Výsledky vyhledávání - "Vincent Gerusz"

Vectorization Efforts To Increase Gram-Negative Intracellular Drug Concentration: A Case Study on HldE-K Inhibitors

Autor: Mayalen Oxoby, François Moreau, Elodie Drocourt, Dmytro Atamanyuk, Benoit Ledoussal, Vincent Gerusz, Fabien Faivre

Publikováno v: Journal of Medicinal Chemistry. 56:1908-1921

In this paper, we present different strategies to vectorize HldE kinase inhibitors with the goal to improve their gram-negative intracellular concentration. Syntheses and biological effects of siderophoric, aminoglycosidic, amphoteric, and polycation

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0bb30726e6c11eeafb71465e3a9f57b
https://doi.org/10.1021/jm400097h

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From Triclosan toward the Clinic: Discovery of Nonbiocidal, Potent FabI Inhibitors for the Treatment of Resistant Bacteria

Publikováno v: Journal of Medicinal Chemistry. 55:9914-9928

In this paper, we present some elements of our optimization program to decouple triclosan's specific FabI effect from its nonspecific cytotoxic component. The implementation of this strategy delivered highly specific, potent, and nonbiocidal new FabI

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8cec45f475491713180acfabe1b6f5a
https://doi.org/10.1021/jm301113w

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The MUT056399 Inhibitor of FabI Is a New Antistaphylococcal Compound

Autor: Kirsty Maher, M. Saccomani, Vincent Gerusz, L. Prouvensier, Ian Morrissey, Vanida Vongsouthi, Sonia Escaich, C. Soulama-Mouze, L. Durant, M. Oxoby, François Moreau

Publikováno v: Antimicrobial Agents and Chemotherapy. 55:4692-4697

MUT056399 is a highly potent new inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli. In vitro , MUT056399 was very active against S. aureus strains, including methicillin-susceptible S. aureus (MSSA), methicillin-resistan

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc03a8e115aafa5fca2f040a5301f25a
https://doi.org/10.1128/aac.01248-10

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Systematic Synthesis of Inhibitors of the Two First Enzymes of the Bacterial Heptose Biosynthetic Pathway: Towards Antivirulence Molecules Targeting Lipopolysaccharide Biosynthesis

Autor: Stéphanie Floquet, Maxime Durka, Stéphane P. Vincent, Mounir Andaloussi, Régis Périon, Elodie Malacain, Vincent Gerusz, Michael Bosco, Mayalen Oxoby, Abdellatif Tikad, François Moreau

Publikováno v: Chemistry - A European Journal. 17:11305-11313

L-Heptoses (L-glycero-D-manno-heptopyranoses) are constituents of the inner core of lipolysaccharide (LPS), a molecule playing key roles in the mortality of many infectious diseases as well as in the virulence of many human pathogens. The inhibition

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a6219ee91243f8ae9b5eae543828333
https://doi.org/10.1002/chem.201100396

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Towards Gram-positive antivirulence drugs: New inhibitors of Streptococcus agalactiae Stk1

Autor: Lionel Durant, Sonia Escaich, Jean-Marie Genevard, Alexis Denis, François Moreau, Mayalen Oxoby, Vincent Gerusz, Vanida Vongsouthi

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:3486-3490

Haspin is a serine/threonine kinase required for completion of normal mitosis that is highly expressed during cell proliferation, including in a number of neoplasms. Consequently, it has emerged as a potential therapeutic target in oncology. A high t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8fb23333c6fec52e747e2cf542177e92
https://doi.org/10.1016/j.bmcl.2010.05.004

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Towards Gram-negative antivirulence drugs: New inhibitors of HldE kinase

Autor: Alexis Denis, Nicolas Desroy, Sonia Escaich, Lionel Durant, Vincent Gerusz, Vanida Vongsouthi, Géraldine Le Fralliec, François Moreau, Stéphanie Floquet, Sophia Briet

Publikováno v: Bioorganic & Medicinal Chemistry. 17:1276-1289

Gram-negative bacteria lacking heptoses in their lipopolysaccharide (LPS) display attenuated virulence and increased sensitivity to human serum and to some antibiotics. Thus inhibition of bacterial heptose synthesis represents an attractive target fo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5c8e0751613ede387a95852db1e194a
https://doi.org/10.1016/j.bmc.2008.12.021

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Novel HldE-K inhibitors leading to attenuated Gram negative bacterial virulence

Autor: Nicolas Desroy, Vanida Vongsouthi, Stéphanie Floquet, Dmytro Atamanyuk, Vincent Gerusz, Géraldine LeFralliec, François Moreau, Theodore B. Verhey, Ting-Wai Lee, Lionel Durant, Yannick Bonvin, Sophia Briet, Alexis Denis, Mayalen Oxoby, Fabien Faivre, Elodie Drocourt, Sonia Escaich, Chrystelle Oliveira, Murray S. Junop

Publikováno v: Journal of medicinal chemistry. 56(4)

We report here the optimization of an HldE kinase inhibitor to low nanomolar potency, which resulted in the identification of the first reported compounds active on selected E. coli strains. One of the most interesting candidates, compound 86, was sh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2890016c6843ce1a2e7be486ac05f257
https://pubmed.ncbi.nlm.nih.gov/23409840

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Recent Advances in the Inhibition of Bacterial Fatty Acid Biosynthesis

Autor: Vincent Gerusz

Publisher Summary The bacterial fatty acid biosynthesis pathway has recently generated much interest for the development of novel classes of antibacterial agents. The organization of the bacterial fatty acid synthase type II system (FASII system) bas

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::52ae3874a21e93b4633a2b831c650bb3
https://doi.org/10.1016/s0065-7743(10)45018-6

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