Team description

ImPACcell is an imaging and bioscreening platform based on High Content image Screening (HCS) and High Content Image Analysis (HCA) for detecting, analyzing and quantifying multiple components and/or functions in cells and tissues. The platform ImPACcell has settled automation and miniaturization of tests for evaluating the effects of various compounds, including chemicals and drugs (anti-cancer and others drugs) and gene silencing or gene over expression in various cell model systems and culture devices ranging from samples mounted on microscopy slides to multi well microplates and transparent specific cell devices. The added values of the platform include automation, robotization (for both cell culture and imaging) and miniaturization of tests, as well as expertise in imaging software for HCS/HCA, cell engineering and cell biology.

 

 

 

 

Role in the network

Our team will be in charge of the evaluation of the cytotoxicity of chemical inhibitors on various cell lines. Then, they will determine the impact of active inhibitors on apoptosis and proliferation. Bioscreening will be based on High Content image Screening (HCS) and High Content Image Analysis (HCA).

Involvement in tasks 5

 In vitro evaluation of compounds

Valorizations/ Collaborations

Publications / Patents

Team publications

 

Comparative localization and activity of the main drug and bile acids transporters in HepaRG cells and sandwich-cultured primary human hepatocytes. Pamela Bachour-El Azzi*, Ahmad Sharanek*, Audrey Burban, Ruoya Li, Rémy Le Guével, Ziad Abdel-Razzak, Bruno Stieger, Christiane Guguen-Guillouzo and André Guillouzo. Toxicological Sciences, 145(1), 2015, 157–168

 

Inflammatory cytokines promote the retrodifferentiation of tumor-derived hepatocyte-like cells to progenitor cells. Dubois-Pot-Schneider H, Fekir K, Coulouarn C, Glaise D, Aninat C, Jarnouen K, Le Guével R, Kubo T, Ishida S, Morel F, Corlu A. Hepatology. 2014 Dec;60(6):2077-90

 

Estrogenic Potency of Benzophenone UV Filters in Breast Cancer Cells: Proliferative and Transcriptional Activity Substantiated by Docking Analysis. Kerdivel G, Le Guevel R, Habauzit D, Brion F, Ait-Aissa S, Pakdel F. (2013) PLoS ONE 8(4): e60567.

 

Investigation of ifosfamide nephrotoxicity induced in a liver-kidney co-culture biochip. Choucha-Snouber L, Aninat C, Grsicom L, Madalinski G, Brochot C, Poleni PE, Razan F, Guillouzo CG, Legallais C, Corlu A, Leclerc E. BiotechnolBioeng. 2013 Feb;110(2):597-608. doi: 10.1002/bit.24707. Epub 2012 Aug 28.

 

The novel antibacterial compound walrycin A induces human PXR transcriptional activity. Berthier A, Oger F, Gheeraert C, Boulahtouf A, Le Guével R, Balaguer P, Staels B, Salbert G, Lefebvre P. Toxicol Sci. 2012 May;127(1):225-35. doi: 10.1093/toxsci/kfs073. Epub 2012 Feb 7.

 

Synthesis and biological evaluation of new 3-(6-hydroxyindol-2-yl)-5-(Phenyl) pyridine or pyrazine V-Shaped molecules as kinase inhibitors and cytotoxic agents. Kassis P, Brzeszcz J, Bénéteau V, Lozach O, Meijer L, Le Guével R, Guillouzo C, Lewiński K, Bourg S, Colliandre L, Routier S, Mérour JY. Eur J Med Chem. 2011 Nov;46(11):5416-34. doi:10.1016/j.ejmech.2011.08.048. Epub 2011 Sep 8

 

Automated detection of hepatotoxic compounds in human hepatocytes using HepaRG cells and image-based analysis of mitochondrial dysfunction with JC-1 dye. Le Guevel R*, Pernelle K*, Glaise D, Stasio CG, Le Charpentier T, Bouaita B, Corlu A, Guguen-Guillouzo C. ToxicolApplPharmacol. 2011 Aug 1;254(3):256-66. Epub 2011 May 4.

 

Electrochemical synthesis and characterisation of alternating tripyridyl-dipyrrole molecular strands with multiple nitrogen-based donor-acceptor binding sites. Tabatchnik-Rebillon A, Aubé C, Bakkali H, Delaunay T, Manh GT, Blot V, Thobie-Gautier C, Renault E, Soulard M, Planchat A, Le Questel JY, Le Guével R, Guguen-Guillouzo C, Kauffmann B, Ferrand Y, Huc I, Urgin K, Condon S, Léonel E, Evain M, Lebreton J, Jacquemin D, Pipelier M, Dubreuil D. Chemistry. 2010 Oct 18;16(39):11876-89. doi: 10.1002/chem.201000859

 

Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilidehydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring. Oger F, Lecorgne A, Sala E, Nardese V, Demay F, Chevance S, Desravines DC, Aleksandrova N, Le Guével R, Lorenzi S, Beccari AR, Barath P, Hart DJ, Bondon A, Carettoni D, Simonneaux G, Salbert G. J Med Chem. 2010 Mar 11;53(5):1937-50.

