메뉴 건너뛰기




Volumn 43, Issue 12, 2018, Pages 1033-1046

Structural and Druggability Landscape of Frizzled G Protein-Coupled Receptors

Author keywords

class Frizzled receptors; ligand binding site; lipid binding groove; structure

Indexed keywords

CHOLESTEROL; FRIZZLED G PROTEIN COUPLED RECEPTOR; FRIZZLED PROTEIN; UNCLASSIFIED DRUG; WNT PROTEIN; WNT3A PROTEIN; G PROTEIN COUPLED RECEPTOR; SMOOTHENED PROTEIN;

EID: 85054450985     PISSN: 09680004     EISSN: 13624326     Source Type: Journal    
DOI: 10.1016/j.tibs.2018.09.002     Document Type: Review
Times cited : (38)

References (41)
  • 1
    • 84871846692 scopus 로고    scopus 로고
    • WNT signalling pathways as therapeutic targets in cancer
    • Anastas, J.N., Moon, R.T., WNT signalling pathways as therapeutic targets in cancer. Nat. Rev. Cancer 13 (2013), 11–26.
    • (2013) Nat. Rev. Cancer , vol.13 , pp. 11-26
    • Anastas, J.N.1    Moon, R.T.2
  • 2
    • 85020025659 scopus 로고    scopus 로고
    • Wnt/beta-catenin signaling, disease, and emerging therapeutic modalities
    • Nusse, R., Clevers, H., Wnt/beta-catenin signaling, disease, and emerging therapeutic modalities. Cell 169 (2017), 985–999.
    • (2017) Cell , vol.169 , pp. 985-999
    • Nusse, R.1    Clevers, H.2
  • 3
    • 84879414522 scopus 로고    scopus 로고
    • The mechanisms of Hedgehog signalling and its roles in development and disease
    • Briscoe, J., Therond, P.P., The mechanisms of Hedgehog signalling and its roles in development and disease. Nat. Rev. Mol. Cell Biol. 14 (2013), 416–429.
    • (2013) Nat. Rev. Mol. Cell Biol. , vol.14 , pp. 416-429
    • Briscoe, J.1    Therond, P.P.2
  • 4
    • 84954318478 scopus 로고    scopus 로고
    • Hedgehog signaling pathway: a novel model and molecular mechanisms of signal transduction
    • Gorojankina, T., Hedgehog signaling pathway: a novel model and molecular mechanisms of signal transduction. Cell. Mol. Life Sci. 73 (2016), 1317–1332.
    • (2016) Cell. Mol. Life Sci. , vol.73 , pp. 1317-1332
    • Gorojankina, T.1
  • 5
    • 85049249797 scopus 로고    scopus 로고
    • Structural basis for the recognition of Sonic Hedgehog by human Patched1
    • Gong, X., et al. Structural basis for the recognition of Sonic Hedgehog by human Patched1. Science, 361, 2018, 568.
    • (2018) Science , vol.361 , pp. 568
    • Gong, X.1
  • 6
    • 84925852119 scopus 로고    scopus 로고
    • Regulation of the oncoprotein Smoothened by small molecules
    • Sharpe, H.J., et al. Regulation of the oncoprotein Smoothened by small molecules. Nat. Chem. Biol. 11 (2015), 246–255.
    • (2015) Nat. Chem. Biol. , vol.11 , pp. 246-255
    • Sharpe, H.J.1
  • 8
    • 84961133336 scopus 로고    scopus 로고
    • Wnt signaling: role in regulation of haematopoiesis
    • Undi, R.B., et al. Wnt signaling: role in regulation of haematopoiesis. Indian J. Hematol. Blood Transfus. 32 (2016), 123–134.
    • (2016) Indian J. Hematol. Blood Transfus. , vol.32 , pp. 123-134
    • Undi, R.B.1
  • 9
    • 0035811492 scopus 로고    scopus 로고
    • Insights into Wnt binding and signalling from the structures of two Frizzled cysteine-rich domains
    • Dann, C.E., et al. Insights into Wnt binding and signalling from the structures of two Frizzled cysteine-rich domains. Nature 412 (2001), 86–90.
    • (2001) Nature , vol.412 , pp. 86-90
    • Dann, C.E.1
  • 10
    • 84863543371 scopus 로고    scopus 로고
    • Structural basis of Wnt recognition by Frizzled
    • Janda, C.Y., et al. Structural basis of Wnt recognition by Frizzled. Science 337 (2012), 59–64.
    • (2012) Science , vol.337 , pp. 59-64
    • Janda, C.Y.1
  • 11
    • 85016043869 scopus 로고    scopus 로고
