseRodrígues-Poveda, C.A.González-Pacanowska, D.Szajnman, S.H.Rodríguez, J.B.1,1 bisphosphonic acid derivativebisphosphonic acid derivativegeranyltransferasesqualene synthasesqualene synthase inhibitorunclassified drugarticledrug effectdrug mechanismdrug potencyenzyme activityenzyme inhibitionIC 50nonhumanpriority journalTrypanosoma cruziAntiparasitic AgentsChagas DiseaseDiphosphonatesFarnesyl-Diphosphate FarnesyltransferaseGeranyltranstransferaseParasitic Sensitivity TestsStructure-Activity RelationshipTrypanocidal AgentsTrypanosoma cruziAs 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.2012info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfhttp://hdl.handle.net/20.500.12110/paper_00664804_v56_n8_p4483_RodriguesPovedaAntimicrob. Agents Chemother. 2012;56(8):4483-4486reponame:Biblioteca Digital (UBA-FCEN)instname:Universidad Nacional de Buenos Aires. Facultad de Ciencias Exactas y Naturalesinstacron:UBA-FCENenginfo:eu-repo/semantics/openAccesshttp://creativecommons.org/licenses/by/2.5/ar2025-09-04T09:48:47Zpaperaa:paper_00664804_v56_n8_p4483_RodriguesPovedaInstitucionalhttps://digital.bl.fcen.uba.ar/Universidad públicaNo correspondehttps://digital.bl.fcen.uba.ar/cgi-bin/oaiserver.cgiana@bl.fcen.uba.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:18962025-09-04 09:48:49.262Biblioteca Digital (UBA-FCEN) - Universidad Nacional de Buenos Aires. Facultad de Ciencias Exactas y Naturalesfalse
dc.title.none.fl_str_mv 2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase
title 2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase
spellingShingle 2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase
Rodrígues-Poveda, C.A.
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
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
dc.creator.none.fl_str_mv Rodrígues-Poveda, C.A.
González-Pacanowska, D.
Szajnman, S.H.
Rodríguez, J.B.
author Rodrígues-Poveda, C.A.
author_facet Rodrígues-Poveda, C.A.
González-Pacanowska, D.
Szajnman, S.H.
Rodríguez, J.B.
author_role author
author2 González-Pacanowska, D.
Szajnman, S.H.
Rodríguez, J.B.
author2_role author
author
author
dc.subject.none.fl_str_mv 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
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
dc.description.none.fl_txt_mv 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.
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.
publishDate 2012
dc.date.none.fl_str_mv 2012
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/20.500.12110/paper_00664804_v56_n8_p4483_RodriguesPoveda
url http://hdl.handle.net/20.500.12110/paper_00664804_v56_n8_p4483_RodriguesPoveda
dc.language.none.fl_str_mv eng
language eng
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
http://creativecommons.org/licenses/by/2.5/ar
eu_rights_str_mv openAccess
rights_invalid_str_mv http://creativecommons.org/licenses/by/2.5/ar
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv Antimicrob. Agents Chemother. 2012;56(8):4483-4486
reponame:Biblioteca Digital (UBA-FCEN)
instname:Universidad Nacional de Buenos Aires. Facultad de Ciencias Exactas y Naturales
instacron:UBA-FCEN
reponame_str Biblioteca Digital (UBA-FCEN)
collection Biblioteca Digital (UBA-FCEN)
instname_str Universidad Nacional de Buenos Aires. Facultad de Ciencias Exactas y Naturales
instacron_str UBA-FCEN
institution UBA-FCEN
repository.name.fl_str_mv Biblioteca Digital (UBA-FCEN) - Universidad Nacional de Buenos Aires. Facultad de Ciencias Exactas y Naturales
repository.mail.fl_str_mv ana@bl.fcen.uba.ar
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score 12.623145

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