Regulation of Stability and Trafficking of Calcium-Sensing Receptors by Pharmacologic Chaperones

Advances in Pharmacology

Volumn 62, Issue , 2011, Pages 143-173

  Huang, Ying ^a   Cavanaugh, Alice ^b   Breitwieser, Gerda E ^b  

^a ROYAL VICTORIA HOSPITAL   (Canada)

^b WEIS CENTER FOR RESEARCH   (United States)

Author keywords

Calcium sensing receptor; Cotranslational regulation; Endoplasmic reticulum quality control; G protein coupled receptors; Membrane protein biosynthesis; Pharmacologic chaperones

Indexed keywords

CALCIMIMETIC AGENT; CALCIUM SENSING RECEPTOR; CHAPERONE; CHOLECYSTOKININ; CINACALCET; DOPAMINE 4 RECEPTOR; G PROTEIN COUPLED RECEPTOR; GASTRIN; GENTAMICIN; GLUTATHIONE; NEOMYCIN; OPIATE; PARATHYROID HORMONE; POLYAMINE; POLYARGININE; POLYLYSINE; PROTAMINE; SPERMIDINE; SPERMINE; TECALCET; VASOPRESSIN; VASOPRESSIN V1A RECEPTOR; VASOPRESSIN V2 RECEPTOR;

BINDING SITE; BIOSYNTHESIS; BOOK; BREAST CANCER; CALCIUM HOMEOSTASIS; CALCIUM TRANSPORT; CELL DIFFERENTIATION; CELL MEMBRANE; CHRONIC KIDNEY FAILURE; CYTOPLASM; DNA POLYMORPHISM; ENDOPLASMIC RETICULUM; GAIN OF FUNCTION MUTATION; GENE EXPRESSION; HYPOCALCIURIA; HYPOGONADOTROPIC HYPOGONADISM; LIGHT; LOSS OF FUNCTION MUTATION; NONHUMAN; PRIORITY JOURNAL; PROSTATE CANCER; PROTEIN FUNCTION; PROTEIN MODIFICATION; PROTEIN STABILITY; PROTEIN STRUCTURE; RECEPTOR UPREGULATION; SATIETY; SIGNAL TRANSDUCTION; STOMACH ACID;

EID: 80052683888     PISSN: 10543589     EISSN: 15578925     Source Type: Book Series    
DOI: 10.1016/B978-0-12-385952-5.00007-5     Document Type: Chapter

References (184)