 

Reperfusion stress induced during intermittent selective clamping accelerates rat liver regeneration through JNK pathway. Duval H, Mbatchi SF, Grandadam S, Legendre C, Loyer P, Ribault C, Piquet-Pellorce C, Guguen-Guillouzo C, Boudjema K, Corlu A. J Hepatol. 2010 Apr;52(4):560-9. doi: 10.1016/j.jhep.2010.01.013. Epub 2010 Feb 13.

 

Drug-metabolising enzymes are down-regulated by hypoxia in differentiated human hepatoma HepaRG cells: HIF-1alpha involvement in CYP3A4 repression. Legendre C, Hori T, Loyer P, Aninat C, Ishida S, Glaise D, Lucas-Clerc C, Boudjema K, Guguen-Guillouzo C, Corlu A, Morel F. Eur J Cancer. 2009 Nov;45(16):2882-92. doi: 10.1016/j.ejca.2009.07.010. Epub 2009 Aug 18.

 

Cyclin-dependent kinase 1 plays a critical role in DNA replication control during rat liver regeneration. Garnier D, Loyer P, Ribault C, Guguen-Guillouzo C, Corlu A. Hepatology. 2009 Dec;50(6):1946-56. doi: 10.1002/hep.23225.

 

Identification of small molecule regulators of the nuclear receptor HNF4alpha based on naphthofuran scaffolds. Le Guével R, Oger F, Lecorgne A, Dudasova Z, Chevance S, Bondon A, Barath P, Simonneaux G, Salbert G. Bioorg Med Chem. 2009 Oct 1;17(19):7021-30. Epub 2009 Aug 5.

 

Synthesis and kinase inhibitory activity of novel substituted indigoids. Beauchard A, Laborie H, Rouillard H, Lozach O, Ferandin Y, Le Guével R, Guguen-Guillouzo C, Meijer L, Besson T, Thiéry V. Bioorg Med Chem. 2009 Sep 1;17(17):6257-63. Epub 2009 Jul 25.

 

Team publication in connection with the CGO

 

Prospective study directed to the synthesis of unsymmetrical linked bis-5-arylidene rhodanine derivatives via ‘‘one-pot two steps’’ reactions under microwave irradiation with their antitumor activity. WacothonKarime Coulibaly, Ludovic Paquin, Anoubile´ Bénie Yves-Alain Békro, Rémy Le Guével, Myriam Ravache, Anne Corlu,Jean Pierre Bazureau. MedicinalChemistryResearch, April 2015, Volume 24,

 

Microwave Assisted Organic Synthesis (MAOS) of New Dispacamide A Derivatives Bearing a Thiazolinone Platform, Biological Assays on Inhibition of Protein Kinases and Cell Effects. Guiheneuf, S., Paquin, L., Carreaux, F., Durieu, E., Bénédetti, B., Le Guevel, R., Corlu, A., Meijer, L. and Bazureau, J. P. CurrentMicrowaveChemistry (2014) 1 (1) 33-40

 

Design, synthesis, and biological activity of pyridopyrimidine scaffolds as novel PI3K/mTOR dual inhibitors. Saurat T, Buron F, Rodrigues N, de Tauzia ML, Colliandre L, Bourg S, Bonnet P, Guillaumet G, Akssira M, Corlu A, Guillouzo C, Berthier P, Rio P, Jourdan ML, Bénédetti H, Routier S. J Med Chem. 2014 Feb 13;57(3):613-31

 

Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors. Bruel A1, Bénéteau R, Chabanne M, Lozach O, Le Guevel R, Ravache M, Bénédetti H, Meijer L, Logé C, Robert JM. Bioorg Med ChemLett. 2014 Nov 1;24(21):5037-40

 

Synthesis of New N,N'-Bis(5-arylidene-4-oxo-4,5-dihydrothiazolin-2-yl)piperazine Derivatives Under Microwave Irradiation and Preliminary Biological Evaluation. Coulibaly WK, Paquin L, Bénié A, Bekro YA, Durieux E, Meijer L, Le Guével R, Corlu A, Bazureau JP. Sci Pharm. 2012 Dec;80(4):825-36. doi: 10.3797/scipharm.1206-04. Epub 2012 Sep 16.

 

Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. Boulahjar R, Ouach A, Matteo C, Bourg S, Ravache M, le Guével R, Marionneau S, Oullier T, Lozach O, Meijer L, Guguen-Guillouzo C, Lazar S, Akssira M, Troin Y, Guillaumet G, Routier S. J Med Chem. 2012 Nov 26;55(22):9589-606. doi: 10.1021/jm3008536. Epub 2012 Nov 1.

 

Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. Bruel A, Logé C, Tauzia ML, Ravache M, Le Guével R, Guillouzo C, Lohier JF, Oliveira Santos JS, Lozach O, Meijer L, Ruchaud S, Bénédetti H, Robert JM. Eur J Med Chem. 2012 Nov;57:225-33. doi: 10.1016/j.ejmech.2012.09.001. Epub 2012 Sep 10.