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Volumn 29, Issue 5, 2015, Pages 1817-1829

MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor

Author keywords

Antagonist; Medulloblastoma; Molecular modeling; Stem cell

Indexed keywords

MRT 92; PROTEIN INHIBITOR; SMOOTHENED PROTEIN; SONIC HEDGEHOG PROTEIN; TALADEGIB; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; G PROTEIN COUPLED RECEPTOR; GUANIDINE DERIVATIVE; MOLECULAR LIBRARY; MRT-92; PROTEIN BINDING; SMO PROTEIN, HUMAN;

EID: 84932607395     PISSN: 08926638     EISSN: 15306860     Source Type: Journal    
DOI: 10.1096/fj.14-267849     Document Type: Article
Times cited : (51)

References (50)
  • 4
    • 84856364898 scopus 로고    scopus 로고
    • Hedgehog trafficking, cilia and brain functions
    • Ruat, M., Roudaut, H., Ferent, J., and Traiffort, E. (2012) Hedgehog trafficking, cilia and brain functions. Differentiation 83, S97-S104
    • (2012) Differentiation , vol.83 , pp. S97-S104
    • Ruat, M.1    Roudaut, H.2    Ferent, J.3    Traiffort, E.4
  • 5
    • 84879414522 scopus 로고    scopus 로고
    • The mechanisms of Hedgehog signalling and its roles in development and disease
    • Briscoe, J., and Therond, P. P. (2013) The mechanisms of Hedgehog signalling and its roles in development and disease. Nat Rev. Mol. Cell Biol. 14, 416-429
    • (2013) Nat Rev. Mol. Cell Biol. , vol.14 , pp. 416-429
    • Briscoe, J.1    Therond, P.P.2
  • 6
    • 0037158748 scopus 로고    scopus 로고
    • Patched acts catalytically to suppress the activity of Smoothened
    • Taipale, J., Cooper, M. K., Maiti, T., and Beachy, P. A (2002) Patched acts catalytically to suppress the activity of Smoothened. Nature 418, 892-897
    • (2002) Nature , vol.418 , pp. 892-897
    • Taipale, J.1    Cooper, M.K.2    Maiti, T.3    Beachy, P.A.4
  • 8
    • 0036829397 scopus 로고    scopus 로고
    • Inhibition of Hedgehog signaling by direct binding of cyclopamine to Smoothened
    • Chen, J. K., Taipale, J., Cooper, M. K., and Beachy, P. A. (2002) Inhibition of Hedgehog signaling by direct binding of cyclopamine to Smoothened. Genes Dev. 16, 2743-27489
    • (2002) Genes Dev. , vol.16 , pp. 2743-27489
    • Chen, J.K.1    Taipale, J.2    Cooper, M.K.3    Beachy, P.A.4
  • 9
    • 84887512714 scopus 로고    scopus 로고
    • Unraveling the therapeutic potential of the Hedgehog pathway in cancer
    • Amakye, D., Jagani, Z., and Dorsch, M. (2013) Unraveling the therapeutic potential of the Hedgehog pathway in cancer. Nat Med. 19, 1410-1422
    • (2013) Nat Med. , vol.19 , pp. 1410-1422
    • Amakye, D.1    Jagani, Z.2    Dorsch, M.3
  • 10
    • 80955181031 scopus 로고    scopus 로고
    • The Hedgehog's tale: Developing strategies for targeting cancer
    • Ng, J. M., and Curran, T. (2011) The Hedgehog's tale: developing strategies for targeting cancer. Nat Rev. Cancer 11, 493-501
    • (2011) Nat Rev. Cancer , vol.11 , pp. 493-501
    • Ng, J.M.1    Curran, T.2
  • 11
    • 84874059433 scopus 로고    scopus 로고
    • Hedgehog pathway inhibitors: A patent review (2009-present)
    • Hadden, M. K. (2013) Hedgehog pathway inhibitors: a patent review (2009-present). Expert Opin TherPat 23, 345-361
    • (2013) Expert Opin TherPat , vol.23 , pp. 345-361
    • Hadden, M.K.1
  • 25
    • 62549159642 scopus 로고    scopus 로고
    • Hedgehog signal transduction by Smoothened: Pharmacologic evidence for a 2-step activation process
    • Rohatgi, R., Milenkovic, L., Corcoran, R. B., and Scott, M. P. (2009) Hedgehog signal transduction by Smoothened: pharmacologic evidence for a 2-step activation process. Proc. Natl. Acad. Sci. USA 106, 3196-3201
    • (2009) Proc. Natl. Acad. Sci. USA , vol.106 , pp. 3196-3201
    • Rohatgi, R.1    Milenkovic, L.2    Corcoran, R.B.3    Scott, M.P.4
  • 26
    • 70349932747 scopus 로고    scopus 로고
    • Towards an integrated view of Wnt signaling in development
    • Van Amerongen, R., and Nusse, R. (2009) Towards an integrated view of Wnt signaling in development. Development 136, 3205-3214
    • (2009) Development , vol.136 , pp. 3205-3214
    • Van Amerongen, R.1    Nusse, R.2
  • 28
    • 0030866154 scopus 로고    scopus 로고
    • Altered neural cell fates and medulloblastoma in mouse patched mutants
    • Goodrich, L. V., Milenković, L., Higgins, K. M., and Scott, M. P. (1997) Altered neural cell fates and medulloblastoma in mouse patched mutants. Science 277, 1109-1113
    • (1997) Science , vol.277 , pp. 1109-1113
    • Goodrich, L.V.1    Milenković, L.2    Higgins, K.M.3    Scott, M.P.4
  • 30
    • 33645211374 scopus 로고    scopus 로고
