Première caractérisation d’un inhibiteur allostérique des récepteurs des fibroblast growth factors

Corentin Herbert; Chantal Alcouffe; Françoise Bono

doi:10.1051/medsci/20132910007

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Volume 29 / Numéro 10 (Octobre 2013)

Med Sci (Paris), 29 10 (2013) 834-836

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Numéro		Med Sci (Paris) Volume 29, Numéro 10, Octobre 2013


Page(s)		834 - 836
Section		Nouvelles
DOI		https://doi.org/10.1051/medsci/20132910007
Publié en ligne		18 octobre 2013

Wesche J, Haglund K, Haugsten EM. Fibroblast growth factors and their receptors in cancer. Biochem J 2011 ; 437 : 199–213. [CrossRef] [PubMed] [Google Scholar]
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Thaker TM, Kaya AI, Preininger AM, et al. Allosteric mechanisms of G protein-coupled receptor signaling: a structural perspective. Methods Mol Biol 2012 ; 796 : 133–174. [CrossRef] [PubMed] [Google Scholar]
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Bono F, De Smet F, Herbert C, et al. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell 2013 ; 23 : 477–488. [CrossRef] [PubMed] [Google Scholar]
Herbert C, Schieborr U, Saxena K, et al. Molecular Mechanism of SSR128129E, an extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling. Cancer Cell 2013 ; 23 : 489–501. [CrossRef] [PubMed] [Google Scholar]
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[1] Wesche J, Haglund K, Haugsten EM. Fibroblast growth factors and their receptors in cancer. Biochem J 2011 ; 437 : 199–213. [CrossRef] [PubMed] [Google Scholar]

[2] Beenken A, Mohammadi M. The FGF family: biology, pathophysiology and therapy. Nat Rev Drug Discov 2009 ; 8 : 235–253. [CrossRef] [PubMed] [Google Scholar]

[3] Daniele G, Corral J, Molife LR, de Bono JS. FGF receptor inhibitors: role in cancer therapy. Curr Oncol Rep 2012 ; 14 : 111–119. [CrossRef] [PubMed] [Google Scholar]

[4] McDermott LA, Simcox M, Higgins B, et al. RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation. Bioorg Med Chem 2005 ; 13 : 4835–4841. [CrossRef] [PubMed] [Google Scholar]

[5] Chahrour O, Cairns D, Omran Z. Small molecule kinase inhibitors as anti-cancer therapeutics. Mini Rev Med Chem 2012 ; 12 : 399–411. [CrossRef] [PubMed] [Google Scholar]

[6] Conn PJ, Christopoulos A, Lindsley CW. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov 2009 ; 8 : 41–54. [CrossRef] [PubMed] [Google Scholar]

[7] Thaker TM, Kaya AI, Preininger AM, et al. Allosteric mechanisms of G protein-coupled receptor signaling: a structural perspective. Methods Mol Biol 2012 ; 796 : 133–174. [CrossRef] [PubMed] [Google Scholar]

[8] Sebag JA, Pantel J. Ciblage thérapeutique des récepteurs couplés aux protéines G : la voie allostérique. Med Sci (Paris) 2012 ; 28 : 845–851. [CrossRef] [EDP Sciences] [PubMed] [Google Scholar]

[9] Bono F, De Smet F, Herbert C, et al. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell 2013 ; 23 : 477–488. [CrossRef] [PubMed] [Google Scholar]

[10] Herbert C, Schieborr U, Saxena K, et al. Molecular Mechanism of SSR128129E, an extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling. Cancer Cell 2013 ; 23 : 489–501. [CrossRef] [PubMed] [Google Scholar]

[11] Christopoulos A. Allosteric binding sites on cell-surface receptors: novel targets for drug discovery. Nat Rev Drug Discov 2002 ; 1 : 198–210. [CrossRef] [PubMed] [Google Scholar]