The Hedgehog (Hh) signaling pathway is vital to animal development as it …

• Abstract
• Background
• Results
• Discussion
• References
• Figures

Biology Articles » Zoology » Zoosemiotics » Small-molecule modulators of Hedgehog signaling: identification and characterization of Smoothened agonists and antagonists » References

References

- Small-molecule modulators of Hedgehog signaling: identification and characterization of Smoothened agonists and antagonists

1. Nusslein-Volhard C, Wieschaus E: Mutations affecting segment number and polarity in Drosophila.

   Nature 1980, 287:795-801.

2. Ingham PW, McMahon AP: Hedgehog signaling in animal development: paradigms and principles.

   Genes Dev 2001, 15:3059-3087.

3. Xie J, Murone M, Luoh SM, Ryan A, Gu Q, Zhang C, Bonifas JM, Lam CW, Hynes M, Goddard A, et al.: Activating Smoothened mutations in sporadic basal-cell carcinoma.

   Nature 1998, 391:90-92.

4. Stone DM, Hynes M, Armanini M, Swanson TA, Gu Q, Johnson RL, Scott MP, Pennica D, Goddard A, Phillips H, et al.: The tumour-suppressor gene patched encodes a candidate receptor for Sonic hedgehog.

   Nature 1996, 384:129-134.

5. Denef N, Neubuser D, Perez L, Cohen SM: Hedgehog induces opposite changes in turnover and subcellular localization of patched and smoothened.

   Cell 2000, 102:521-531.

6. Cuenda A, Alessi DR: Use of kinase inhibitors to dissect signaling pathways.

   Methods Mol Biol 2000, 99:161-175.

7. Sebolt-Leopold JS: Development of anticancer drugs targeting the MAP kinase pathway.

   Oncogene 2000, 19:6594-6599.

8. Lee JC, Kassis S, Kumar S, Badger A, Adams JL: p38 mitogen-activated protein kinase inhibitors - mechanisms and therapeutic potentials.

   Pharmacol Ther 1999, 82:389-397.

9. Cooper MK, Porter JA, Young KE, Beachy PA: Teratogen-mediated inhibition of target tissue response to Shh signaling.

   Science 1998, 280:1603-1607.

10. Incardona JP, Gaffield W, Kapur RP, Roelink H: The teratogenic Veratrum alkaloid cyclopamine inhibits sonic hedgehog signal transduction.

    Development 1998, 125:3553-3562.

11. Taipale J, Chen JK, Cooper MK, Wang B, Mann RK, Milenkovic L, Scott MP, Beachy PA: Effects of oncogenic mutations in Smoothened and Patched can be reversed by cyclopamine.

    Nature 2000, 406:1005-1009.

12. Tekki-Kessaris N, Woodruff R, Hall AC, Gaffield W, Kimura S, Stiles CD, Rowitch DH, Richardson WD: Hedgehog-dependent oligodendrocyte lineage specification in the telencephalon.

    Development 2001, 128:2545-2554.

13. van den Brink GR, Hardwick JC, Tytgat GN, Brink MA, Ten Kate FJ, Van Deventer SJ, Peppelenbosch MP: Sonic hedgehog regulates gastric gland morphogenesis in man and mouse.

    Gastroenterology 2001, 121:317-328.

14. Kim SK, Melton DA: Pancreas development is promoted by cyclopamine, a hedgehog signaling inhibitor.

    Proc Natl Acad Sci USA 1998, 95:13036-13041.

15. Chiang C, Swan RZ, Grachtchouk M, Bolinger M, Litingtung Y, Robertson EK, Cooper MK, Gaffield W, Westphal H, Beachy PA, Dlugosz AA: Essential role for Sonic hedgehog during hair follicle morphogenesis.

    Dev Biol 1999, 205:1-9.

16. Sukegawa A, Narita T, Kameda T, Saitoh K, Nohno T, Iba H, Yasugi S, Fukuda K: The concentric structure of the developing gut is regulated by Sonic hedgehog derived from endodermal epithelium.

    Development 2000, 127:1971-1980.

