Allosteric modulation of the calcium-sensing receptor

Current Neuropharmacology

Volumn 5, Issue 3, 2007, Pages 180-186

  Jensen, Anders A ^a   Bräuner Osborne, Hans ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

Allosteric modulator; Calcilytic; Calcimimetic; Calcium sensing receptor; CaR; Cinacalcet; Hyperparathyroidism

Indexed keywords

1 (3 METHOXYPHENYL) N (3 PHENYLPROPYL)ETHYLAMINE; 4 AMINOBUTYRIC ACID B RECEPTOR; ALPHA AMINO ACID; CALCIMIMETIC AGENT; CALCITONIN; CALCIUM ION; CALCIUM SENSING RECEPTOR; CALCIUM SENSING RECEPTOR BLOCKING AGENT; CALHEX 231; CALINDOL; CINACALCET; FENDILINE; G PROTEIN COUPLED RECEPTOR; GLUTAMATE RECEPTOR; JKJ 05; MAGNESIUM ION; N [2 HYDROXY 3 (2 CYANO 3 CHLOROPHENOXY)PROPYL] 1,1 DIMETHYL 2 (2 NAPHTYL)ETHYLAMINE; N [3 (2 CHLOROPHENYL)PROPYL] 1 (3 METHOXYPHENYL)ETHYLAMINE; PARATHYROID HORMONE; RECEPTOR BLOCKING AGENT;

ALLOSTERISM; AMINO TERMINAL SEQUENCE; BONE DENSITY; CHEMICAL STRUCTURE; CONCENTRATION RESPONSE; CRYSTAL STRUCTURE; DRUG APPROVAL; DRUG RESEARCH; DRUG STRUCTURE; DRUG TARGETING; EXTRACELLULAR CALCIUM; GENE MUTATION; HUMAN; HYPERCALCEMIA; HYPERPARATHYROIDISM; HYPOCALCEMIA; HYPOCALCIURIA; KIDNEY TUBULE; NONHUMAN; OSTEOPOROSIS; PARATHYROID CARCINOMA; PARATHYROID HORMONE RELEASE; PATHOGENESIS; PRIMARY HYPERPARATHYROIDISM; PROTEIN BINDING; PROTEIN DOMAIN; PROTEIN FAMILY; RECEPTOR BINDING; RECEPTOR UPREGULATION; REVIEW; SECONDARY HYPERPARATHYROIDISM; SIGNAL TRANSDUCTION; THYROID CELL; WILD TYPE;

EID: 45749141326     PISSN: 1570159X     EISSN: None     Source Type: Journal    
DOI: 10.2174/157015907781695982     Document Type: Review

References (84)

