Substituted α-mercaptoketones, new types of specific neprilysin inhibitors

Autor: Simon Leiris, Rémi Patouret, Marie-Claude Fournie-Zaluski, Tanja Ouimet, Hervé Poras, Bernard P. Roques

Publikováno v: Bioorganic & Medicinal Chemistry Letters
Bioorganic & Medicinal Chemistry Letters, 2017, 27 (16), pp.3883-3890. ⟨10.1016/j.bmcl.2017.06.050⟩

International audience; New neprilysin inhibitors containing an alpha-mercaptoketone HSC((RR2)-R-1)CO group, as zinc ligand were designed. Two parameters were explored for potency optimization: the size of the inhibitor which could interact with the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9411e861939bab86b816c14d00b9419
https://pubmed.ncbi.nlm.nih.gov/28676269

Comparison of Fluorigenic Peptide Substrates PL50, SNAPtide, and BoTest A/E for BoNT/A Detection and Quantification: Exosite Binding Confers High-Assay Sensitivity

Autor: Hervé Poras, Tanja Ouimet, Marie-Claude Fournie-Zaluski, Sophie Duquesnoy, Bernard P. Roques

Publikováno v: SLAS Discovery. 18:726-735

Detection and quantification of low doses of botulinum toxin serotype A (BoNT/A) in medicinal preparations require precise and sensitive methods. With mounting pressure from governmental authorities to replace the mouse LD50 assay, interest in altern

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f4663b8a39d3d30cba2e5b519f6d7bb
https://doi.org/10.1177/1087057113476089

Highly Sensitive Quenched Fluorescent Substrate of Legionella Major Secretory Protein (Msp) Based on Its Structural Analysis

Autor: Michèle Vialette, Emilie Dange, Tanja Ouimet, Marie-Claude Fournie-Zaluski, Sophie Duquesnoy, Anthony Pinon, Hervé Poras

Publikováno v: Journal of Biological Chemistry. 287:20221-20230

Legionella pneumophila has been shown to secrete a protease termed major secretory protein (Msp). This protease belongs to the M4 family of metalloproteases and shares 62.9% sequence similarity with pseudolysin (EC 3.4.24.26). With the aim of develop

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d9b26f8b25eb8182e2c9a2b48bfcd3e
https://doi.org/10.1074/jbc.m111.334334

Pluripotentialities of a quenched fluorescent peptide substrate library: enzymatic detection, characterization, and isoenzymes differentiation

Autor: Sou-Vinh Orng, Emilie Dange, Marie-Claude Fournie-Zaluski, Hervé Poras, Tanja Ouimet, Bernard P. Roques

Publikováno v: Analytical Biochemistry. 419:95-105

Protease inhibitors represent a major class of drugs, even though a large number of proteases remain unexplored. Consequently, a great interest lies in the identification of highly sensitive substrates useful for both the characterization and the val

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::784b5bbeaab2c1c6509f523b5ca9ddeb
https://doi.org/10.1016/j.ab.2011.08.016

Involvement of enkephalins in the inhibition of osteosarcoma-induced thermal hyperalgesia evoked by the blockade of peripheral P2X3 receptors

Autor: Luis Menéndez, Marie-Claude Fournie-Zaluski, Bernard P. Roques, Agustín Hidalgo, Sara González-Rodríguez, Ana Baamonde, Marta Pevida

Publikováno v: Neuroscience Letters. 465:285-289

Although previous studies describe the up-regulation of purinergic P2X(3) receptors expressed at peripheral nociceptive fibers in experimental painful neoplastic processes, the analgesic efficacy of P2X(3) receptor antagonists has not been tested in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b35c5ef0da03a329ceea3ddb7a14e7a8
https://doi.org/10.1016/j.neulet.2009.09.015