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Items: 1 to 20 of 61


1D NMR WaterLOGSY as an efficient method for fragment-based lead discovery.

Raingeval C, Cala O, Brion B, Le Borgne M, Hubbard RE, Krimm I.

J Enzyme Inhib Med Chem. 2019 Dec;34(1):1218-1225. doi: 10.1080/14756366.2019.1636235.


Synthesis and biological evaluation of zinc chelating compounds as metallo-β-lactamase inhibitors.

Kildahl-Andersen G, Schnaars C, Prandina A, Radix S, Le Borgne M, Jordheim LP, Gjøen T, Andresen AMS, Lauksund S, Fröhlich C, Samuelsen Ø, Rongved P, Åstrand OAH.

Medchemcomm. 2019 Mar 8;10(4):528-537. doi: 10.1039/c8md00578h. eCollection 2019 Apr 1.


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.

Alameh G, Emptoz-Bonneton A, Rolland de Ravel M, Matera EL, Mappus E, Balaguer P, Rocheblave L, Lomberget T, Dumontet C, Le Borgne M, Pugeat M, Grenot C, Cuilleron CY.

J Enzyme Inhib Med Chem. 2019 Dec;34(1):684-691. doi: 10.1080/14756366.2019.1575825.


2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site.

Bestgen B, Krimm I, Kufareva I, Kamal AAM, Seetoh WG, Abell C, Hartmann RW, Abagyan R, Cochet C, Le Borgne M, Engel M, Lomberget T.

J Med Chem. 2019 Feb 28;62(4):1803-1816. doi: 10.1021/acs.jmedchem.8b01766. Epub 2019 Feb 18.


2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action.

Bestgen B, Kufareva I, Seetoh W, Abell C, Hartmann RW, Abagyan R, Le Borgne M, Filhol O, Cochet C, Lomberget T, Engel M.

J Med Chem. 2019 Feb 28;62(4):1817-1836. doi: 10.1021/acs.jmedchem.8b01765. Epub 2019 Feb 13.


Behaviour of Tetrabenazine in Acid Medium: Reassessment and Impact on Formulation.

Ettouati L, Senta-Loys Z, Bourgeois S, Fenet B, Borgne ML, Fessi H.

Pharmaceutics. 2019 Jan 20;11(1). pii: E44. doi: 10.3390/pharmaceutics11010044.


Synthesis and Preclinical Evaluation of TPA-Based Zinc Chelators as Metallo-β-lactamase Inhibitors.

Schnaars C, Kildahl-Andersen G, Prandina A, Popal R, Radix S, Le Borgne M, Gjøen T, Andresen AMS, Heikal A, Økstad OA, Fröhlich C, Samuelsen Ø, Lauksund S, Jordheim LP, Rongved P, Åstrand OAH.

ACS Infect Dis. 2018 Sep 14;4(9):1407-1422. doi: 10.1021/acsinfecdis.8b00137. Epub 2018 Aug 2.


Synthesis, X-ray structure, in silico calculation, and carbonic anhydrase inhibitory properties of benzylimidazole metal complexes.

Bouchouit M, Bouacida S, Zouchoune B, Merazig H, Bua S, Bouaziz Z, Le Borgne M, Supuran CT, Bouraiou A.

J Enzyme Inhib Med Chem. 2018 Dec;33(1):1150-1159. doi: 10.1080/14756366.2018.1481404.


Synthesis, Spectroscopic Characterization, and In Vitro Antibacterial Evaluation of Novel Functionalized Sulfamidocarbonyloxyphosphonates.

Bouzina A, Bechlem K, Berredjem H, Belhani B, Becheker I, Lebreton J, Le Borgne M, Bouaziz Z, Marminon C, Berredjem M.

Molecules. 2018 Jul 10;23(7). pii: E1682. doi: 10.3390/molecules23071682.


Structure-based design and profiling of novel 17β-HSD14 inhibitors.

Braun F, Bertoletti N, Möller G, Adamski J, Frotscher M, Guragossian N, Madeira Gírio PA, Le Borgne M, Ettouati L, Falson P, Müller S, Vollmer G, Heine A, Klebe G, Marchais-Oberwinkler S.