1. Angers S., Salahpour A., Bouvier M. Dimerization: An emerging concept for G protein-coupled receptor ontogeny and function. Annual Review of Pharmacology and Toxicology 2002, 42:409-435.
2. Arthur J.M., Lawrence M.S., Payne C.R., Rane M.J., McLeish K.R. The calcium-sensing receptor stimulates JNK in MDCK cells. Biochemical and Biophysical Research Communications 2000, 275:538-541.
3. Babbar N., Gerner E.W. Targeting polyamines and inflammation for cancer prevention. Recent Results in Cancer Research 2011, 188:49-54.
4. Bai M., Trivedi S., Kifor O., Quinn S.J., Brown E.M. Intermolecular interactions between dimeric calcium-sensing receptor monomers are important for its normal function. Proceedings of the National Academy of Sciences of the United States of America 1999, 96:2834-2839.
5. Bandyopadhyay S., Tfelt-Hansen J., Chattopadhyay N. Diverse roles of extracellular calcium-sensing receptor in the central nervous system. Journal of Neuroscience Research 2010, 88:2073-2082.
6. Bernier V., Bichet D.G., Bouvier M. Pharmacological chaperone action on G-protein-coupled receptors. Current Opinion in Pharmacology 2004, 4:528-533.
7. Bernier V., Lagace M., Bichet D.G., Bouvier M. Pharmacological chaperones: Potential treatment for conformational diseases. Trends in Endocrinology and Metabolism 2004, 15:222-228.
8. Brauner-Osborne H., Wellendorph P., Jensen A.A. Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors. Current Drug Targets 2007, 8:169-184.
9. Breitwieser G.E. Extracellular calcium as an integrator of tissue function. The International Journal of Biochemistry and Cell Biology 2008, 40:1467-1480.
10. Breitwieser G.E., Gama L. Calcium-sensing receptor activation induces intracellular calcium oscillations. American Journal of Physiology. Cell Physiology 2001, 280:C1412-C1421.
11. Breitwieser G.E., Miedlich S.U., Zhang M. Calcium sensing receptors as integrators of multiple metabolic signals. Cell Calcium 2004, 35:209-216.
12. Brennan S.C., Conigrave A.D. Regulation of cellular signal transduction pathways by the extracellular calcium-sensing receptor. Current Pharmaceutical Biotechnology 2009, 10:270-281.
13. Broadhead G.K., Mun H.-C., Avlani V.A., Jourdon O., Church W.B., Christopoulos A., Delbridge L., Conigrave A.D. Allosteric modulation of the calcium-sensing receptor by γ-glutamyl peptides: Inhibition of PTH secretion, suppression of intracellular cAMP levels and a common mechanism of action with L-amino acids. The Journal of Biological Chemistry, 2010, 286:8786-8797.
14. Brown E.M. Four parameter model of the sigmoidal relations between parathyroid hormone release and extracellular calcium concentration in normal and abnormal parathyroid tissue. The Journal of Clinical Endocrinology and Metabolism 1983, 56:572-581.
15. Brown E.M. Extracellular Ca2+-sensing, regulation of parathyroid cell function and role of Ca2+ and other ions as extracellular (first) messengers. Physiological Reviews 1991, 71:371-411.
16. Brown E.M. Anti-parathyroid and anti-calcium sensing receptor antibodies in autoimmune hypoparathyroidism. Endocrinology and Metabolism Clinics of North America 2009, 38:437-445.
17. Bruce J.I.E., Yang X., Ferguson C.J., Elliott A.C., Steward M.C., Case R.M., Riccardi D. Molecular and functional identification of a Ca2+ (polyvalent cation)-sensing receptor in rat pancreas. The Journal of Biological Chemistry 1999, 274:20561-20568.
18. Bulenger S., Marullo S., Bouvier M. Emerging role of homo- and heterodimerization in G-protein-coupled receptor biosynthesis and maturation. Trends in Pharmacological Sciences 2005, 26:131-137.
19. Calebiro D., Nikolaev V.O., Lohse M.J. Imaging of persistent cAMP signaling by internalized G protein-coupled receptors. Journal of Molecular Endocrinology 2010, 45:1-8.
