Force et spécificité du criblage pour des molécules bioactives au CMBA-Grenoble - Une plate-forme dédiée à la découverte et à l’analyse de molécules bioactives et candidats médicaments

Caroline Barette; Emmanuelle Soleilhac; Céline Charavay; Claude Cochet; Marie-Odile Fauvarque

doi:10.1051/medsci/20153104017

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Volume 31 / Numéro 4 (Avril 2015)

Med Sci (Paris), 31 4 (2015) 423-431

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Chémobiologie

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Numéro		Med Sci (Paris) Volume 31, Numéro 4, Avril 2015 Chémobiologie


Page(s)		423 - 431
Section		M/S Revues
DOI		https://doi.org/10.1051/medsci/20153104017
Publié en ligne		8 mai 2015

Arrowsmith J. A decade of change. Nat Rev Drug Discov 2012 ; 11 : 17–18. [CrossRef] [PubMed] [Google Scholar]
Zheng W, Thorne N, McKew JC. Phenotypic screens as a renewed approach for drug discovery. Drug Discov Today 2013 ; 18 : 1067–1073. [CrossRef] [PubMed] [Google Scholar]
Prudent R, Vassal-Stermann E, Nguyen CH, et al. Pharmacological inhibition of LIM kinase stabilizes microtubules and inhibits neoplastic growth. Cancer Res 2012 ; 72 : 4429–4439. [CrossRef] [PubMed] [Google Scholar]
Moucadel V, Prudent R, Sautel CF, et al. Antitumoral activity of allosteric inhibitors of protein kinase CK2. Oncotarget 2011 ; 2 : 997–1010. [PubMed] [Google Scholar]
Prudent R, Moucadel V, Nguyen CH, et al. Antitumor activity of pyridocarbazole and benzopyridoindole derivatives that inhibit protein kinase CK2. Cancer Res 2010 ; 70 : 9865–9874. [CrossRef] [PubMed] [Google Scholar]
Lopez-Ramos M, Prudent R, Moucadel V, et al. New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights. FASEB J 2010 ; 24 : 3171–3185. [CrossRef] [PubMed] [Google Scholar]
Prudent R, Hasenknopf B, Cochet C Les polyoxométallates : des inhibiteurs inorganiques de la protéine kinase CK2. Med Sci (Paris) 2008 ; 24 : 1012–1014. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]
Prudent R, Moucadel V, Laudet B, et al. Identification of polyoxometalates as nanomolar noncompetitive inhibitors of protein kinase CK2. Chem Biol 2008 ; 15 : 683–692. [CrossRef] [PubMed] [Google Scholar]
Prudent R, Cochet C. New protein kinase CK2 inhibitors: jumping out of the catalytic box. Chem Biol 2009 ; 16 : 112–120. [CrossRef] [PubMed] [Google Scholar]
Hibert MF. French/European academic compound library initiative. Drug Discov Today 2009 ; 14 : 723–725. [CrossRef] [PubMed] [Google Scholar]
Prudent R, Soleilhac E, Barette C, et al. Les criblages phénotypiques ou comment faire d’une pierre deux coups. Med Sci (Paris) 2013 ; 29 : 897–905. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]
Hoang TMN, Favier B, Valette A, et al. Benzo[e]pyridoindoles, novel inhibitors of the aurora kinases. Cell Cycle 2009 ; 8 : 765–772. [CrossRef] [PubMed] [Google Scholar]
Camara D, Bisanz C, Barette C, et al. Inhibition of p-aminobenzoate and folate syntheses in plants and apicomplexan parasites by natural product rubreserine. J Biol Chem 2012 ; 287 : 22367–22376. [CrossRef] [PubMed] [Google Scholar]
Boussouar A, Barette C, Nadon R, et al. Acacetin and chrysin, two polyphenolic compounds, alleviate telomeric position effect in human cells. Mol Ther Nucleic Acids 2013 ; 2 : e116. [CrossRef] [PubMed] [Google Scholar]
Deininger M, Buchdunger E, Druker BJ. The development of imatinib as a therapeutic agent for chronic myeloid leukemia. Blood 2005 ; 105 : 2640–2653. [CrossRef] [PubMed] [Google Scholar]
Kawasumi M, Nghiem P. Chemical genetics: elucidating biological systems with small-molecule compounds. J Invest Dermatol 2007 ; 127 : 1577–1584. [CrossRef] [PubMed] [Google Scholar]
O’Connor CJ, Laraia L, Spring DR. Chemical genetics. Chem Soc Rev 2011 ; 40 : 4332–4345. [CrossRef] [PubMed] [Google Scholar]
McPherson A, Nguyen C, Cudney R, et al. The role of small molecule additives and chemical modification in protein crystallization. Cryst Growth Des 2011 ; 11 : 1469–1474. [CrossRef] [Google Scholar]
Laramas M, Pasquier D, Filhol O, et al. Nuclear localization of protein kinase CK2 catalytic subunit (CK2alpha) is associated with poor prognostic factors in human prostate cancer. Eur J Cancer 2007 ; 43 : 928–934. [CrossRef] [PubMed] [Google Scholar]