    • Structure and functional properties of Norrin mimic Wnt for signalling with Frizzled4, Lrp5/6, and proteoglycan
    • Chang, T.H., et al. Structure and functional properties of Norrin mimic Wnt for signalling with Frizzled4, Lrp5/6, and proteoglycan. eLife, 4(July), 2015.
    • (2015) eLife , vol.4 , Issue.July
    • Chang, T.H.1
  • 12
    • 84940891731 scopus 로고    scopus 로고
    • Structural basis of the Norrin-Frizzled 4 interaction
    • Shen, G., et al. Structural basis of the Norrin-Frizzled 4 interaction. Cell Res. 25 (2015), 1078–1081.
    • (2015) Cell Res. , vol.25 , pp. 1078-1081
    • Shen, G.1
  • 13
    • 85020191672 scopus 로고    scopus 로고
    • Wnt5a promotes Frizzled-4 signalosome assembly by stabilizing cysteine-rich domain dimerization
    • DeBruine, Z.J., et al. Wnt5a promotes Frizzled-4 signalosome assembly by stabilizing cysteine-rich domain dimerization. Genes Dev. 31 (2017), 916–926.
    • (2017) Genes Dev. , vol.31 , pp. 916-926
    • DeBruine, Z.J.1
  • 14
    • 85017659327 scopus 로고    scopus 로고
    • Unsaturated fatty acyl recognition by Frizzled receptors mediates dimerization upon Wnt ligand binding
    • Nile, A.H., et al. Unsaturated fatty acyl recognition by Frizzled receptors mediates dimerization upon Wnt ligand binding. Proc. Natl. Acad. Sci. U. S. A. 114 (2017), 4147–4152.
    • (2017) Proc. Natl. Acad. Sci. U. S. A. , vol.114 , pp. 4147-4152
    • Nile, A.H.1
  • 15
    • 85046657566 scopus 로고    scopus 로고
    • Structural basis for recognition of frizzled proteins by Clostridium difficile toxin B
    • Chen, P., et al. Structural basis for recognition of frizzled proteins by Clostridium difficile toxin B. Science 360 (2018), 664–669.
    • (2018) Science , vol.360 , pp. 664-669
    • Chen, P.1
  • 16
    • 85045093070 scopus 로고    scopus 로고
    • A selective peptide inhibitor of Frizzled 7 receptors disrupts intestinal stem cells
    • Nile, A.H., et al. A selective peptide inhibitor of Frizzled 7 receptors disrupts intestinal stem cells. Nat. Chem. Biol. 14 (2018), 582–590.
    • (2018) Nat. Chem. Biol. , vol.14 , pp. 582-590
    • Nile, A.H.1
  • 17
    • 84878112106 scopus 로고    scopus 로고
    • Structure of the human smoothened receptor bound to an antitumour agent
    • Wang, C., et al. Structure of the human smoothened receptor bound to an antitumour agent. Nature 497 (2013), 338–343.
    • (2013) Nature , vol.497 , pp. 338-343
    • Wang, C.1
  • 18
    • 84982728617 scopus 로고    scopus 로고
    • Structural basis of Smoothened regulation by its extracellular domains
    • Byrne, E.F.X., et al. Structural basis of Smoothened regulation by its extracellular domains. Nature 535 (2016), 517–522.
    • (2016) Nature , vol.535 , pp. 517-522
    • Byrne, E.F.X.1
  • 19
    • 85019947839 scopus 로고    scopus 로고
    • Crystal structure of a multi-domain human smoothened receptor in complex with a super stabilizing ligand
    • Zhang, X., et al. Crystal structure of a multi-domain human smoothened receptor in complex with a super stabilizing ligand. Nat. Commun., 8, 2017, 15383.
    • (2017) Nat. Commun. , vol.8
    • Zhang, X.1
  • 20
    • 85047212092 scopus 로고    scopus 로고
    • Structural basis of Smoothened activation in Hedgehog signaling
    • 312–324.e16
    • Huang, P., et al. Structural basis of Smoothened activation in Hedgehog signaling. Cell, 174, 2018 312–324.e16.
    • (2018) Cell , vol.174
    • Huang, P.1
  • 21
    • 85052670328 scopus 로고    scopus 로고
    • Crystal structure of Frizzled 4 receptor in a ligand-free state
    • Yang, S., et al. Crystal structure of Frizzled 4 receptor in a ligand-free state. Nature 560 (2018), 666–670.
    • (2018) Nature , vol.560 , pp. 666-670