1. Arey, B.J., Seethala, R., Ma, Z., Fura, A., Morin, J., Swartz, J., Vyas, V., Yang, W., Dickson, J.K., Jr, Feyen, J H. (2005) A novel calcium-sensing receptor antagonist transiently stimulates parathyroid hormone secretion in vivo. Endocrinology, 146, 2015-2022.
2. Bai, M., Trivedi, S., Brown, E.M. (1998) Dimerization of the extracellular calcium-scnsing receptor (CaR) on (he cell surface of CaR-transfected HEK293. J. Biol. Chem., 273, 23605-23610.
3. B receptors. Physiol. Rev., 84, 835-867.
4. B receptor. J. Biol. Chem., 279, 29085-29091.
5. Block, G.A., Martin, K.J., de Francisco, A.L., Turner, S.A., Avram, M.M., Suranyi, M.G., Hercz, G., Cunningham, J., Abu-Alfa, A.K., Messa, P., Coyne, D.W., Locatelli, F., Cohen, R.M., Evenepoel, P., Moe, S.M., Fournier, A., Braun, J., McCary, L.C., Zani, V.J., Olson, K.A., Drueke, T.B., Goodman, W.G. (2004) Cinacalcet for secondary hyperparathyroidism in patients receiving hemodialysis. N. Engl. J. Med., 350, 1516-1525.
6. Bräuner-Osborne, H., Jensen, A.A., Sheppard, P.O., O'Hara, P., Krogsgaard-Larsen, P. (1999) The agonist-binding domain of the calcium-sensing receptor is located at the amino-terminal domain. J. Biol. Chem., 274, 18382-18386.
7. 2+ and other ions as extracellular (first) messengers. Physiol. Rev., 71, 371-411.
8. Brown, E.M. (2007) Clinical lessons from the calcium-sensing receptor. Nat. Clin. Pract. Endocrinol. Metab., 3, 122-133.
9. 2+-sensing receptor from bovine parathyroid. Nature, 366, 575-580.
10. Brown, E.M., MacLeod, R.J. (2001) Extracellular calcium sensing and extracellular calcium signaling. Physiol. Rev., 81, 239-297.
11. Chan, A.K., Duh, Q.Y., Katz, M.H., Siperstein, A.E., Clark, O.H. (1995) Clinical manifestations of primary hyperparathyroidism before and after parathyroidectomy. A case-control study. Ann. Surg., 222, 402-412.
12. Chattopadhyay, N., Brown, E.M. (2006) Role of calcium-sensing receptor in mineral ion metabolism and inherited disorders of calcium-sensing. Mol. Genet. Metab., 89, 189-202.
13. Christiansen, B., Hansen, K.B., Wellendorph, P., Bräuner-Osborne, H. (2007) Pharmacological characterization of mouse GPRC6A, as L-α-amino acid receptor with ability to sense divalent cations. Br. J. Pharmacol., 150, 798-807.
14. Conigrave, A.D., Brown, E.M. (2006) Taste receptors in the gastrointestinal tract. II. L-amino acid sensing by calcium-sensimg receptors: implications for GI physiology. Am. J. Physiol., 291, G753-761.
15. Conigrave, A.D., Hampson, D.R. (2006) Broad-spectrum L-amino acid sensing by class 3 G-protein-coupled receptors. Trends Endocrinol. Metab., 17, 398-407.
16. Conigrave, A.D., Mun, H.C., Delbridge, L., Quinn, S.J., Wilkinson, M., Brown, E.M. (2004) L-amino acids regulate parathyroid hormone secretion. J. Biol. Chem., 279, 38151-38159.
17. 2+-sensing receptor. Proc. Natl. Acad. Sci. USA, 97, 4814-4819.
18. Corbetta, S., Mantovani, G., Lania, A., Borgato, S., Vicentini, L., Beretta, E., Faglia, G., Di Blasio, A.M., Spada, A. (2000) Calcium-sensing receptor expression and signalling in human parathyroid adenomas and primary hyperplasia. Clin. Endocrinol., 52, 339-348.
19. B receptors: a new paradigm in G protein signaling. Mol. Cell Neurosci., 16, 296-312.
20. 2-(1-aryl)ethyl-3-phenylpropane-1,2-diamines as novel calcimimetics acting on the calcium sensing receptor. Bioorg. Med. Chem. Lett., 10, 2001-2004.
21. B1 subunit. Mol. Pharmacol., 70, 2027-2036.