Giusiano S, Cochet C, Filhol O, et al. Protein kinase CK2alpha subunit over-expression correlates with metastatic risk in breast carcinomas: quantitative immunohistochemistry in tissue microarrays. Eur J Cancer 2011 ; 47 : 792–801. [CrossRef] [PubMed] [Google Scholar]
Buchou T, Cochet C. La protéine kinase CK2, une enzyme qui cultive la différence. Med Sci (Paris) 2003 ; 19 : 709–716. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]
Filhol O, Martiel JL, Cochet C. Protein kinase CK2: a new view of an old molecular complex. EMBO Rep 2004 ; 5 : 351–355. [CrossRef] [PubMed] [Google Scholar]
Laudet B, Barette C, Dulery V, et al. Structure-based design of small peptide inhibitors of protein kinase CK2 subunit interaction. Biochem J 2007 ; 408 : 363–373. [CrossRef] [PubMed] [Google Scholar]
Laudet B, Prudent R, Filhol O, et al. Des agents thérapeutiques ciblant des interactions protéine-protéine. Med Sci (Paris) 2007 ; 23 : 273–278. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]
Moffat JG, Rudolph J, Bailey D. Phenotypic screening in cancer drug discovery-past, present and future. Nat Rev Drug Discov 2014 ; 13 : 588–602. [CrossRef] [PubMed] [Google Scholar]
Brodin P, Del Nery, Elaine, Soleilhac E. Criblage phénotypique à haut contenu pour la chémobiologie et ses enjeux. Med Sci (Paris) 2015 ; 31 : 187–196. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]
Vassal E, Barette C, Fonrose X, et al. Miniaturization and validation of a sensitive multiparametric cell-based assay for the concomitant detection of microtubule-destabilizing and microtubule-stabilizing agents. J Biomol Screen 2006 ; 11 : 377–389. [CrossRef] [PubMed] [Google Scholar]
Eggert US, Mitchison TJ. Small molecule screening by imaging. Curr Opin Chem Biol 2006 ; 10 : 232–237. [CrossRef] [PubMed] [Google Scholar]
Korn K, Krausz E. Cell-based high-content screening of small-molecule libraries. Curr Opin Chem Biol 2007 ; 11 : 503–510. [CrossRef] [PubMed] [Google Scholar]
Soleilhac E, Nadon R, Lafanechere L. High-content screening for the discovery of pharmacological compounds: advantages, challenges and potential benefits of recent technological developments. Expert Opin Drug Discov 2010 ; 5 : 135–144. [CrossRef] [PubMed] [Google Scholar]
Martinez A, Soleilhac E, Barette C, et al. Novel synthetic pharmacophores inducing a stabilization of cellular microtubules. Curr Cancer Drug Targets 2014 ; 15 : 2–13. [CrossRef] [Google Scholar]
Lo E, Soleilhac E, Martinez A, et al. Intensity quantile estimation and mapping: a novel algorithm for the correction of image non-uniformity bias in HCS data. Bioinforma Oxf Engl 2012 ; 28 : 2632–2639. [CrossRef] [PubMed] [Google Scholar]
Murie C, Barette C, Lafanechere L, et al. Single assay-wide variance experimental (SAVE) design for high-throughput screening. Bioinforma Oxf Engl 2013 ; 29 : 3067–3072. [CrossRef] [Google Scholar]
Murie C, Barette C, Lafanechère L, et al. Control-plate regression (CPR) normalization for high-throughput screens with many active features. J Biomol Screen 2014 ; 19 : 661–671. [CrossRef] [PubMed] [Google Scholar]
Murie C, Barette C, Button J, et al. Improving detection of rare biological events in high-throughput screens. J Biomol Screen 2014 ; 20 : 230–241. [CrossRef] [PubMed] [Google Scholar]
Thomas CJ, Auld DS, Huang R, et al. The pilot phase of the NIH chemical genomics center. Curr Top Med Chem 2009 ; 9 : 1181–1193. [CrossRef] [PubMed] [Google Scholar]
Voisset C, Blondel M. Chémobiologie à l’happy hour : la levure comme modèle de criblage pharmacologique. Med Sci (Paris) 2014 ; 30 : 1161–1168. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]
Mahuteau-Betzer F. Chimiothèque Nationale : avancées et perspectives. Med Sci (Paris) 2015 ; 31 : 417–422. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]
Vidalain PO, Lucas-Hourani M, Helynck O, Tangy F, Munier-Lehmann H. Activation de la réponse innée antivirale par des inhibiteurs de la biosynthèse des pyrimidines : les surprises d’un criblage phénotypique. Med Sci (Paris) 2015 ; 31 : 98–104. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]