    • Yang, S.1
  • 22
    • 84867059613 scopus 로고    scopus 로고
    • Hedgehog signaling inhibition by the small molecule smoothened inhibitor GDC-0449 in the bone forming prostate cancer xenograft MDA PCa 118b
    • Karlou, M., et al. Hedgehog signaling inhibition by the small molecule smoothened inhibitor GDC-0449 in the bone forming prostate cancer xenograft MDA PCa 118b. Prostate 72 (2012), 1638–1647.
    • (2012) Prostate , vol.72 , pp. 1638-1647
    • Karlou, M.1
  • 23
    • 84983298724 scopus 로고    scopus 로고
    • Sonidegib for the treatment of advanced basal cell carcinoma: a comprehensive review of sonidegib and the BOLT trial with 12-month update
    • Chen, L., et al. Sonidegib for the treatment of advanced basal cell carcinoma: a comprehensive review of sonidegib and the BOLT trial with 12-month update. Future Oncol. 12 (2016), 2095–2105.
    • (2016) Future Oncol. , vol.12 , pp. 2095-2105
    • Chen, L.1
  • 24
    • 84924242647 scopus 로고    scopus 로고
    • Smoothened variants explain the majority of drug resistance in basal cell carcinoma
    • Atwood, S.X., et al. Smoothened variants explain the majority of drug resistance in basal cell carcinoma. Cancer Cell 27 (2015), 342–353.
    • (2015) Cancer Cell , vol.27 , pp. 342-353
    • Atwood, S.X.1
  • 25
    • 84924262003 scopus 로고    scopus 로고
    • Genomic analysis of smoothened inhibitor resistance in basal cell carcinoma
    • Sharpe, H.J., et al. Genomic analysis of smoothened inhibitor resistance in basal cell carcinoma. Cancer Cell 27 (2015), 327–341.
    • (2015) Cancer Cell , vol.27 , pp. 327-341
    • Sharpe, H.J.1
  • 26
    • 84904325982 scopus 로고    scopus 로고
    • Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs
    • Wang, C., et al. Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs. Nat. Commun., 5, 2014, 4355.
    • (2014) Nat. Commun. , vol.5 , pp. 4355
    • Wang, C.1
  • 27
    • 85001130088 scopus 로고    scopus 로고
    • Cholesterol activates the G-protein coupled receptor Smoothened to promote Hedgehog signaling
    • Luchetti, G., et al. Cholesterol activates the G-protein coupled receptor Smoothened to promote Hedgehog signaling. eLife, 5(October), 2016.
    • (2016) eLife , vol.5 , Issue.October
    • Luchetti, G.1
  • 28
    • 85018920897 scopus 로고    scopus 로고
    • Surrogate Wnt agonists that phenocopy canonical Wnt and beta-catenin signalling
    • Janda, C.Y., et al. Surrogate Wnt agonists that phenocopy canonical Wnt and beta-catenin signalling. Nature 545 (2017), 234–237.
    • (2017) Nature , vol.545 , pp. 234-237
    • Janda, C.Y.1
  • 29
    • 84863938543 scopus 로고    scopus 로고
    • Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors
    • Gurney, A., et al. Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors. Proc. Natl. Acad. Sci. U. S. A. 109 (2012), 11717–11722.
    • (2012) Proc. Natl. Acad. Sci. U. S. A. , vol.109 , pp. 11717-11722
    • Gurney, A.1
  • 30
    • 85027119058 scopus 로고    scopus 로고
    • Agonist-induced dimer dissociation as a macromolecular step in G protein-coupled receptor signaling
    • Petersen, J., et al. Agonist-induced dimer dissociation as a macromolecular step in G protein-coupled receptor signaling. Nat. Commun., 8, 2017, 226.
    • (2017) Nat. Commun. , vol.8
    • Petersen, J.1
  • 31
    • 0034727078 scopus 로고    scopus 로고
    • An LDL-receptor-related protein mediates Wnt signalling in mice
    • Pinson, K.I., et al. An LDL-receptor-related protein mediates Wnt signalling in mice. Nature 407 (2000), 535–538.
    • (2000) Nature , vol.407 , pp. 535-538
    • Pinson, K.I.1
  • 32
    • 85009106648 scopus 로고    scopus 로고
