Výsledky vyhledávání - "Muriel, Gelin"

Akademický článek

Fragment-based discovery of a new family of non-peptidic small-molecule cyclophilin inhibitors with potent antiviral activities

Autor: Abdelhakim Ahmed-Belkacem, Lionel Colliandre, Nazim Ahnou, Quentin Nevers, Muriel Gelin, Yannick Bessin, Rozenn Brillet, Olivier Cala, Dominique Douguet, William Bourguet, Isabelle Krimm, Jean-Michel Pawlotsky, Jean- François Guichou

Publikováno v: Nature Communications, Vol 7, Iss 1, Pp 1-11 (2016)

Cyclophilins play a key role in the life cycle of many viruses and represent important drug targets for broad-spectrum antiviral therapies. Here, the authors use fragment-based drug discovery to develop non-peptidic inhibitors of human cyclophilins w

Externí odkaz: https://doaj.org/article/39ec7c8e931548f1a43d8bd4de43a06f

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Structure‐based design, synthesis and biological evaluation of a NAD+ analogue targeting Pseudomonas aeruginosa NAD kinase

Autor: Rahila Rahimova, Pauline Nogaret, Valérie Huteau, Muriel Gelin, David A. Clément, Gilles Labesse, Sylvie Pochet, Anne‐Béatrice Blanc‐Potard, Corinne Lionne

Publikováno v: FEBS Journal
FEBS Journal, 2023, 290 (2), pp.482-501. ⟨10.1111/febs.16604⟩

International audience; Multi-drug resistance is a major public health problem that requires the urgent development of new antibiotics and therefore the identification of novel bacterial targets. The activity of nicotinamide adenine dinucleotide kina

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e4db5351ff34c7b5c26f7b045216087
https://hal.science/hal-03765406

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Akademický článek

New Chemical Probe Targeting Bacterial NAD Kinase

Autor: David A. Clément, Clarisse Leseigneur, Muriel Gelin, Dylan Coelho, Valérie Huteau, Corinne Lionne, Gilles Labesse, Olivier Dussurget, Sylvie Pochet

Publikováno v: Molecules, Vol 25, Iss 21, p 4893 (2020)

Nicotinamide adenine dinucleotide (NAD) kinases are essential and ubiquitous enzymes involved in the tight regulation of NAD/nicotinamide adenine dinucleotide phosphate (NADP) levels in many metabolic pathways. Consequently, they represent promising

Externí odkaz: https://doaj.org/article/44ffd8ae00fd408e8ebb615e36417972

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Synthesis and structure-activity relationship studies of original cyclic diadenosine derivatives as nanomolar inhibitors of NAD kinase from pathogenic bacteria

Autor: David A. Clément, Muriel Gelin, Clarisse Leseigneur, Valérie Huteau, Lou Mondange, Jean-Luc Pons, Olivier Dussurget, Corinne Lionne, Gilles Labesse, Sylvie Pochet

Publikováno v: European journal of medicinal chemistry. 246

Nicotinamide adenine dinucleotide kinases (NAD kinases) are essential and ubiquitous enzymes involved in the production of NADP(H) which is an essential cofactor in many metabolic pathways. Targeting NAD kinase (NADK), a rate limiting enzyme of NADP

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f95eb760a9086f91c0e0e90ccf232fe
https://pubmed.ncbi.nlm.nih.gov/36455355

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Structure-based design, synthesis and biological evaluation of a NAD

Autor: Rahila, Rahimova, Pauline, Nogaret, Valérie, Huteau, Muriel, Gelin, David A, Clément, Gilles, Labesse, Sylvie, Pochet, Anne-Béatrice, Blanc-Potard, Corinne, Lionne

Publikováno v: The FEBS journalReferences.