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[1] Arrowsmith J. A decade of change. Nat Rev Drug Discov 2012 ; 11 : 17–18. [CrossRef] [PubMed] [Google Scholar]

[2] Zheng W, Thorne N, McKew JC. Phenotypic screens as a renewed approach for drug discovery. Drug Discov Today 2013 ; 18 : 1067–1073. [CrossRef] [PubMed] [Google Scholar]

[3] Prudent R, Vassal-Stermann E, Nguyen CH, et al. Pharmacological inhibition of LIM kinase stabilizes microtubules and inhibits neoplastic growth. Cancer Res 2012 ; 72 : 4429–4439. [CrossRef] [PubMed] [Google Scholar]

[4] Moucadel V, Prudent R, Sautel CF, et al. Antitumoral activity of allosteric inhibitors of protein kinase CK2. Oncotarget 2011 ; 2 : 997–1010. [PubMed] [Google Scholar]

[5] Prudent R, Moucadel V, Nguyen CH, et al. Antitumor activity of pyridocarbazole and benzopyridoindole derivatives that inhibit protein kinase CK2. Cancer Res 2010 ; 70 : 9865–9874. [CrossRef] [PubMed] [Google Scholar]

[6] Lopez-Ramos M, Prudent R, Moucadel V, et al. New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights. FASEB J 2010 ; 24 : 3171–3185. [CrossRef] [PubMed] [Google Scholar]

[7] Prudent R, Hasenknopf B, Cochet C Les polyoxométallates : des inhibiteurs inorganiques de la protéine kinase CK2. Med Sci (Paris) 2008 ; 24 : 1012–1014. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]

[8] Prudent R, Moucadel V, Laudet B, et al. Identification of polyoxometalates as nanomolar noncompetitive inhibitors of protein kinase CK2. Chem Biol 2008 ; 15 : 683–692. [CrossRef] [PubMed] [Google Scholar]

[9] Prudent R, Cochet C. New protein kinase CK2 inhibitors: jumping out of the catalytic box. Chem Biol 2009 ; 16 : 112–120. [CrossRef] [PubMed] [Google Scholar]

[10] Hibert MF. French/European academic compound library initiative. Drug Discov Today 2009 ; 14 : 723–725. [CrossRef] [PubMed] [Google Scholar]

[11] Prudent R, Soleilhac E, Barette C, et al. Les criblages phénotypiques ou comment faire d’une pierre deux coups. Med Sci (Paris) 2013 ; 29 : 897–905. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]

[12] Hoang TMN, Favier B, Valette A, et al. Benzo[e]pyridoindoles, novel inhibitors of the aurora kinases. Cell Cycle 2009 ; 8 : 765–772. [CrossRef] [PubMed] [Google Scholar]

[13] Camara D, Bisanz C, Barette C, et al. Inhibition of p-aminobenzoate and folate syntheses in plants and apicomplexan parasites by natural product rubreserine. J Biol Chem 2012 ; 287 : 22367–22376. [CrossRef] [PubMed] [Google Scholar]

[14] Boussouar A, Barette C, Nadon R, et al. Acacetin and chrysin, two polyphenolic compounds, alleviate telomeric position effect in human cells. Mol Ther Nucleic Acids 2013 ; 2 : e116. [CrossRef] [PubMed] [Google Scholar]

[15] Deininger M, Buchdunger E, Druker BJ. The development of imatinib as a therapeutic agent for chronic myeloid leukemia. Blood 2005 ; 105 : 2640–2653. [CrossRef] [PubMed] [Google Scholar]

[16] Kawasumi M, Nghiem P. Chemical genetics: elucidating biological systems with small-molecule compounds. J Invest Dermatol 2007 ; 127 : 1577–1584. [CrossRef] [PubMed] [Google Scholar]

[17] O’Connor CJ, Laraia L, Spring DR. Chemical genetics. Chem Soc Rev 2011 ; 40 : 4332–4345. [CrossRef] [PubMed] [Google Scholar]

[18] McPherson A, Nguyen C, Cudney R, et al. The role of small molecule additives and chemical modification in protein crystallization. Cryst Growth Des 2011 ; 11 : 1469–1474. [CrossRef] [Google Scholar]

[19] Laramas M, Pasquier D, Filhol O, et al. Nuclear localization of protein kinase CK2 catalytic subunit (CK2alpha) is associated with poor prognostic factors in human prostate cancer. Eur J Cancer 2007 ; 43 : 928–934. [CrossRef] [PubMed] [Google Scholar]

