• Plateforme de criblage KISSf - FR2424 Station Biologique de Roscoff
• Place Georges Teissier
• CS 90074
• 29688 ROSCOFF Cedex
• Tél : 02 98 29 23 65
• Email : beatrice.josselin@sb-roscoff.fr
• Site internet : www.sb-roscoff.fr/fr/station-biologique-de-roscoff/services/plateformes-technologiques/kissf-plate-forme-de-criblage-d-inhibiteurs-de-proteines-kinases

Plateforme

• Kinase Inhibitor Specialized Screening facility - KISSf - FR2424/ CNRS/ Sorbonne Univ.

Brevets / Publications / Communications

2021

Choudhary BS, Sukanya, Mehta P, Bach S, Ruchaud S, Robert T, Josselin B, Filipek S, Malik R. Discovery of thiazolidin-4-one analogue as selective GSK-3β inhibitor through structure based virtual screening. Bioorg Med Chem Lett. 2021 Nov 15;52:128375. doi: 10.1016/j.bmcl.2021.128375.

Juillet C, Ermolenko L, Boyarskaya D, Baratte B, Josselin B, Nedev H, Bach S, Iorga BI, Bignon J, Ruchaud S, Al-Mourabit A. From Synthetic Simplified Marine Metabolite Analogues to New Selective Allosteric Inhibitor of Aurora B Kinase. J Med Chem. 2021 Jan 28;64(2):1197-1219. doi: 10.1021/acs.jmedchem.0c02064.

2020

 Elie J, Feizbakhsh O, Desban N, Josselin B, Baratte B, Bescond A, Duez J, Fant X, Bach S, Marie D, Place M, Ben Salah S, Chartier A, Berteina-Raboin S, Chaikuad A, Knapp S, Carles F, Bonnet P, Buron F, Routier S, Ruchaud S. Design of new disubstituted imidazo[1,2-b]pyridazine derivatives as selective Haspin inhibitors. Synthesis, binding mode and anticancer biological evaluation. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1840-1853. doi: 10.1080/14756366.2020.1825408.

 Benchekroun M, Ermolenko L, Tran MQ, Vagneux A, Nedev H, Delehouzé C, Souab M, Baratte B, Josselin B, Iorga BI, Ruchaud S, Bach S, Al-Mourabit A. Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1. Eur J Med Chem. 2020 Sep 1;201:112337. doi: 10.1016/j.ejmech.2020.112337.

Qhobosheane MA, Legoabe LJ, Josselin B, Bach S, Ruchaud S, Beteck RM. Synthesis and evaluation of C3 substituted chalcone-based derivatives of 7-azaindole as protein kinase inhibitors. Chem Biol Drug Des. 2020 Dec;96(6):1395-1407. doi: 10.1111/cbdd.13748.

Ibrahim N, Bonnet P, Brion JD, Peyrat JF, Bignon J, Levaique H, Josselin B, Robert T, Colas P, Bach S, Messaoudi S, Alami M, Hamze A. Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency. Eur J Med Chem. 2020 Aug 1;199:112355. doi: 10.1016/j.ejmech.2020.112355.

Qhobosheane MA, Legoabe LJ, Josselin B, Bach S, Ruchaud S, Petzer JP, Beteck RM. Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors. Bioorg Med Chem. 2020 Jun 1;28(11):115468. doi: 10.1016/j.bmc.2020.115468.

2019

 Zeinyeh W, Esvan YJ, Josselin B, Baratte B, Bach S, Nauton L, Théry V, Ruchaud S, Anizon F, Giraud F, Moreau P. Kinase inhibitions in pyrido[4,3-h] and [3,4-g]quinazolines: Synthesis, SAR and molecular modeling studies. Bioorg Med Chem. 2019 May 15;27(10):2083-2089. doi: 10.1016/j.bmc.2019.04.005.

Oukoloff K, Coquelle N, Bartolini M, Naldi M, Le Guevel R, Bach S, Josselin B, Ruchaud S, Catto M, Pisani L, Denora N, Iacobazzi RM, Silman I, Sussman JL, Buron F, Colletier JP, Jean L, Routier S, Renard PY. Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3. Eur J Med Chem. 2019 Apr 15;168:58-77. doi: 10.1016/j.ejmech.2018.12.063.

Tazarki H, Zeinyeh W, Esvan YJ, Knapp S, Chatterjee D, Schröder M, Joerger AC, Khiari J, Josselin B, Baratte B, Bach S, Ruchaud S, Anizon F, Giraud F, Moreau P. New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis. Eur J Med Chem. 2019 Mar 15;166:304-317. doi: 10.1016/j.ejmech.2019.01.052.

Motuhi SE, Feizbakhsh O, Foll-Josselin B, Baratte B, Delehouzé C, Cousseau A, Fant X, Bulinski JC, Payri CE, Ruchaud S, Mehiri M, Bach S. Neurymenolide A, a Novel Mitotic Spindle Poison from the New Caledonian Rhodophyta Phacelocarpus neurymenioides. Mar Drugs. 2019 Feb 1;17(2):93. doi: 10.3390/md17020093.

Masłyk M, Janeczko M, Martyna A, Czernik S, Tokarska-Rodak M, Chwedczuk M, Foll-Josselin B, Ruchaud S, Bach S, Demchuk OM, Kubiński K. The Anti-Candida albicans Agent 4-AN Inhibits Multiple Protein Kinases.  Molecules. 2019 Jan 2;24(1):153. doi: 10.3390/molecules24010153.