Zobrazeno 1 - 10 of 86 pro vyhledávání: '"Thierry, Lomberget"'
1
Akademický článek
Cancer selective cell death induction by a bivalent CK2 inhibitor targeting the ATP site and the allosteric αD pocket
Autor: Alexandre Bancet, Rita Frem, Florian Jeanneret, Angélique Mularoni, Pauline Bazelle, Caroline Roelants, Jean-Guy Delcros, Jean-François Guichou, Catherine Pillet, Isabelle Coste, Toufic Renno, Christophe Battail, Claude Cochet, Thierry Lomberget, Odile Filhol, Isabelle Krimm
Publikováno v: iScience, Vol 27, Iss 2, Pp 108903- (2024)
Summary: Although the involvement of protein kinase CK2 in cancer is well-documented, there is a need for selective CK2 inhibitors suitable for investigating CK2 specific roles in cancer-related biological pathways and further exploring its therapeut
Externí odkaz: https://doaj.org/article/41eefb09154c47d1a837761d86fb8080
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2
Akademický článek
In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts
Autor: Ghina Alameh, Agnès Emptoz-Bonneton, Marc Rolland de Ravel, Eva L. Matera, Elisabeth Mappus, Patrick Balaguer, Luc Rocheblave, Thierry Lomberget, Charles Dumontet, Marc Le Borgne, Michel Pugeat, Catherine Grenot, Claude Y. Cuilleron
Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 684-691 (2019)
Synthetic progesterone and 5α/β-pregnane-3,20-dione derivatives were evaluated as in vitro and in vivo modulators of multidrug-resistance (MDR) using two P-gp-expressing human cell lines, the non-steroidogenic K562/R7 erythroleukaemia cells and the
Externí odkaz: https://doaj.org/article/55b0290ee7904a11adb07838554e6862
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5
Pharmacomodulation of a ligand targeting the HBV capsid hydrophobic pocket
Autor: Mathilde Briday, François Hallé, Lauriane Lecoq, Sylvie Radix, Juliette Martin, Roland Montserret, Marie Dujardin, Marie-Laure Fogeron, Michael Nassal, Beat H. Meier, Thierry Lomberget, Anja Böckmann
Publikováno v: Chemical Science, 13 (30)
Hepatitis B virus (HBV) is a small enveloped retrotranscribing DNA virus and an important human pathogen. Its capsid-forming core protein (Cp) features a hydrophobic pocket proposed to be central notably in capsid envelopment. Indeed, mutations in an
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcbe6ac2592fec220726c542109d7fc6
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6
Akademický článek
In Search of Small Molecule Inhibitors Targeting the Flexible CK2 Subunit Interface
Autor: Benoît Bestgen, Zakia Belaid-Choucair, Thierry Lomberget, Marc Le Borgne, Odile Filhol, Claude Cochet
Publikováno v: Pharmaceuticals, Vol 10, Iss 1, p 16 (2017)
Protein kinase CK2 is a tetrameric holoenzyme composed of two catalytic (α and/or α’) subunits and two regulatory (β) subunits. Crystallographic data paired with fluorescence imaging techniques have suggested that the formation of the CK2 holoen
Externí odkaz: https://doaj.org/article/0f8d4e0a389a48888fcf88e77cc213fa
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7
Fragment Linking Strategies for Structure-Based Drug Design
Autor: Alexandre Bancet, Claire Raingeval, Thierry Lomberget, Jean-François Guichou, Isabelle Krimm, Marc Le Borgne
Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2020, 63 (20), pp.11420-11435. ⟨10.1021/acs.jmedchem.0c00242⟩
Journal of Medicinal Chemistry, 2020, 63 (20), pp.11420-11435. ⟨10.1021/acs.jmedchem.0c00242⟩
International audience; Fragment-based drug discovery is a strategy widely used in both academia and pharmaceutical companies to generate small-molecule protein inhibitors and drug candidates. Among the approaches reported in the literature (growing,
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c05ee129f575cbff72f7c36846be933
https://hal.archives-ouvertes.fr/hal-03045139
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8
Discovery of holoenzyme-disrupting chemicals as substrate-selective CK2 inhibitors
Autor: Ruben Abagyan, Renaud Prudent, Thierry Lomberget, Céline F. Sautel, Béatrice Laudet, Matthias Engel, Isabelle Krimm, Odile Filhol, Marc Le Borgne, Irina Kufareva, Mohamed Ettaoussi, Claude Cochet, Paul Brear, Benoit Bestgen, Virginie Moucadel
Publikováno v: Scientific Reports
Scientific Reports, Nature Publishing Group, 2019, 9 (1), ⟨10.1038/s41598-019-52141-5⟩
Scientific Reports, Nature Publishing Group, 2019, 9 (1), pp.15893. ⟨10.1038/s41598-019-52141-5⟩
Scientific Reports, 2019, 9 (1), pp.15893. ⟨10.1038/s41598-019-52141-5⟩
Scientific reports, vol 9, iss 1
Scientific Reports, Vol 9, Iss 1, Pp 1-16 (2019)
CK2 is a constitutively active protein kinase overexpressed in numerous malignancies. Interaction between CK2α and CK2β subunits is essential for substrate selectivity. The CK2α/CK2β interface has been previously targeted by peptides to achieve f
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb42963b4bb31b7a9a23b98e865c8e28
https://hal.archives-ouvertes.fr/hal-02466039
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9
Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies
Autor: Thierry Lomberget, Jordane Preto, Abdelfattah Faouzi, Cong Viet Do, Alexandre Arnaud, Marion Verrière, Caroline Barette, Alexandre Bancet, Marie-Odile Fauvarque, Roland Barret, Zineb Bousfiha, Amaury Farce, Lars Petter Jordheim, Thi Thanh Binh Nguyen
Publikováno v: European Journal of Medicinal Chemistry. 215:113275
Combretastatin A-4 inspired heterocyclic derivatives were synthesized and evaluated for their biological activities on tubulin polymerization and cell proliferation. Among the 19 described sulfur-containing compounds, derivatives (Z)-4h and (Z)-4j ex
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c344e855b8654f20eab79087cd723fe2
https://doi.org/10.1016/j.ejmech.2021.113275
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10
Determination of surfactant bio-sourced origin by isotope-ratio mass spectrometry
Autor: Magali Batteau, Anthony Anchisi, Yohann Clément, Alexandra Gaubert, Patrick Jame, Hervé Casabianca, Pierre Lanteri, Claire Bordes, Thierry Lomberget, Sylvie Guibert
Publikováno v: Rapid Communications in Mass Spectrometry. 30:1108-1114
RATIONALE To develop more eco-friendly laundry detergents, renewable surfactants synthesized from vegetal sources are increasingly being used. In a more stringent regulation context, the determination of bio-sourced surfactant origin thus appears ess
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fbcf4cd36fd575a1f6826888b9e6041d
https://doi.org/10.1002/rcm.7537
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