20. Canaff L., Hendy G.N. Human calcium-sensing receptor gene. Vitamin D response elements in promoters P1 and P2 confer transcriptional responsiveness to 1,25-dihydroxyvitamin D. The Journal of Biological Chemistry 2002, 277:30337-30350.
21. Canaff L., Hendy G.N. Calcium-sensing receptor gene transcription is up-regulated by the proinflammatory cytokine, Interleukin-1β. Role of the NF-κB pathway and κB elements. The Journal of Biological Chemistry 2005, 280:14177-14188.
22. Canaff L., Zhou X., Hendy G.N. The proinflammatory cytokine, Interleukin-6, up-regulates calcium-sensing receptor gene transcription via Stat1/3 and Sp1/3. The Journal of Biological Chemistry 2008, 283:13586-13600.
23. Canaff L., Zhou X., Mosesova I., Cole D.E., Hendy G.N. Glial Cells Missing-2 (GCM2) transactivates the calcium-sensing receptor gene: Effect of a dominant-negative GMC2 mutant associated with autosomal dominant hypoparathyroidism. Human Mutation 2009, 30:85-92.
24. Caroppo R., Gerbino A., Debellis L., Kifor O., Soybel D.I., Brown E.M., Hofer A.M., Curci S. Asymmetrical, agonist-induced fluctuations in local extracellular [Ca2+] in intact polarized epithelia. The EMBO Journal 2001, 20:6316-6325.
25. Carvalho P., Goder V., Rapoport T.A. Distinct ubiquitin-ligase complexes define convergent pathways for the degradation of ER proteins. Cell 2006, 126:361-373.
26. Casero R.A., Marton L.J. Targeting polyamine metabolism and function in cancer and other hyperproliferative diseases. Nature Reviews. Drug Discovery 2007, 6:373-390.
27. Cavanaugh A., McKenna J., Stepanchick A., Breitwieser G.E. Calcium-sensing receptor biosynthesis includes a cotranslational conformational checkpoint and endoplasmic reticulum retention. The Journal of Biological Chemistry 2010, 285:19854-19864.
28. Chakravarthi S., Jessop C.E., Bulleid N.J. The role of glutathione in disulfide bond formation and endoplasmic-reticulum-generated oxidative stress. EMBO Reports 2006, 7:271-275.
29. Chattopadhyay N., Baum M., Bai M., Hebert S.C., Harris H.W., Brown E.M. Ontogeny of the extracellular calcium-sensing receptor in rat kidney. The American Journal of Physiology 1996, 271:F736-F743.
30. Chattopadhyay N., Légrádi G., Bai M., Kifor O., Ye C., Vassilev P.M., Brown E.M., Lechan R.M. Calcium-sensing receptor in the rat hippocampus: A developmental study. Developmental Brain Research 1997, 100:13-21.
31. Chaudhuri T.K., Paul S. Protein-misfolding diseases and chaperone-based therapeutic approaches. The FEBS Journal 2006, 273:1331-1349.
32. Chen R.A., Goodman W.G. Role of the calcium-sensing receptor in parathyroid gland physiology. American Journal of Physiology. Renal Physiology 2004, 286:F1005-F1011.
33. Cole D.E., Yun F.H., Wong B.Y., Shuen A.Y., Booth R.A., Scillitani A., Pidasheva S., Zhou X., Canaff L., Hendy G.N. Calcium-sensing receptor mutations and denaturing high performance liquid chromatography. Journal of Molecular Endocrinology 2009, 42:331-339.
34. Conigrave A.D., Brown E.M. Taste receptors in the gastrointestinal tract II. L-Amino acid sensing by calcium-sensing receptors: Implications for GI physiology. American Journal of Physiology. Gastrointestinal and Liver Physiology 2006, 291:G753-G761.
35. Conn P.M., Knollman P.E., Brothers S.P., Janovick J.A. Protein folding as posttranslational regulation: Evolution of a mechanism for controlled plasma membrane expression of a G protein-coupled receptor. Molecular Endocrinology 2006, 20:3035-3041.
36. Conn M.P., Ulloa-Aguirre A., Ito J., Janovick J.A. G protein-coupled receptor trafficking in health and disease: Lessons learned to prepare for therapeutic mutant rescue in vivo. Pharmacological Reviews 2007, 59:225-250.