22. Fox, J., Lowe, S.H., Conklin, R.L., Petty, B.A., Nemeth, E.F. (1999) Calcimimetic compound NPS R-568 stimulates calcitonin secretion but selectively targets parathyroid gland Ca(2+) receptor in rats. J. Pharmacol. Exp. Ther., 290, 480-486.
23. Fox, J., Lowe, S.H., Petty, B.A., Nemeth, E.F. (1999) NPS R-568: a type II calcimimetic compound that acts on parathyroid cell calcium receptor of rats to reduce plasma levels of parathyroid hormone and calcium. J. Pharmacol. Exp. Ther., 290, 473-479.
24. 2+ activation of the human calcium sensing receptor. A study with receptor-green fluorescent protein fusions. J. Biol. Chem., 273, 29712-29718.
25. Gasparini, F., Kuhn, R., Pin, J.P. (2002) Allosteric modulators of group I metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives. Curr. Opin. Pharmacol., 2, 43-49.
26. Gavai, A.V., Vaz, R.J., Mikkilineni, A.B., Roberge, J.Y., Liu, Y., Lawrence, R.M., Corte, J.R., Yang, W., Bednarz, M., Dickson, J.K., Jr., Ma, Z., Seethala, R., Feyen, J.H. (2005) Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists. Bioorg. Med. Chem. Lett., 15, 5478-5482.
27. Gogusev, J., Duchambon, P., Hory, B., Giovannini, M., Goureau, Y., Sarfati, E., Drueke, T.B. (1997) Depressed expression of calcium receptor in parathyroid gland tissue of patients with hyperparathyroidism. Kidney Int., 51, 328-336.
28. Goudet C., Gaven, F., Kniazeff, J., Vol, C., Liu, J., Cohen-Gonsaud, M., Acher, F., Prezeau, L., Pin, J.P. (2004) Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors. Proc. Natl. Acad. Set. USA, 101, 378-383.
29. Gowen, M., Stroup, G.B., Dodds, R.A., James, I.E., Votta, B.J., Smith, B.R., Bhatnagar, P.K., Lago, A.M., CAllahan, J.F., DelMar, E.G., Miller, MA., Nemeth, E.F., Fox, J. (2000) Antagonizing the parathyroid calcium receptor stimulates parathyroid hormone secretion and bone formation in osteopenic rats. J. Clin. Invest., 105, 1595-1604.
30. 2+ receptor expressed in Xenopus laevis oocytes by NPS 467 or NPS 568. Mol. Pharmacol., 53, 1083-1088.
31. 2+ receptors. Mol. Pharmacol., 55, 642-648.
32. 2+ receptor/ metabotropic glutamate chimeric receptors. Endocrinology, 141, 4156-4163.
33. Ho, C., Conner, D.A., Pollak, M.R., Ladd, D.J., Kifor, O., Warren, H.B., Brown, E.M., Seidman, J.G., Seidman, C.E. (1995) A mouse model of human familial hypocalciuric hypercalcemia and neonatal severe hyperparathyroidism. Nat. Genet., 11, 389-394.
34. Hofer, A.M., Brown, E.M. (2003) Extracellular calcium sensing and signalling. Nat. Cell Biol., 4, 530-538.
35. 2+ receptor converts a negative allosteric modulator into a positive allosteric modulator. J. Biol. Chem., 281, 21558-21565.
36. 2+ and a positive allosteric modulator. J. Biol. Chem., 277, 46622-46631.
37. Jensen, A.A. (2004) Molecular pharmacology of the metabotropic glutamate receptors. In: Schousboe, A., Bräuner-Osborne, H. Eds, Molecular Neuropharmacology. Strategies and Methods, Humana Press. pp. 47-82.
38. Jensen, A.A., Greenwood, J.R., Bräuner-Osborne, H. (2002) The dance of the clams: twists and turns in the family C GPCR homodimer. Trends Pharmacol. Sci., 23, 491-493.
39. Jensen, A.A., Spalding, T.A. (2004) Allosteric modulation of G-protein coupled receptors. Eur. J. Pharm. Sci., 21, 407-420.
40. Jingami, H., Nakanishi, S., Morikawa, K. (2003) Structure of the metabotropic glutamate receptor. Curr. Opin. Neurobiol., 13, 271-278.
