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...
| Autores: | , , , |
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| Tipo de documento: | artigo |
| Estado: | Versão publicada |
| Data de publicação: | 2012 |
| País: | Argentina |
| Recursos: | Universidad Nacional de Buenos Aires. Facultad de Ciencias Exactas y Naturales |
| Repositório: | Biblioteca Digital (UBA-FCEN) |
| Idioma: | inglês |
| OAI Identifier: | paperaa:paper_00664804_v56_n8_p4483_RodriguesPoveda |
| Acesso em linha: | http://hdl.handle.net/20.500.12110/paper_00664804_v56_n8_p4483_RodriguesPoveda |
| Access Level: | Acceso aberto |
| Palavra-chave: | 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 |
| Resumo: | 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. |
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