37. Cormier J.H., Tamura T., Sunryd J.C., Hebert D.N. EDEM1 recognition and delivery of misfolded proteins to the SEL1L-containing ERAD complex. Molecular Cell 2009, 34:627-633.
38. Crump C.M., Xiang Y., Thomas L., Gu F., Austin C., Tooze S.A., Thomas G. PACS-1 binding to adaptors is required for acidic cluster motif-mediated protein traffic. The EMBO Journal 2001, 20:2191-2201.
39. Csala M., Banhegyi G., Benedetti A. Endoplasmic reticulum: A metabolic compartment. FEBS Letters 2006, 580:2160-2165.
40. D'Angelo J.A., Dehlink E., Platzer B., Dwyer P., Circu M.L., Garay J., Aw T.Y., Feibiger E., Dickinson B.L. The cystine/glutamate antiporter regulates dendritic cell differentiation and antigen presentation. The Journal of Immunology 2010, 185:3217-3225.
41. Davies S.L., Ozawa A., McCormick W.D., Cvorak M.M., Ward D.T. Protein kinase C-mediated phosphorylation of the calcium-sensing receptor is stimulated by receptor activation and attenuated by calyculin-sensitive phosphatase activity. The Journal of Biological Chemistry 2007, 282:15048-15056.
42. Diaz Vivancos P., Wolff T., Markovic J., Pallardo F.V., Foyer C.H. A nuclear glutathione cycle within the cell cycle. The Biochemical Journal 2010, 431:169-178.
43. Didiuk M.T., Griffith D.A., Benbow J.W., Liu K.K., Walker D.P., Bi F.C., Morris J., et al. Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists. Bioorganic & Medicinal Chemistry Letters 2009, 19:4555-4559.
44. Dolmetsch R.E., Xu K., Lewis R.S. Calcium oscillations increase the efficiency and specificity of gene expression. Nature 1998, 392:933-936.
45. Dupre D.J., Baragli A., Rebois R.V., Ethier N., Hebert T.E. Signalling complexes associated with adenylyl cyclase II are assembled during their biosynthesis. Cellular Signalling 2006, 19:481-489.
46. Dupre D.J., Robitaille M., Ethier N., Villeneuve L.R., Mamarbachi A.M., Hebert T.E. Seven transmembrane receptor core signaling complexes are assembled prior to plasma membrane trafficking. The Journal of Biological Chemistry 2006, 281:34561-34573.
47. Dupre D.J., Robitaille M., Rebois R.V., Hebert T.E. The role of Gβγ subunits in the organization, assembly, and function of GPCR signaling complexes. Annual Review of Pharmacology and Toxicology 2009, 49:31-56.
48. Dupre D.J., Robitaille M., Richer M., Ethier N., Mamarbachi A.M., Hebert T.E. Dopamine receptor-interacting protein 78 acts as a molecular chaperone for Gγ subunits before assembly with Gβ. The Journal of Biological Chemistry 2007, 282:13703-13715.
49. Egbuna O.I., Brown E.M. Hypercalcaemic and hypocalcaemic conditions due to calcium-sensing receptor mutations. Best Practice & Research. Clinical Rheumatology 2008, 22:129-148.
50. Eren P.A., Turan K., Berber I., Canbakan M., Kara M., Tellioglu G., Bugan U., Sevinc C., Turkmen F., Titiz M.I. The clinical significance of parathyroid tissue calcium sensing receptor gene polymorphisms and expression levels in end-stage renal disease patients. Clinical Nephrology 2009, 72:114-121.
51. Evenepoel P. Calcimimetics in chronic kidney disease: Evidence, opportunities and challenges. Kidney International 2008, 74:265-275.
52. Feng J., Petersen C.D., Coy D.H., Jiang J.-K., Thomas C.J., Pollak M.R., Wank S.A. Calcium-sensing receptor is a physiologic multimodal chemosensor regulating gastric G-cell growth and gastrin secretion. Proceedings of the National Academy of Sciences of the United States of America 2010, 107:17791-17796.
53. Finney B.A., del Moral P.M., Wilkinson W.J., Cayzac S., Cole M., Warburton D., Kemp P.J., Riccardi D. Regulation of mouse lung development by the extracellular calcium-sensing receptor, CaR. The Journal of Physiology 2008, 586:6007-6019.
