Design, synthesis, and evaluation of substrate – analogue inhibitors of Trypanosoma cruzi ribose 5-phosphate isomerase type B

2021 ◽  
Vol 32 ◽  
pp. 127723
Author(s):  
Soledad Natalia Gonzalez ◽  
Jonathan J. Mills ◽  
Dante Maugeri ◽  
Christopher Olaya ◽  
Breana L. Laguera ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Type B ◽  
Design Synthesis ◽  
Substrate Analogue

Design, Synthesis and Activity Against Trypanosoma cruzi of Azaheterocyclic Analogs of Megazol

2007 ◽  
Vol 3 (5) ◽  
pp. 460-465 ◽  
Author(s):  
A. Carvalho ◽  
R. Menna-Barreto ◽  
N. Romeiro ◽  
S. de Castro ◽  
N. Boechat
Keyword(s):  
Trypanosoma Cruzi ◽  
Design Synthesis

scholarly journals Ribose 5-phosphate isomerase type B from Trypanosoma cruzi: kinetic properties and site-directed mutagenesis reveal information about the reaction mechanism

2006 ◽  
Vol 401 (1) ◽  
pp. 279-285 ◽  
Author(s):  
Ana L. Stern ◽  
Emmanuel Burgos ◽  
Laurent Salmon ◽  
Juan J. Cazzulo
Keyword(s):  
Trypanosoma Cruzi ◽  
Chagas Disease ◽  
Pentose Phosphate ◽  
Site Directed Mutagenesis ◽  
Directed Mutagenesis ◽  
Kinetic Properties ◽  
Type B ◽  
Nucleotide Synthesis ◽  
Gene Coding ◽  
Genes Encoding

Trypanosoma cruzi, the human parasite that causes Chagas disease, contains a functional pentose phosphate pathway, probably essential for protection against oxidative stress and also for R5P (ribose 5-phosphate) production for nucleotide synthesis. The haploid genome of the CL Brener clone of the parasite contains one gene coding for a Type B Rpi (ribose 5-phosphate isomerase), but genes encoding Type A Rpis, most frequent in eukaryotes, seem to be absent. The RpiB enzyme was expressed in Escherichia coli as a poly-His tagged active dimeric protein, which catalyses the reversible isomerization of R5P to Ru5P (ribulose 5-phos-phate) with Km values of 4 mM (R5P) and 1.4 mM (Ru5P).4-Phospho-D-erythronohydroxamic acid, an analogue to the reaction intermediate when the Rpi acts via a mechanism involving the formation of a 1,2-cis-enediol, inhibited the enzyme competi-tively, with an IC50 value of 0.7 mM and a Ki of 1.2 mM. Site-directed mutagenesis allowed the demonstration of a role for His102, but not for His138, in the opening of the ribose furanosic ring. A major role in catalysis was confirmed for Cys69, since the C69A mutant was inactive in both forward and reverse directions of the reaction. The present paper contributes to the know-ledge of the mechanism of the Rpi reaction; in addition, the absence of RpiBs in the genomes of higher animals makes this enzyme a possible target for chemotherapy of Chagas disease.

2-(phenylthio)ethylidene derivatives as anti-Trypanosoma cruzi compounds: Structural design, synthesis and antiparasitic activity

2019 ◽  
Vol 180 ◽  
pp. 191-203 ◽  
Author(s):  
Marcos Veríssimo de Oliveira Cardoso ◽  
Gevanio Bezerra de Oliveira Filho ◽  
Lucianna Rabelo Pessoa de Siqueira ◽  
José Wanderlan Pontes Espíndola ◽  
Elany Barbosa da Silva ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Structural Design ◽  
Design Synthesis ◽  
Antiparasitic Activity

Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi

2017 ◽  
Vol 141 ◽  
pp. 346-361 ◽  
Author(s):  
Gevanio Bezerra de Oliveira Filho ◽  
Marcos Veríssimo de Oliveira Cardoso ◽  
José Wanderlan Pontes Espíndola ◽  
Dayane Albuquerque Oliveira e Silva ◽  
Rafaela Salgado Ferreira ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Structural Design ◽  
Design Synthesis ◽  
Pharmacological Evaluation

Competitive inhibitors of type B ribose 5-phosphate isomerases: design, synthesis and kinetic evaluation of new d-allose and d-allulose 6-phosphate derivatives

2009 ◽  
Vol 344 (7) ◽  
pp. 869-880 ◽  
Author(s):  
Sandrine Mariano ◽  
Annette K. Roos ◽  
Sherry L. Mowbray ◽  
Laurent Salmon
Keyword(s):  
Type B ◽  
Design Synthesis ◽  
Kinetic Evaluation ◽  
Competitive Inhibitors

Design, synthesis and enzymatic evaluation of 3- O -substituted aryl β- d -galactopyranosides as inhibitors of Trypanosoma cruzi trans -sialidase

2014 ◽  
Vol 24 (18) ◽  
pp. 4529-4532 ◽  
Author(s):  
Bruno L. Silva ◽  
José D. S. Filho ◽  
Peterson Andrade ◽  
Ivone Carvalho ◽  
Ricardo J. Alves
Keyword(s):  
Trypanosoma Cruzi ◽  
Design Synthesis

Design, synthesis, molecular modelling, and in vitro evaluation of tricyclic coumarins against Trypanosoma cruzi

2018 ◽  
Vol 93 (3) ◽  
pp. 337-350 ◽  
Author(s):  
Gleicekelly Silva Coelho ◽  
Josimara Souza Andrade ◽  
Viviane Flores Xavier ◽  
Policarpo Ademar Sales Junior ◽  
Barbara Caroline Rodrigues de Araujo ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Molecular Modelling ◽  
Design Synthesis ◽  
In Vitro Evaluation

scholarly journals Design, Synthesis, Calorimetry, and Crystallographic Analysis of 2-Alkylaminoethyl-1,1-bisphosphonates as Inhibitors of Trypanosoma cruzi Farnesyl Diphosphate Synthase

2012 ◽  
Vol 55 (14) ◽  
pp. 6445-6454 ◽  
Author(s):  
Srinivas Aripirala ◽  
Sergio H. Szajnman ◽  
Jean Jakoncic ◽  
Juan B. Rodriguez ◽  
Roberto Docampo ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Crystallographic Analysis ◽  
Farnesyl Diphosphate ◽  
Farnesyl Diphosphate Synthase ◽  
Design Synthesis

Design, synthesis and evaluation of novel uracil amino acid conjugates for the inhibition of Trypanosoma cruzi dUTPase

2006 ◽  
Vol 16 (14) ◽  
pp. 3809-3812 ◽  
Author(s):  
Orla K. Mc Carthy ◽  
Alessandro Schipani ◽  
Alex Musso Buendía ◽  
Luis M. Ruiz-Perez ◽  
Marcel Kaiser ◽  
...  
Keyword(s):  
Amino Acid ◽  
Trypanosoma Cruzi ◽  
Design Synthesis ◽  
Amino Acid Conjugates
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