    • Purmorphamine activates the Hedgehog pathway by targeting Smoothened
    • Sinha, S., and Chen, J. K. (2006) Purmorphamine activates the Hedgehog pathway by targeting Smoothened. Nat. Chem. Biol. 2, 29-30
    • (2006) Nat. Chem. Biol. , vol.2 , pp. 29-30
    • Sinha, S.1    Chen, J.K.2
  • 31
    • 0037434582 scopus 로고    scopus 로고
    • Surflex: Fully automatic flexible molecular docking using a molecular similarity-based search engine
    • Jain, A. N. (2003) Surflex: fully automatic flexible molecular docking using a molecular similarity-based search engine. J. Med. Chem. 46, 499-511
    • (2003) J. Med. Chem. , vol.46 , pp. 499-511
    • Jain, A.N.1
  • 34
    • 67650289584 scopus 로고    scopus 로고
    • Mechanisms of Hedgehog pathway activation in cancer and implications for therapy
    • Scales, S. J., and De Sauvage, F. J. (2009) Mechanisms of Hedgehog pathway activation in cancer and implications for therapy. Trends Pharmacol. Sci. 30, 303-312
    • (2009) Trends Pharmacol. Sci. , vol.30 , pp. 303-312
    • Scales, S.J.1    De Sauvage, F.J.2
  • 35
    • 84866365997 scopus 로고    scopus 로고
    • Molecular pathways: The hedgehog signaling pathway in cancer
    • MRT-92 BLOCKS OVERLAPPING BINDING SITES OF SMO
    • McMillan, R., and Matsui, W. (2012) Molecular pathways: the hedgehog signaling pathway in cancer. Clin. Cancer Res. 18, 4883-4888 MRT-92 BLOCKS OVERLAPPING BINDING SITES OF SMO
    • (2012) Clin. Cancer Res. , vol.18 , pp. 4883-4888
    • McMillan, R.1    Matsui, W.2
  • 36
    • 84861352086 scopus 로고    scopus 로고
    • Hedgehog pathway as a drug target: Smoothened inhibitors in development
    • Lin, T. L., and Matsui, W. (2012) Hedgehog pathway as a drug target: Smoothened inhibitors in development. Onco Targets Ther 5, 47-58
    • (2012) Onco Targets Ther , vol.5 , pp. 47-58
    • Lin, T.L.1    Matsui, W.2
  • 42
    • 84891742744 scopus 로고    scopus 로고
    • Hedgehog pathway agonism: Therapeutic potential and small-molecule development
    • Hadden, M. K. (2014) Hedgehog pathway agonism: therapeutic potential and small-molecule development. ChemMedChem 9, 27-37
    • (2014) ChemMedChem , vol.9 , pp. 27-37
    • Hadden, M.K.1
  • 45
    • 34247647971 scopus 로고    scopus 로고
    • Distribution of Smoothened at hippocampal mossy fiber synapses
    • Masdeu, C., Bernard, V., Faure, H., Traiffort, E., and Ruat, M. (2007) Distribution of Smoothened at hippocampal mossy fiber synapses. Neuroreport 18, 395-399
    • (2007) Neuroreport , vol.18 , pp. 395-399
    • Masdeu, C.1    Bernard, V.2    Faure, H.3    Traiffort, E.4    Ruat, M.5
  • 46
    • 1542512393 scopus 로고    scopus 로고
    • Hedgehog interacting protein in the mature brain: Membrane-associated and soluble forms
    • Coulombe, J., Traiffort, E., Loulier, K., Faure, H., and Ruat, M. (2004) Hedgehog interacting protein in the mature brain: membrane-associated and soluble forms. Mol. Cell. Neurosci. 25, 323-333
    • (2004) Mol. Cell. Neurosci. , vol.25 , pp. 323-333
    • Coulombe, J.1    Traiffort, E.2    Loulier, K.3    Faure, H.4    Ruat, M.5
  • 48
    • 41149130332 scopus 로고    scopus 로고
    • Post-transcriptional down-regulation of Atoh1/Math1 by bone morphogenic proteins suppresses medulloblastoma development
    • Zhao, H., Ayrault, O., Zindy, F., Kim, J. H., and Roussel, M. F. (2008) Post-transcriptional down-regulation of Atoh1/Math1 by bone morphogenic proteins suppresses medulloblastoma development. Genes Dev. 22, 722-727
    • (2008) Genes Dev. , vol.22 , pp. 722-727
    • Zhao, H.1    Ayrault, O.2    Zindy, F.3    Kim, J.H.4    Roussel, M.F.5
  • 49
    • 1442358771 scopus 로고    scopus 로고
    • Modeling and mutagenesis of the binding site of Calhex 231, a novel negative allosteric modulator of the extracellular Ca (2+)-sensing receptor
    • Petrel, C., Kessler, A., Maslah, F., Dauban, P., Dodd, R. H., Rognan, D., and Ruat, M. (2003) Modeling and mutagenesis of the binding site of Calhex 231, a novel negative allosteric modulator of the extracellular Ca (2+)-sensing receptor. J. Biol. Chem. 278, 49487-49494
    • (2003) J. Biol. Chem. , vol.278 , pp. 49487-49494
    • Petrel, C.1    Kessler, A.2    Maslah, F.3    Dauban, P.4    Dodd, R.H.5    Rognan, D.6    Ruat, M.7
  • 50
    • 0015861774 scopus 로고
    • Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction
    • Cheng, Y., and Prusoff, W. H. (1973) Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 22, 3099-3108
    • (1973) Biochem. Pharmacol. , vol.22 , pp. 3099-3108
    • Cheng, Y.1    Prusoff, W.H.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.