54. Fryer R.M., Segreti J.A., Widomski D.L., Franklin P.H., Banfor P.N., Koch K.A., Nakane M., Wu-Wong J.R., Cox B.F., Rinehart G.A. Systemic activation of the calcium sensing receptor produces acute effects on vascular tone and circulatory function in uremic and normal rats: Focus on central versus peripheral control of vascular tone and blood pressure by cinacalcet. The Journal of Pharmacology and Experimental Therapeutics 2007, 323:217-226.
55. Gama L., Breitwieser G.E. A carboxyl-terminal domain controls the cooperativity for extracellular Ca2+ activation of the human calcium sensing receptor: A study with receptor-green fluorescent protein fusions. The Journal of Biological Chemistry 1998, 273:29712-29718.
56. Gardner R.G., Swarbrick G.M., Bays N.W., Cronin S.R., Wilhovsky S., Seelig L., Kim C., Hampton R.Y. Endoplasmic reticulum degradation requires lumen to cytosol signaling: Transmembrane control of Hrd1p by Hrd3p. The Journal of Cell Biology 2000, 151:69-82.
57. Girod A., Kinzel V., Bossemeyer K. In vivo activation of recombinant cAPK catalytic subunit active site mutants by coexpression of the wild-type enzyme, evidence for intermolecular cotranslational phosphorylation. FEBS Letters 1996, 391:121-125.
58. Harrington P.E., Fotsch C. Calcium sensing receptor activators: Calcimimetics. Current Medicinal Chemistry 2007, 14:3027-3034.
59. Herrera-Vigenor F., Hernandez-Garcia R., Valadez-Sanchez M., Vazquez-Prado J., Reyes-Cruz G. AMSH regulates calcium-sensing receptor signaling through direct interactions. Biochemical and Biophysical Research Communications 2006, 347:924-930.
60. Hizaki K., Yamomoto H., Taniguchi H., Adachi Y., Nakazawa M., Tanuma T., Kato N., Sukawa Y., Sanchez J.V., Suzuki H., Sasaki S., Imai K., Shinomura Y. Epigenetic inactivation of calcium-sensing receptor in colorectal carcinogenesis. Modern Pathology 2011, 24:876-884.
61. Hlavackova V., Goudet C., Kniazeff J., Zikova A., Maurel D., Vol C., Trojanova J., Prezeau L., Pin J.-P., Blahos J. Evidence for a single heptahelical domain being turned on upon activation of a dimeric GPCR. The EMBO Journal 2005, 24:499-509.
62. Hobson S.A., McNeil S.E., Lee F., Rodland K.D. Signal transduction mechanisms linking increased extracellular calcium to proliferation in ovarian surface epithelial cells. Experimental Cell Research 2000, 258:1-11.
63. Hodgkin M.N., Hills C.E., Squires P.E. The calcium-sensing receptor and insulin secretion: A role outside systemic control 15 years on. The Journal of Endocrinology 2008, 199:1-4.
64. Hofer A.M., Brown E.M. Extracellular calcium sensing and signalling. Nature Reviews. Molecular Cell Biology 2003, 4:530-538.
65. Hofer A.M., Gerbino A., Caroppo R., Curci S. The extracellular calcium-sensing receptor and cell-cell signaling in epithelia. Cell Calcium 2004, 35:297-306.
66. Hofer A.M., Lefkimmiatis K. Extracellular calcium and cAMP: Second messengers as 'third messengers'?. Physiology (Bethesda) 2007, 22:320-327.
67. Hosokawa N., Kamiya Y., Kamiya D., Kato K., Nagata K. Human OS-9, a lectin required for glycoprotein endoplasmic reticulum-associated degradation, recognizes mannose-trimmed N-glycans. The Journal of Biological Chemistry 2009, 284:17061-17068.
68. Hovland R., Doskeland A.P., Eikhom T.S., Robaye B., Doskeland S.O. cAMP induces co-translational modification of proteins in IPC-81 cells. The Biochemical Journal 1999, 342:369-377.
69. Hu J., Hauache O., Spiegel A.M. Human Ca2+ receptor cysteine-rich domain. Analysis of function of mutant and chimeric receptors. The Journal of Biological Chemistry 2000, 275:16382-16389.