Multidrug resistance is a major public health problem that requires the urgent development of new antibiotics and therefore the identification of novel bacterial targets. The activity of nicotinamide adenine dinucleotide kinase, NADK, is essential in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::8d4954113025d152292308e178151bbd
https://pubmed.ncbi.nlm.nih.gov/36036789

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Structure-Based and Knowledge-Informed Design of B-Raf Inhibitors Devoid of Deleterious PXR Binding

Autor: Melanie Schneider, Vanessa Delfosse, Muriel Gelin, Marina Grimaldi, Meritxell Granell, Laurène Heriaud, Jean-Luc Pons, Martin Cohen Gonsaud, Patrick Balaguer, William Bourguet, Gilles Labesse

Publikováno v: Journal of medicinal chemistry. 65(2)

Dabrafenib is an anticancer drug currently used in the clinics, alone or in combination. However, dabrafenib was recently shown to potently activate the human nuclear receptor pregnane X receptor (PXR). PXR activation increases the clearance of vario

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::caf2206d2619a6b92fece59fe7c0b160
https://pubmed.ncbi.nlm.nih.gov/34958586

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Discovery of a cryptic site at the interface 2 of TEAD – Towards a new family of YAP/TAZ-TEAD inhibitors

Autor: Jean-François Guichou, Manon Sturbaut, Romain Magnez, Marie-Christine Chartier-Harlin, Patricia Melnyk, Martine Pugnière, Maxime Liberelle, Pasquale Sileo, Philippe Cotelle, Xavier Thuru, Muriel Gelin, Fabrice Bailly, Mathilde Coevoet, Frédéric Allemand

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2021, 226, pp.113835. ⟨10.1016/j.ejmech.2021.113835⟩
European Journal of Medicinal Chemistry, 2021, 226, pp.113835. ⟨10.1016/j.ejmech.2021.113835⟩

International audience; The Hippo pathway is involved in organ size control and tissue homeostasis by regulating cell growth, proliferation and apoptosis. It controls the phosphorylation of the transcription co-activator YAP (Yes associated protein)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7429a293a362569302e5cdb8210bf10b
https://hal.archives-ouvertes.fr/hal-03429462

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Small-Molecule Inhibitors of Cyclophilins Block Opening of the Mitochondrial Permeability Transition Pore and Protect Mice From Hepatic Ischemia/Reperfusion Injury

Autor: Muriel Gelin, Fred Allemand, Cong Trung Nguyen, Mathieu Panel, Abdelhakim Ahmed-Belkacem, Bijan Ghaleh, Rozenn Brillet, Isaac Ruiz, Julien Calderaro, Fouad Lafdil, Jean-François Guichou, Fatima Teixeira-Clerc, Didier Morin, Jean-Michel Pawlotsky

Publikováno v: Gastroenterology
Gastroenterology, 2019, 157 (5), pp.1368-1382. ⟨10.1053/j.gastro.2019.07.026⟩
Gastroenterology, WB Saunders, 2019, 157 (5), pp.1368-1382. ⟨10.1053/j.gastro.2019.07.026⟩
Gastroenterology, Elsevier, 2019, 157 (5), pp.1368-1382. ⟨10.1053/j.gastro.2019.07.026⟩

International audience; Background & Aims: Hepatic ischemia-reperfusion injury is a complication of liver surgery that involves mitochondrial dysfunction resulting from mitochondrial permeability transition pore (mPTP) opening. Cyclophilin D (PPIF or

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::424ff5ba006afde654f849b4425268c0
https://doi.org/10.1053/j.gastro.2019.07.026

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Crystal structure of human NADK2 reveals a dimeric organization and active site occlusion by lysine acetylation

Autor: Charline Mary, Mona Hoseini Soflaee, Rushendhiran Kesavan, Muriel Gelin, Harrison Brown, G. Zacharias, Thomas P. Mathews, Andrew Lemoff, Corinne Lionne, Gilles Labesse, Gerta Hoxhaj

Publikováno v: Molecular Cell
Molecular Cell, In press, 82 (17), pp.3299-3311.e8. ⟨10.1016/j.molcel.2022.06.026⟩

Submitted document; International audience; NAD+ kinases (NADKs) are metabolite kinases that phosphorylate NAD+ molecules to make NADP+, a limiting substrate for the generation of reducing power NADPH. NADK2 sustains mitochondrial NADPH production th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::815c3abada04e55d08d1b241520253bd
https://doi.org/10.1016/j.molcel.2022.06.026

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