Literature DB >> 11937331

Comparison of the inhibition of human and Trypanosoma cruzi prolyl endopeptidases.

Sandrine Vendeville1, Filip Goossens, Marie Ange Debreu-Fontaine, Valérie Landry, Elisabeth Davioud-Charvet, Philippe Grellier, Simon Scharpe, Christian Sergheraert.   

Abstract

Prolyl endopeptidases (PEPs) have been found in numerous species. Inhibitors of human enzyme could correct cognitive deficits in Alzheimer patients while inhibition of Trypanosoma cruzi PEP could prevent invasion phase in Chagas disease. A structure-activity relationship study carried out in a tetrahydroisoquinoline series allowed to obtain potent competitive inhibitors superior to SUAM-1221. Besides, inhibitors expected to act according to an irreversible mechanism revealed to be superior to JPT-4819, for applications linked to human enzyme inhibition.

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Year:  2002        PMID： 11937331     DOI： 10.1016/s0968-0896(02)00035-4

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  3 in total

1.  Molecular, functional and structural properties of the prolyl oligopeptidase of Trypanosoma cruzi (POP Tc80), which is required for parasite entry into mammalian cells.

Authors:  Izabela M D Bastos; Philippe Grellier; Natalia F Martins; Gloria Cadavid-Restrepo; Marian R de Souza-Ault; Koen Augustyns; Antonio R L Teixeira; Joseph Schrével; Bernard Maigret; José F da Silveira; Jaime M Santana
Journal:  Biochem J       Date:  2005-05-15       Impact factor: 3.857

Review 2.  Parasite prolyl oligopeptidases and the challenge of designing chemotherapeuticals for Chagas disease, leishmaniasis and African trypanosomiasis.

Authors:  I M D Bastos; F N Motta; P Grellier; J M Santana
Journal:  Curr Med Chem       Date:  2013       Impact factor: 4.530

3.  Prolyl Oligopeptidase From Leishmania infantum: Biochemical Characterization and Involvement in Macrophage Infection.

Authors:  Camila Lasse; Clênia S Azevedo; Carla N de Araújo; Flávia N Motta; Milene A Andrade; Amanda Pereira Rocha; Iracyara Sampaio; Sébastien Charneau; Marc Gèze; Philippe Grellier; Jaime M Santana; Izabela M D Bastos
Journal:  Front Microbiol       Date:  2020-05-28       Impact factor: 5.640
  3 in total

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