17. Williams JA, Guicherit OM, Zaharian BI, Xu Y, Chai L, Gatchalian C, Porter JA, Rubin LL, Wang FY: Identification of novel inhibitors of the hedgehog signaling pathway: Effects on basal cell carcinoma-like lesions.

    Proc Natl Acad Sci USA, in press.

18. Tian SS, Lamb P, King AG, Miller SG, Kessler L, Luengo JI, Averill L, Johnson RK, Gleason JG, Pelus LM, et al.: A small, nonpeptidyl mimic of granulocyte colony-stimulating factor.

    Science 1998, 281:257-259.

19. Zhang B, Salituro G, Szalkowski D, Li Z, Zhang Y, Royo I, Vilella D, Diez MT, Pelaez F, Ruby C, et al.: Discovery of a small molecule insulin mimetic with antidiabetic activity in mice.

    Science 1999, 284:974-977.

20. Sasaki H, Hui C, Nakafuku M, Kondoh H: A binding site for Gli proteins is essential for HNF-3beta floor plate enhancer activity in transgenics and can respond to Shh in vitro.

    Development 1997, 124:1313-1322.

21. Taylor FR, Wen D, Garber EA, Carmillo AN, Baker DP, Arduini RM, Williams KP, Weinreb PH, Rayhorn P, Hronowski X, et al.: Enhanced potency of human Sonic hedgehog by hydrophobic modification.

    Biochemistry 2001, 40:4359-4371.

22. Ericson J, Rashbass P, Schedl A, Brenner-Morton S, Kawakami A, van Heyningen V, Jessell TM, Briscoe J: Pax6 controls progenitor cell identity and neuronal fate in response to graded Shh signaling.

    Cell 1997, 90:169-180.

23. Ericson J, Morton S, Kawakami A, Roelink H, Jessell TM: Two critical periods of Sonic Hedgehog signaling required for the specification of motor neuron identity.

    Cell 1996, 87:661-673.

24. Tanabe Y, William C, Jessell TM: Specification of motor neuron identity by the MNR2 homeodomain protein.

    Cell 1998, 95:67-80.

25. Goodrich LV, Milenkovic L, Higgins KM, Scott MP: Altered neural cell fates and medulloblastoma in mouse patched mutants.

    Science 1997, 277:1109-1113.

26. Zhang XM, Ramalho-Santos M, McMahon AP: Smoothened mutants reveal redundant roles for Shh and Ihh signaling including regulation of L/R asymmetry by the mouse node.

    Cell 2001, 105:781-792.

27. Chiang C, Litingtung Y, Lee E, Young KE, Corden JL, Westphal H, Beachy PA: Cyclopia and defective axial patterning in mice lacking Sonic hedgehog gene function.

    Nature 1996, 383:407-413.

28. Enna SJ, Williams M, Ferkany JW, Kenakin T, Porsolt RD, Sullivan JP, (eds.):

    Current Protocols in Pharmacology New York: John Wiley and Sons 2000.

29. Samama P, Cotecchia S, Costa T, Lefkowitz RJ: A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.

    J Biol Chem 1993, 268:4625-4636.

30. Taipale J, Beachy PA: The Hedgehog and Wnt signalling pathways in cancer.

    Nature 2001, 411:349-354.

31. De Lean A, Stadel JM, Lefkowitz RJ: A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.

    J Biol Chem 1980, 255:7108-7117.

32. Howard AD, McAllister G, Feighner SD, Liu Q, Nargund RP, Van der Ploeg LH, Patchett AA: Orphan G-protein-coupled receptors and natural ligand discovery.

    Trends Pharmacol Sci 2001, 22:132-140.

33. Civelli O, Nothacker HP, Saito Y, Wang Z, Lin SH, Reinscheid RK: Novel neurotransmitters as natural ligands of orphan G-protein-coupled receptors.

    Trends Neurosci 2001, 24:230-237.

34. Dohlman HG, Thorner J, Caron MG, Lefkowitz R: Model systems for the study of seven-transmembrane-segment receptors.

    Annu Rev Biochem 1991, 60:653-688.