Eur J Med Chem. 2018 Jul 15;155:61-76. doi: 10.1016/j.ejmech.2018.05.029. Epub 2018 May 22.


Inhibition of Shiga toxin-converting bacteriophage development by novel antioxidant compounds.

Bloch S, Nejman-Faleńczyk B, Pierzynowska K, Piotrowska E, Węgrzyn A, Marminon C, Bouaziz Z, Nebois P, Jose J, Le Borgne M, Saso L, Węgrzyn G.

J Enzyme Inhib Med Chem. 2018 Dec;33(1):639-650. doi: 10.1080/14756366.2018.1444610.


Self-Assembled Supramolecular Nanoparticles Improve the Cytotoxic Efficacy of CK2 Inhibitor THN7.

Nacereddine A, Bollacke A, Róka E, Marminon C, Bouaziz Z, Fenyvesi F, Bácskay IK, Jose J, Perret F, Le Borgne M.

Pharmaceuticals (Basel). 2018 Jan 26;11(1). pii: E10. doi: 10.3390/ph11010010.


Enhancement of iodinin solubility by encapsulation into cyclodextrin nanoparticles.

Prandina A, Herfindal L, Radix S, Rongved P, Døskeland SO, Le Borgne M, Perret F.

J Enzyme Inhib Med Chem. 2018 Dec;33(1):370-375. doi: 10.1080/14756366.2017.1421638.


Unexpected Binding Mode of a Potent Indeno[1,2-b]indole-Type Inhibitor of Protein Kinase CK2 Revealed by Complex Structures with the Catalytic Subunit CK2α and Its Paralog CK2α'.

Hochscherf J, Lindenblatt D, Witulski B, Birus R, Aichele D, Marminon C, Bouaziz Z, Le Borgne M, Jose J, Niefind K.

Pharmaceuticals (Basel). 2017 Dec 13;10(4). pii: E98. doi: 10.3390/ph10040098.


The combined use of analytical tools for exploring tetanus toxin and tetanus toxoid structures.

Bayart C, Peronin S, Jean E, Paladino J, Talaga P, Borgne ML.

J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Jun 1;1054:80-92. doi: 10.1016/j.jchromb.2017.04.009. Epub 2017 Apr 4.


Sleep Disorders and Therapeutic Management: A Survey in a French Population of Prisoners.

Goudard A, Lalande L, Bertin C, Sautereau M, Le Borgne M, Cabelguenne D.

J Correct Health Care. 2017 Apr;23(2):193-202. doi: 10.1177/1078345817700163. Epub 2017 Mar 30.


An Updated View on an Emerging Target: Selected Papers from the 8th International Conference on Protein Kinase CK2.

Jose J, Le-Borgne M, Pinna LA, Montenarh M.

Pharmaceuticals (Basel). 2017 Mar 23;10(2). pii: E33. doi: 10.3390/ph10020033.


In Search of Small Molecule Inhibitors Targeting the Flexible CK2 Subunit Interface.

Bestgen B, Belaid-Choucair Z, Lomberget T, Le Borgne M, Filhol O, Cochet C.

Pharmaceuticals (Basel). 2017 Feb 3;10(1). pii: E16. doi: 10.3390/ph10010016.


Development of Pharmacophore Model for Indeno[1,2-b]indoles as Human Protein Kinase CK2 Inhibitors and Database Mining.

Haidar S, Bouaziz Z, Marminon C, Laitinen T, Poso A, Le Borgne M, Jose J.

Pharmaceuticals (Basel). 2017 Jan 9;10(1). pii: E8. doi: 10.3390/ph10010008.


2-Indolylmethylenebenzofuranones as first effective inhibitors of ABCC2.

Baiceanu E, Nguyen KA, Gonzalez-Lobato L, Nasr R, Baubichon-Cortay H, Loghin F, Le Borgne M, Chow L, Boumendjel A, Peuchmaur M, Falson P.

Eur J Med Chem. 2016 Oct 21;122:408-418. doi: 10.1016/j.ejmech.2016.06.039. Epub 2016 Jun 27.


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