[20] Giusiano S, Cochet C, Filhol O, et al. Protein kinase CK2alpha subunit over-expression correlates with metastatic risk in breast carcinomas: quantitative immunohistochemistry in tissue microarrays. Eur J Cancer 2011 ; 47 : 792–801. [CrossRef] [PubMed] [Google Scholar]

[21] Buchou T, Cochet C. La protéine kinase CK2, une enzyme qui cultive la différence. Med Sci (Paris) 2003 ; 19 : 709–716. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]

[22] Filhol O, Martiel JL, Cochet C. Protein kinase CK2: a new view of an old molecular complex. EMBO Rep 2004 ; 5 : 351–355. [CrossRef] [PubMed] [Google Scholar]

[23] Laudet B, Barette C, Dulery V, et al. Structure-based design of small peptide inhibitors of protein kinase CK2 subunit interaction. Biochem J 2007 ; 408 : 363–373. [CrossRef] [PubMed] [Google Scholar]

[24] Laudet B, Prudent R, Filhol O, et al. Des agents thérapeutiques ciblant des interactions protéine-protéine. Med Sci (Paris) 2007 ; 23 : 273–278. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]

[25] Moffat JG, Rudolph J, Bailey D. Phenotypic screening in cancer drug discovery-past, present and future. Nat Rev Drug Discov 2014 ; 13 : 588–602. [CrossRef] [PubMed] [Google Scholar]

[26] Brodin P, Del Nery, Elaine, Soleilhac E. Criblage phénotypique à haut contenu pour la chémobiologie et ses enjeux. Med Sci (Paris) 2015 ; 31 : 187–196. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]

[27] Vassal E, Barette C, Fonrose X, et al. Miniaturization and validation of a sensitive multiparametric cell-based assay for the concomitant detection of microtubule-destabilizing and microtubule-stabilizing agents. J Biomol Screen 2006 ; 11 : 377–389. [CrossRef] [PubMed] [Google Scholar]

[28] Eggert US, Mitchison TJ. Small molecule screening by imaging. Curr Opin Chem Biol 2006 ; 10 : 232–237. [CrossRef] [PubMed] [Google Scholar]

[29] Korn K, Krausz E. Cell-based high-content screening of small-molecule libraries. Curr Opin Chem Biol 2007 ; 11 : 503–510. [CrossRef] [PubMed] [Google Scholar]

[30] Soleilhac E, Nadon R, Lafanechere L. High-content screening for the discovery of pharmacological compounds: advantages, challenges and potential benefits of recent technological developments. Expert Opin Drug Discov 2010 ; 5 : 135–144. [CrossRef] [PubMed] [Google Scholar]

[31] Martinez A, Soleilhac E, Barette C, et al. Novel synthetic pharmacophores inducing a stabilization of cellular microtubules. Curr Cancer Drug Targets 2014 ; 15 : 2–13. [CrossRef] [Google Scholar]

[32] Lo E, Soleilhac E, Martinez A, et al. Intensity quantile estimation and mapping: a novel algorithm for the correction of image non-uniformity bias in HCS data. Bioinforma Oxf Engl 2012 ; 28 : 2632–2639. [CrossRef] [PubMed] [Google Scholar]

[33] Murie C, Barette C, Lafanechere L, et al. Single assay-wide variance experimental (SAVE) design for high-throughput screening. Bioinforma Oxf Engl 2013 ; 29 : 3067–3072. [CrossRef] [Google Scholar]

[34] Murie C, Barette C, Lafanechère L, et al. Control-plate regression (CPR) normalization for high-throughput screens with many active features. J Biomol Screen 2014 ; 19 : 661–671. [CrossRef] [PubMed] [Google Scholar]

[35] Murie C, Barette C, Button J, et al. Improving detection of rare biological events in high-throughput screens. J Biomol Screen 2014 ; 20 : 230–241. [CrossRef] [PubMed] [Google Scholar]

[36] Thomas CJ, Auld DS, Huang R, et al. The pilot phase of the NIH chemical genomics center. Curr Top Med Chem 2009 ; 9 : 1181–1193. [CrossRef] [PubMed] [Google Scholar]

[37] Voisset C, Blondel M. Chémobiologie à l’happy hour : la levure comme modèle de criblage pharmacologique. Med Sci (Paris) 2014 ; 30 : 1161–1168. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]

[38] Mahuteau-Betzer F. Chimiothèque Nationale : avancées et perspectives. Med Sci (Paris) 2015 ; 31 : 417–422. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]

[39] Vidalain PO, Lucas-Hourani M, Helynck O, Tangy F, Munier-Lehmann H. Activation de la réponse innée antivirale par des inhibiteurs de la biosynthèse des pyrimidines : les surprises d’un criblage phénotypique. Med Sci (Paris) 2015 ; 31 : 98–104. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]