35. Christopoulos A: Allosteric binding sites on cell-surface receptors: novel targets for drug discovery.

    Nat Rev Drug Discov 2002, 1:198-210.

36. Taipale J, Cooper MK, Maiti T, Beachy PA: Patched acts catalytically to suppress the activity of Smoothened.

    Nature 2002, 418:892-897.

37. Bourne HR: How receptors talk to trimeric G proteins.

    Curr Opin Cell Biol 1997, 9:134-142.

38. DeCamp D, Thompson TM, de Sauvage FJ, Lerner MR: Smoothened activates Galphai-mediated signaling in frog melanophores.

    J Biol Chem 2000, 275:26322-26327.

39. Trousse F, Marti E, Gruss P, Torres M, Bovolenta P: Control of retinal ganglion cell axon growth: a new role for Sonic hedgehog.

    Development 2001, 128:3927-3936.

40. Carstea ED, Morris JA, Coleman KG, Loftus SK, Zhang D, Cummings C, Gu J, Rosenfeld MA, Pavan WJ, Krizman DB, et al.: Niemann-Pick C1 disease gene: homology to mediators of cholesterol homeostasis.

    Science 1997, 277:228-231.

41. Hampton RY: Cholesterol homeostasis: ESCAPe from the ER.

    Curr Biol 2000, 10:R298-R301.

42. Davies JP, Chen FW, Ioannou YA: Transmembrane molecular pump activity of Niemann-Pick C1 protein.

    Science 2000, 290:2295-2298.

43. Traiffort E, Charytoniuk DA, Faure H, Ruat M: Regional distribution of Sonic Hedgehog, patched, and smoothened mRNA in the adult rat brain.

    J Neurochem 1998, 70:1327-1330.

44. Parmantier E, Lynn B, Lawson D, Turmaine M, Namini SS, Chakrabarti L, McMahon AP, Jessen KR, Mirsky R: Schwann cell-derived Desert hedgehog controls the development of peripheral nerve sheaths.

    Neuron 1999, 23:713-724.

45. St-Jacques B, Dassule HR, Karavanova I, Botchkarev VA, Li J, Danielian PS, McMahon JA, Lewis PM, Paus R, McMahon AP: Sonic hedgehog signaling is essential for hair development.

    Curr Biol 1998, 8:1058-1068.

46. Sato N, Leopold PL, Crystal RG: Induction of the hair growth phase in postnatal mice by localized transient expression of Sonic hedgehog.

    J Clin Invest 1999, 104:855-864.

47. Pola R, Ling LE, Silver M, Corbley MJ, Kearney M, Pepinsky RB, Shapiro R, Taylor FR, Baker DP, Asahara T, Isner JM: The morphogen Sonic hedgehog is an indirect angiogenic agent upregulating two families of angiogenic growth factors.

    Nat Med 2001, 7:706-711.

48. Vortkamp A, Pathi S, Peretti GM, Caruso EM, Zaleske DJ, Tabin CJ: Recapitulation of signals regulating embryonic bone formation during postnatal growth and in fracture repair.

    Mech Dev 1998, 71:65-76.

49. Pepinsky RB, Shapiro RI, Wang S, Chakraborty A, Gill A, Lepage DJ, Wen D, Rayhorn P, Horan GS, Taylor FR, et al.: Long-acting forms of Sonic hedgehog with improved pharmacokinetic and pharmacodynamic properties are efficacious in a nerve injury model.

    J Pharm Sci 2002, 91:371-387.

50. Tsuboi K, Shults CW: Intrastriatal injection of sonic hedgehog reduces behavioral impairment in a rat model of Parkinson's.

    Exp Neurol 2002, 173:95-104.

51. Chen JK, Taipale J, Cooper M, Beachy PA: Inhibition of Hedgehog signaling by direct binding of cyclopamine to Smoothened.

    Genes Dev 2002, 16:2743-2748.

52. Chen JK, Taipale J, Young JE, Maiti T, Beachy PA: Small molecule modulation of Smoothened activity.

    Proc Natl Acad Sci USA 2002, 99:14071-14076.