2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase
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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Acceso en línea: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00664804_v56_n8_p4483_RodriguesPoveda http://hdl.handle.net/20.500.12110/paper_00664804_v56_n8_p4483_RodriguesPoveda |
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paper:paper_00664804_v56_n8_p4483_RodriguesPoveda2023-06-08T15:06:11Z 2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase Szajnman, Sergio Hernán Rodríguez, Juan Bautista 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 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00664804_v56_n8_p4483_RodriguesPoveda 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) |
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 Szajnman, Sergio Hernán Rodríguez, Juan Bautista 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. |
author |
Szajnman, Sergio Hernán Rodríguez, Juan Bautista |
author_facet |
Szajnman, Sergio Hernán Rodríguez, Juan Bautista |
author_sort |
Szajnman, Sergio Hernán |
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 |
https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00664804_v56_n8_p4483_RodriguesPoveda http://hdl.handle.net/20.500.12110/paper_00664804_v56_n8_p4483_RodriguesPoveda |
work_keys_str_mv |
AT szajnmansergiohernan 2alkylaminoethyl11bisphosphonicacidsarepotentinhibitorsoftheenzymaticactivityoftrypanosomacruzisqualenesynthase AT rodriguezjuanbautista 2alkylaminoethyl11bisphosphonicacidsarepotentinhibitorsoftheenzymaticactivityoftrypanosomacruzisqualenesynthase |
_version_ |
1768541978820083712 |