41. 2-[1- (1-naphthyl)ethyl]-trans-1,2-diaminocyclohexanes: Development of 4-chlorophenylcarboxamide (calhex 231) as a new calcium sensing receptor ligand demonstrating potent calcilytic activity. J. Med. Chem., 49, 5119-5128.
42. Kessler, A., Faure, H., Petrel, C., Ruat, M., Dauban, P., Dodd, R.H. (2004) N2-benzyl-Nl-(1-(1-naphthyl)ethyl)-3-phenylpropane-1,2-diamines and conformatonally restrained indole analogues: development of calindol as a new calcimimetic acting at the calcium sensing receptor. Bioorg. Med. Chem. Lett., 14, 3345-3349.
43. Kifer, O., McElduff, A., LeBoff, M.S., Moore, F.D., Jr., Butters, R., Gao, P., Cantor, T.L., Kifor, I. Brown, E.M. (2004) Activating antibodies to the calcim sensing receptor in two patients with autoimmune hypoparathyroidism. J. Clin. Endocrinol. Metab., 89, 548-556.
44. Kifor, O., Moore, F.D., Jr., Delaney, M., Garber, J., Hendy, G.N., Butters, R., Gao, P., Cantor, T.L, Kifor, I., Brown, E.M., Wysolmerski, J. (2003) A syndrome of hypocalciuric hypercalcemia caused by autoantibodies directed at the calcium-sensing receptor. J. Clin. Endocrinol. Metab., 88, 60-72.
45. Kuang, D., Yao, Y., Larn, J., Tsushima, R.G. Hampson, D.R. (2005) Cloning and characterization of a family C-orphan G-protein coupled receptor. J. Neurochem., 93, 383-391.
46. 2+-sensing function of the metabotropic glutamate receptors. Science, 279, 1722-1725.
47. Kunishima, N., Shimada, Y., Tsuji, Y., Sato, T., Yamamoto, M., Kumasaka, T., Nakanishi, S., Jinggami, H., Morikawa, K. (2000) Structural basis of glutamate recognition by a dimeric metabotropic glutamate receptor. Nature, 407, 971-976.
48. Miedlich, S.U., Gama, L., Seuwen, K., Wolf, R.M., Breitwieser, G.E. (2004) Homology modelling of the transmembrane domain of the human calcium sensing receptor and localization of an allosteric binding site. J. Biol. Chem., 279, 7254-7263.
49. 2+-sensing receptor's venus flytrap domain that selectively disables L-amino acid sensing. J. Biol. Chem., 280, 29067-29072.
50. 2+-sensing receptor is required for L-amino acid sensing. J. Biol. Chem., 279, 51739-51744.
51. Nelson, G., Chandrashekar, J., Hoon, M.A., Feng, L., Zhao, G., Ryba, N.J., Zuker, C.S. (2002) An amino-acid taste receptor. Nature, 416, 199-202.
52. Nelson, G., Hoon, M.A., Chandrasheckar, J., Zhang, Y., Ryba, N.J., Zuker, C.S. (2001) Mammalian sweet taste receptors. Cell, 106, 381-390.
53. 2+ receptor antagonists that stimulate secretion of parathyroid hormone. J. Pharmarcol. Exp. Ther., 299, 323-331.
54. 2+ receptor antagonists that stimulate secretion of parathyroid hormone. J. Pharmacol Exp. Ther., 299, 323-331.
55. Nemeth, E.F., Heaton, W.H., Miller, M., Fox, J., Balandrin, M.F., Van Wagenen, B.C., Colloton, M., Karbon, W., Scherrer, J., Shatzen, E., Rishton, G., Scully, S., Qi, M., Harris, R., Lacey, D., Martin, D. (2004) Pharmacodynamics of the type II calcimimetic-compound cinacalcet HCI. J. Pharmacol. Exp. Ther., 308, 627-635.
56. Nemeth, E.F., Steffey, M.E., Hammerland, L.G., Hung, B.C.P., van Wagenen, B.C., DelMar, E.G., Balandrin, M.F. (1998) Calcimimetics with potent and selective activity on the parathyroid calcium receptor. Proc. Natl. Acad. Sci. USA, 95, 4040-4045.
57. 236. J. Biol. Chem., 274, 11629-11634.
58. Peacock, M., Bilezikian, J.P., Klassen, P.S., Guo, M.D., Turner, S.A., Shoback, D. (2005) Cinacalcet hydrochloride maintains long-term normocalcemia in patients with primary hyperparathyroidism. J. Clin. Endocrinol. Metab., 90, 135-141.
