Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group

Glutathionylspermidine synthetase/amidase (GspS) is an essential enzyme in the biosynthesis and turnover of trypanothione and represents an attractive target for the design of selective anti-parasitic drugs. We synthesised a series of analogues of glutathione (L-γ-Glu-L-Leu-Gly-X) where the glycine...

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Autores principales:	Ravaschino, Esteban Luis, Rodríguez, Juan Bautista
Publicado:	2002
Materias:	acylsulfonamide amide boronic acid derivative carboxylic acid enzyme inhibitor glutathione glutathione derivative glutathionylspermidine synthethase glycine hydroxamic acid synthetase tetrazole derivative tripeptide unclassified drug acidity amino acid substitution amino acid synthesis article IC 50 protein analysis Amide Synthases Carboxylic Acids Enzyme Inhibitors Glutathione Glycine Oligopeptides
Acceso en línea:	https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v12_n18_p2553_Amssoms http://hdl.handle.net/20.500.12110/paper_0960894X_v12_n18_p2553_Amssoms
Aporte de:	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

id	paper:paper_0960894X_v12_n18_p2553_Amssoms
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spelling	paper:paper_0960894X_v12_n18_p2553_Amssoms2023-06-08T15:57:48Z Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group Ravaschino, Esteban Luis Rodríguez, Juan Bautista acylsulfonamide amide boronic acid derivative carboxylic acid enzyme inhibitor glutathione glutathione derivative glutathionylspermidine synthethase glycine hydroxamic acid synthetase tetrazole derivative tripeptide unclassified drug acidity amino acid substitution amino acid synthesis article IC 50 protein analysis Amide Synthases Carboxylic Acids Enzyme Inhibitors Glutathione Glycine Oligopeptides Glutathionylspermidine synthetase/amidase (GspS) is an essential enzyme in the biosynthesis and turnover of trypanothione and represents an attractive target for the design of selective anti-parasitic drugs. We synthesised a series of analogues of glutathione (L-γ-Glu-L-Leu-Gly-X) where the glycine carboxylic acid group (X) has been substituted for other acidic groups such as tetrazole, hydroxamic acid, acylsulphonamide and boronic acid. The boronic acid appears the most promising lead compound (IC50 of 17.2 μM). © 2002 Elsevier Science Ltd. All rights reserved. Fil:Ravaschino, E. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Rodriguez, J.B. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. 2002 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v12_n18_p2553_Amssoms http://hdl.handle.net/20.500.12110/paper_0960894X_v12_n18_p2553_Amssoms
institution	Universidad de Buenos Aires
institution_str	I-28
repository_str	R-134
collection	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA)
topic	acylsulfonamide amide boronic acid derivative carboxylic acid enzyme inhibitor glutathione glutathione derivative glutathionylspermidine synthethase glycine hydroxamic acid synthetase tetrazole derivative tripeptide unclassified drug acidity amino acid substitution amino acid synthesis article IC 50 protein analysis Amide Synthases Carboxylic Acids Enzyme Inhibitors Glutathione Glycine Oligopeptides
spellingShingle	acylsulfonamide amide boronic acid derivative carboxylic acid enzyme inhibitor glutathione glutathione derivative glutathionylspermidine synthethase glycine hydroxamic acid synthetase tetrazole derivative tripeptide unclassified drug acidity amino acid substitution amino acid synthesis article IC 50 protein analysis Amide Synthases Carboxylic Acids Enzyme Inhibitors Glutathione Glycine Oligopeptides Ravaschino, Esteban Luis Rodríguez, Juan Bautista Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group
topic_facet	acylsulfonamide amide boronic acid derivative carboxylic acid enzyme inhibitor glutathione glutathione derivative glutathionylspermidine synthethase glycine hydroxamic acid synthetase tetrazole derivative tripeptide unclassified drug acidity amino acid substitution amino acid synthesis article IC 50 protein analysis Amide Synthases Carboxylic Acids Enzyme Inhibitors Glutathione Glycine Oligopeptides
description	Glutathionylspermidine synthetase/amidase (GspS) is an essential enzyme in the biosynthesis and turnover of trypanothione and represents an attractive target for the design of selective anti-parasitic drugs. We synthesised a series of analogues of glutathione (L-γ-Glu-L-Leu-Gly-X) where the glycine carboxylic acid group (X) has been substituted for other acidic groups such as tetrazole, hydroxamic acid, acylsulphonamide and boronic acid. The boronic acid appears the most promising lead compound (IC50 of 17.2 μM). © 2002 Elsevier Science Ltd. All rights reserved.
author	Ravaschino, Esteban Luis Rodríguez, Juan Bautista
author_facet	Ravaschino, Esteban Luis Rodríguez, Juan Bautista
author_sort	Ravaschino, Esteban Luis
title	Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group
title_short	Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group
title_full	Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group
title_fullStr	Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group
title_full_unstemmed	Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group
title_sort	glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. part 1: substitution of the glycine carboxylic acid group
publishDate	2002
url	https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v12_n18_p2553_Amssoms http://hdl.handle.net/20.500.12110/paper_0960894X_v12_n18_p2553_Amssoms
work_keys_str_mv	AT ravaschinoestebanluis glutathioneliketripeptidesasinhibitorsofglutathionylspermidinesynthetasepart1substitutionoftheglycinecarboxylicacidgroup AT rodriguezjuanbautista glutathioneliketripeptidesasinhibitorsofglutathionylspermidinesynthetasepart1substitutionoftheglycinecarboxylicacidgroup
_version_	1768544604347432960

Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group

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