    • Conformational freedom of the LRP6 ectodomain is regulated by N-glycosylation and the binding of the Wnt antagonist Dkk1
    • Matoba, K., et al. Conformational freedom of the LRP6 ectodomain is regulated by N-glycosylation and the binding of the Wnt antagonist Dkk1. Cell Rep. 18 (2017), 32–40.
    • (2017) Cell Rep. , vol.18 , pp. 32-40
    • Matoba, K.1
  • 33
    • 77950592184 scopus 로고    scopus 로고
    • Reconstitution of a frizzled8.Wnt3a.LRP6 signaling complex reveals multiple Wnt and Dkk1 binding sites on LRP6
    • Bourhis, E., et al. Reconstitution of a frizzled8.Wnt3a.LRP6 signaling complex reveals multiple Wnt and Dkk1 binding sites on LRP6. J. Biol. Chem. 285 (2010), 9172–9179.
    • (2010) J. Biol. Chem. , vol.285 , pp. 9172-9179
    • Bourhis, E.1
  • 34
    • 12144289950 scopus 로고    scopus 로고
    • Vascular development in the retina and inner ear: control by Norrin and Frizzled-4, a high-affinity ligand-receptor pair
    • Xu, Q., et al. Vascular development in the retina and inner ear: control by Norrin and Frizzled-4, a high-affinity ligand-receptor pair. Cell 116 (2004), 883–895.
    • (2004) Cell , vol.116 , pp. 883-895
    • Xu, Q.1
  • 35
    • 85031700231 scopus 로고    scopus 로고
    • Assembly and architecture of the Wnt/beta-catenin signalosome at the membrane
    • DeBruine, Z.J., et al. Assembly and architecture of the Wnt/beta-catenin signalosome at the membrane. Br. J. Pharmacol. 174 (2017), 4564–4574.
    • (2017) Br. J. Pharmacol. , vol.174 , pp. 4564-4574
    • DeBruine, Z.J.1
  • 36
    • 85021276430 scopus 로고    scopus 로고
    • Targeting the Wnt pathway in cancer: a review of novel therapeutics
    • Tabatabai, R., et al. Targeting the Wnt pathway in cancer: a review of novel therapeutics. Target. Oncol. 12 (2017), 623–641.
    • (2017) Target. Oncol. , vol.12 , pp. 623-641
    • Tabatabai, R.1
  • 37
    • 85021626077 scopus 로고    scopus 로고
    • A structurally guided dissection-then-evolution strategy for ligand optimization of smoothened receptor
    • Ye, L., et al. A structurally guided dissection-then-evolution strategy for ligand optimization of smoothened receptor. MedChemComm 8 (2017), 1332–1336.
    • (2017) MedChemComm , vol.8 , pp. 1332-1336
    • Ye, L.1
  • 38
    • 84894037590 scopus 로고    scopus 로고
    • Lipidic cubic phase injector facilitates membrane protein serial femtosecond crystallography
    • Weierstall, U., et al. Lipidic cubic phase injector facilitates membrane protein serial femtosecond crystallography. Nat. Commun., 5, 2014, 3309.
    • (2014) Nat. Commun. , vol.5 , pp. 3309
    • Weierstall, U.1
  • 39
    • 84887326705 scopus 로고    scopus 로고
    • Structure and function of the Smoothened extracellular domain in vertebrate Hedgehog signaling
    • Nachtergaele, S., et al. Structure and function of the Smoothened extracellular domain in vertebrate Hedgehog signaling. eLife, 2, 2013, e01340.
    • (2013) eLife , vol.2
    • Nachtergaele, S.1
  • 40
    • 84983804225 scopus 로고    scopus 로고
    • Cellular cholesterol directly activates Smoothened in Hedgehog signaling
    • e1114
    • Huang, P., et al. Cellular cholesterol directly activates Smoothened in Hedgehog signaling. Cell 166 (2016), 1176–1187 e1114.
    • (2016) Cell , vol.166 , pp. 1176-1187
    • Huang, P.1
  • 41
    • 84890897900 scopus 로고    scopus 로고
    • Structural insights into the role of the Smoothened cysteine-rich domain in Hedgehog signalling
    • Rana, R., et al. Structural insights into the role of the Smoothened cysteine-rich domain in Hedgehog signalling. Nat. Commun., 4, 2013, 2965.
    • (2013) Nat. Commun. , vol.4 , pp. 2965
    • Rana, R.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.