59. 2+-sensing receptor interact within overlapping but not identical binding sites in the transmembrane domain. J. Biol. Chem., 279, 18990-18997.
60. 2- sensing receptor. J. Biol. Chem., 278, 49487-49494.
61. Pi, M., Faber, P., Ekema, G., Jackson, P.D., Ting, A., Wang, N., Fontilla-Poole, M., Mays, R.W., Brunden, K.R., Harrington, J.J., Quarles, L.D. (2005) Identification of a novel extracelluar cation-sensing G-protein-coupled receptor. J. Biol. Chem., 280, 40201-40209.
62. Pin, J.-P., Galvez, T., Prézeau, L. (2003) Evolution, structure and activation mechanism of family 3/C G-protein coupled receptors. Pharmacol. Ther., 98, 325-354.
63. B receptor heteromer. Neuropharmacology, 38, A36-30.
64. Quinn, S.J., Bai, M., Brown, E.M. (2004) pH Sensing by the calcium-sensing receptor. J. Biol. Chem., 279, 37241-37249.
65. Quinn, S.J., Kifor, O., Trivedi, S., Diaz, R., Vassilev, P., Brown, E. (1998) Sodium and ionic strength sensing by the calcium receptor. J. Biol Chem., 31, 19579-19586.
66. 2+-sensing receptor: a target for polyamines. Am. J. Physiol., 273, C1315-C1323.
67. 2+ receptor critical for dimerization. J. Biol. Chem., 274, 27642-27650.
68. 2+ receptor. J. Biol. Chem., 277, 18908-18913.
69. 2+. J. Biol. Chem., 280, 37013-37020.
70. 2+ oscillations by the calcium-sensing receptor. J. Biol. Chem., 281, 38730-38737.
71. 2+-sensing receptor are mediated by a phospholipase C/inositol 1,4,5-trisphosphate-independent pathway that requires G12, Rho, filamin-A, and the actin cytoskeleton. J. Biol. Chem., 280, 22875-22882.
72. 5 dimerization. Mol. Pharmacol., 59, 46-53.
73. Romano, C., Yang, W.-L., O'Malley, K.L. (1996) Metabotropic glutamate receptor 5 is a disulfide-linked dimer. J. Biol. Chem., 271, 28612-28616.
74. 2+ binding pocket within the venus flytrap module of the human calcium-sensing receptor. J. Biol. Chem., 280, 37917-37923.
75. Slatopolsky, E., Brown, A., Dusso, A. (1999) Pathogenesis of secondary hyperparathyroidism. Kidney Int. Suppl., 73, S14-19.
76. Tfelt-Hansen, J., Brown, E.M. (2005) The calcium-sensing receptor in normal pbysiology and pathophysiology: areview. Crit. Rev. Clin. Lab. Sci., 42, 35-70.
77. 3+. Proc. Natl. Acad Sci. USA, 99, 2660-2665.
78. Wellendorph, P., Hansen, K.B., Balsgaard, A., Greenwood, J.R., Egebjerg, J., Bräuner-Osborne, H. (2005) Deorphanization of GPRC6A: a promiscuous L-α-amino acid receptor with preference for basic amino acids. Mol. Pharmacol., 67, 589-597.
79. Weston, A.H., Absi, M., Wand, D.T., Ohanian, J., Dodd, R.H., Dauban, P., Petrel, C., Ruat, M., Edwards, G. (2005) Evidence in favor of a calcium-sensing receptor in arterial endothelial cells: studies with calindol and Calhex 231. Circ. Res., 97, 391-398.
80. B receptor. Neuropharmacology, 38, 1647-1656.
81. Yang, W., Wang, Y., Roberge, J.Y., Ma, Z., Liu, Y., Michael Lawrence, R., Rotella, D.P., Seethala, R., Feyen, J.H., Dickson, J.K., Jr. (2005) Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists. Bioorg. Med Chem. Lett., 15, 1225-1228.
82. +-sensing receptor. Am. J. Physiol., 282, C1414-1422.
83. Zhang, Z., Qiu, W., Quinn, S.J., Conigrave, A.D., Brown, E.M Bai, M. (2002) Three adjacent serines in the extracellular domains of the CaR are required for L-amino acid-mediated potentiation of receptor function. J. Biol. Chem., 277, 33727-33735.
84. Zhao, G.Q., Zhang, Y., Hoon, M.A., Chandrashekar, J., Erlenbach, I., Ryba, N.J., Zuker, C.S. (2003) The receptors for mammalian sweet and umami taste. Cell, 115, 255-266.