70. Hu J., Spiegel A.M. Structure and function of the human calcium-sensing receptor: Insights from natural and engineered mutations and allosteric modulators. Journal of Cellular and Molecular Medicine 2007, 11:908-922.
71. Huang Y., Breitwieser G.E. Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint in receptor biogenesis. The Journal of Biological Chemistry 2007, 282:8517-9524.
72. Huang Z., Cheng S.L., Slatopolsky E. Sustained activation of the extracellular signal-regulated kinase pathway is required for extracellular calcium stimulation of human osteoblast proliferation. The Journal of Biological Chemistry 2001, 276:21351-21358.
73. Huang C., Hydo L.M., Liu S., Miller R.T. Activation of choline kinase by extracellular Ca2+ is Ca2+-sensing receptor, Galpha12 and Rho-dependent in breast cancer cells. Cellular Signalling 2009, 21:1894-1900.
74. Huang Y., Niwa J., Sobue G., Breitwieser G.E. Calcium-sensing receptor ubiquitination and degradation mediated by the E3 ubiquitin ligase dorfin. The Journal of Biological Chemistry 2006, 281:11610-11617.
75. Huang Y., Zhou Y., Yang W., Butters R., Lee W.H., Li S., Castiblanco A., Brown E.M., Yang J.J. Identification and dissection of Ca2+-binding sites in the extracellular domain of Ca2+-sensing receptor. The Journal of Biological Chemistry 2007, 282:19000-19010.
76. Jacob C., Cottrell G.S., Gehringer D., Schmidlin F., Grady E.F., Bunnett N.W. c-Cbl mediates ubiquitination, degradation, and down-regulation of human protease-activated receptor 2. The Journal of Biological Chemistry 2005, 280:8929-8937.
77. Jalink K., Moolenaar W.H. G protein-coupled receptors: The inside story. BioEssays 2010, 32:13-16.
78. Jensen A.A., Brauner-Osborne H. Allosteric modulation of the calcium-sensing receptor. Current Neuropharmacology 2007, 5:180-188.
79. Jong Y.-J.I., Kumar V., Kingston A.E., Romano C., O'Malley K.L. Functional metabotropic glutamate receptors on nuclei from brain and primary cultured striatal neurons. Role of transporters in delivering ligand. The Journal of Biological Chemistry 2005, 280:30469-30480.
80. Jong Y.J.I., Kumar V., O'Malley K.L. Intracellular metabotropic glutamate receptor 5 (mguR5) activates signaling cascades distinct from cell surface counterparts. The Journal of Biological Chemistry 2009, 284:35827-35838.
81. Kaul D., Wu C.L., Adkins C.B., Jordan K.W., Defeo E.M., Habbel P., Peterson R.T., McDougal W.S., Pohl U., Cheng L.L. Assessing prostate cancer growth with mRNA of spermine metabolic enzymes. Cancer Biology & Therapy 2010, 9:736-742.
82. Kawata T., Nagano N., Obi M., Miyata S., Koyama C., Kobayashi N., Wakita S., Wada M. Cinacalcet suppresses calcification of the aorta and heart in uremic rats. Kidney International 2008, 74:1270-1277.
83. Kessler A., Faure H., Petrel C., Rognan D., Cersario M., Ruat M., Dauban P., Dodd R.H. N1-Benzoyl-N2-[1-(1-napthyl)ethyl]-trans-1,2-diaminocyclohexanes: Development of 4-chlorophenylcarboxamide (calhex 231) as a new calcium sensing receptor ligand demonstrating potent calcilytic activity. Journal of Medicinal Chemistry 2006, 49:5119-5128.
84. Kifor O., Kifor I., Moore F.D., Butters R.R., Cantor T., Gao P., Brown E.M. Decreased expression of caveolin-1 and altered regulation of mitogen-activated protein kinase in cultured bovine parathyroid cells and human parathyroid adenomas. The Journal of Clinical Endocrinology and Metabolism 2002, 88:4455-4464.
85. Kifor O., MacLeod R.J., Diaz R., Bai M., Yamaguchi T., Yao T., Kifor I., Brown E.M. Regulation of MAP kinase by calcium -sensing receptor in bovine parathyroid and CaR-transfected HEK293 cells. American Journal of Physiology. Renal Physiology 2001, 280:F291-F302.
