Výsledky vyhledávání - "Valérie Landry"

Identification of indole-based activators of insulin degrading enzyme

Autor: Julie Charton, Clara Maillard, Chau Phi Dinh, Adrien Herledan, Florence Leroux, Catherine Piveteau, Benoit Deprez, Isabelle Duplan, Nicolas Kraupner, Nathalie Hennuyer, Xiaoan Wen, Rebecca Deprez-Poulain, Damien Bosc, Sandrine Warenghem, Bart Staels, Valérie Landry

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, 2021, pp.113982. ⟨10.1016/j.ejmech.2021.113982⟩
European Journal of Medicinal Chemistry, Elsevier, 2021, pp.113982. ⟨10.1016/j.ejmech.2021.113982⟩

International audience; Insulin degrading enzyme (IDE) is a zinc metalloprotease that cleaves numerous substrates among which amyloid-β and insulin. It has been linked through genetic studies to the risk of type-2 diabetes (T2D) or Alzheimer's disea

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15ed5fe0bfb1f46856b4bc660d9fb3a7
https://hal.science/hal-03430475

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NMR spectroscopy of the main protease of SARS‐CoV‐2 and fragment‐based screening identify three protein hotspots and an antiviral fragment

Autor: Florence Leroux, Julie Charton, François-Xavier Cantrelle, Xavier Hanoulle, Sandrine Belouzard, Danai Moschidi, Isabelle Landrieu, Lucile Brier, Jean Dubuisson, Valérie Landry, Emmanuelle Boll, Benoit Deprez, Frédérique Dewitte

Publikováno v: Angewandte Chemie International Edition
Angewandte Chemie International Edition, In press, 60 (48), pp.25428-25435. ⟨10.1002/anie.202109965⟩
Angewandte Chemie International Edition, Wiley-VCH Verlag, In press, 60 (48), pp.25428-25435. ⟨10.1002/anie.202109965⟩
Angewandte Chemie (International Ed. in English)

The main protease (3CLp) of the SARS‐CoV‐2, the causative agent for the COVID‐19 pandemic, is one of the main targets for drug development. To be active, 3CLp relies on a complex interplay between dimerization, active site flexibility, and allo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b9f57c9062d78db7309da0eef562a88
https://hal.science/hal-03363607

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Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening

Autor: Valérie Landry, Valentin Guillaume, Julie Charton, Florence Leroux, Wei-Jen Tang, Terence Beghyn, Sandrine Warenghem, Wenguang G. Liang, Sarah Urata, Virginie Pottiez, Paul Hermant, Li Sheng, Rebecca Deprez-Poulain, Damien Bosc, Adrien Herledan, Benoit Deprez

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, 2019, 179, pp.557-566. ⟨10.1016/j.ejmech.2019.06.057⟩
European Journal of Medicinal Chemistry, Elsevier, 2019, 179, pp.557-566. ⟨10.1016/j.ejmech.2019.06.057⟩
Eur J Med Chem

International audience; Insulin-degrading enzyme, IDE, is a metalloprotease implicated in the metabolism of key peptides such as insulin, glucagon, β-amyloid peptide. Recent studies have pointed out its broader role in the cell physiology. In order

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3d8372949902200aa76e63f083a7335
https://hal.science/hal-03243182

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Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis

Autor: Céline Crauste, Priscille Brodin, Stéphane Audebert, Vincent Delorme, Jean-Marie Galano, Matthieu Pophillat, Anaïs Bénarouche, Valérie Landry, Alexandre Guy, Thierry Durand, Phuong Chi Nguyen, Jean-François Cavalier, Luc Camoin, Stéphane Canaan

Publikováno v: Bioorganic Chemistry
Bioorganic Chemistry, 2018, 81, pp.414-424. ⟨10.1016/j.bioorg.2018.08.025⟩
Bioorganic Chemistry, Elsevier, 2018, 81, pp.414-424. ⟨10.1016/j.bioorg.2018.08.025⟩

International audience; A set of 19 oxadiazolone (OX) derivatives have been investigated for their antimycobacterial activity against two pathogenic slow-growing mycobacteria, Mycobacterium marinum and Mycobacterium bovis BCG, and the avirulent Mycob

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b05c1092d88d6aca62a70db5830dcc9
https://amu.hal.science/hal-01875577/document

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Structure–activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme

Publikováno v: European Journal of Medicinal Chemistry. 90:547-567

Insulin degrading enzyme (IDE) is a zinc metalloprotease that degrades small amyloid peptides such as amyloid-β and insulin. So far the dearth of IDE-specific pharmacological inhibitors impacts the understanding of its role in the physiopathology of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79c74dfe290bc3333504b03476d0d01a
https://doi.org/10.1016/j.ejmech.2014.12.005

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2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1

Publikováno v: ACS Chemical Biology. 10:705-714

Phenotypic screening of a quinoxaline library against replicating Mycobacterium tuberculosis led to the identification of lead compound Ty38c (3-((4-methoxybenzyl)amino)-6-(trifluoromethyl)quinoxaline-2-carboxylic acid). With an MIC99 and MBC of 3.1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::97a9ef14555ed6107ec3fddebc5347a9
https://doi.org/10.1021/cb5007163

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Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-β hydrolysis

Autor: Marion Gauriot, Virginie Pottiez, Valérie Landry, Malika Hamdane, Nathalie Hennuyer, Wei-Jen Tang, Julie Charton, Qing Guo, Olivier Sperandio, Bart Staels, Julie Dumont, Florence Leroux, Rebecca Deprez-Poulain, Xavier Marechal, Luc Buée, Marion Flipo, Benoit Deprez

Insulin degrading enzyme (IDE) is a highly conserved zinc metalloprotease that is involved in the clearance of various physiologically peptides like amyloid-beta and insulin. This enzyme has been involved in the physiopathology of diabetes and Alzhei

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a2edfeab3feb6e614eabba39bb8e78f
https://europepmc.org/articles/PMC4128174/

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A microscopic phenotypic assay for the quantification of intracellular mycobacteria adapted for high-throughput/high-content screening

Autor: Alain R. Baulard, Raffaella Iantomasi, Nathalie Deboosere, Valérie Landry, Romain Veyron-Churlet, Christophe J. Queval, Vincent Delorme, Priscille Brodin, Ok-Ryul Song

Publikováno v: Journal of visualized experiments : JoVE. (83)

Despite the availability of therapy and vaccine, tuberculosis (TB) remains one of the most deadly and widespread bacterial infections in the world. Since several decades, the sudden burst of multi- and extensively-drug resistant strains is a serious

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72d1715c87f1e5ad86791bb4aff6e42a
https://pubmed.ncbi.nlm.nih.gov/24473237

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Potent and specific inhibitors of trypanothione reductase from Trypanosoma cruzi

Autor: Sophie Girault, Valérie Landry, Marie-Ange Debreu, Louis Maes, Jean-François Dubremetz, Christian Sergheraert, Elisabeth Davioud-Charvet

Publikováno v: Bioorganic & Medicinal Chemistry. 9:837-846

In order to optimise the activity of bis(2-aminodiphenylsulfides) upon trypanothione reductase (TR) from Trypanosoma cruzi , a new series of bis(2-aminodiphenylsulfides) possessing three side chains was synthesized. Various moieties were introduced a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f2a8db675b11e9e62c24aad3600d5bc6
https://doi.org/10.1016/s0968-0896(00)00312-6

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