86. Kitsou-Mylona I., Burns C.J., Squires P.E., Persaud S.J., Jones P.M. A role for the extracellular calcium-sensing receptor in cell-cell communication in pancreatic islets of langerhans. Cellular Physiology and Biochemistry 2008, 22:557-566.
87. Kniazeff J., Prezeau L., Rondard P., Pin J.-P., Goudet C. Dimers and beyond: The functional puzzles of class C GPCRs. Pharmacology & Therapeutics 2011, 130:9-25.
88. Koleganova N., Piecha G., Ritz E., Schmott C.P., Gross M.L. A calcimimetic (R-568) but not calcitriol, prevents vascular remodeling in uremia. Kidney International 2009, 75:60-71.
89. Kumar V., Jong Y.-J.I., O'Malley K.L. Activated nuclear metabotropic glutamate receptor mGlu5 couples to nuclear Gq/11 proteins to generate inositol 1,4,5-trisphosphate-mediated nuclear Ca2+ release. The Journal of Biological Chemistry 2008, 283:14072-14083.
90. Kumar R., Thompson J.R. The regulation of parathyroid hormone secretion and synthesis. Journal of the American Society of Nephrology 2011, 22:216-224.
91. Lee D.K., Lanca A.J., Cheng R., Nguyen T., Ji X.D., Gobeil F., Chemtob S., George S.R., O'Dowd B.F. Agonist-independent nuclear localization of the apelin, angiotensin AT1, and bradykinin B2 receptors. The Journal of Biological Chemistry 2004, 279:7901-7908.
92. Leskela T.T., Markkanen P.M.H., Pietila E.M., Tuusa J.T., Petaja-Repo U.E. Opioid receptor pharmacological chaperones act by binding and stabilizing newly synthesized receptor in the endoplasmic reticulum. The Journal of Biological Chemistry 2007, 282:23171-23183.
93. Letz S., Rus R., Haag C., Dorr H.G., Schnabel D., Mohlig M., Schulze E., Frank-Raue K., Raue F., Mayr B., Schofl C. Novel activating mutations of the calcium-sensing receptor: The calcilytic NPS 2143 mitigates excessive signal transduction of mutant receptors. The Journal of Clinical Endocrinology and Metabolism 2010, 95:E229-E233.
94. Lewis R.S. Calcium oscillations in T-cells: Mechanisms and consequences for gene expression. Biochemical Society Transactions 2003, 31:925-929.
95. Li W.-H., Llopis J., Whitney M., Zlokarnik G., Tsien R.Y. Cell-permeant caged InsP3 ester shows that Ca2+ spike frequency can optimize gene expression. Nature 1998, 392:936-941.
96. Li H., Ruan G., Li Z., Liu Z., Zheng X., Cheng G., Li B., Zhan M. The calcimimetic R-568 induces apoptotic cell death in prostate cancer cells. Journal of Experimental & Clinical Cancer Research 2009, 28:100.
97. Lienhardt A., Bai M., Lagarde J.P., Rigaud M., Zhang Z., Jiang Y., Kottler M.-L., Brown E.M., Garabedian M. Activating mutations of the calcium-sensing receptor: Management of hypocalcemia. The Journal of Clinical Endocrinology and Metabolism 2001, 86:5313-5323.
98. Lin K.I., Chattopadhyay N., Bai M., Alvarez R., Dang C.V., Baraban J.M., Brown E.M., Ratan R.R. Elevated extracellular calcium can prevent apoptosis via the calcium-sensing receptor. Biochemical and Biophysical Research Communications 1998, 249:325-331.
99. Liu G., Hu X., Chakrabarty S. Calcium sensing receptor down-regulates malignant cell behavior and promotes chemosensitivity in human breast cancer cells. Cell Calcium 2009, 45:216-225.
100. Loo T.W., Clarke D.M. Chemical and pharmacological chaperones as the new therapeutic agents. Expert Reviews in Molecular Medicine 2008, 9:1-18.
101. Loretz C.A. Extracellular calcium-sensing receptors in fishes. Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology 2008, 149:225-245.
102. Loretz C.A., Pollina C., Hyodo S., Takei Y., Chang W., Shoback D. cDNA cloning and functional expression of a Ca2+-sensing receptor with truncated C-terminal tail from the Mozambique tilapia (Oreochromis mossambicus). The Journal of Biological Chemistry 2004, 279:53288-53297.
103. Lu J.Y., Yang Y., Gnacadja G., Christopoulos A., Reagan J.D. Effect of the calcimimetic R-568 [e-(2-chlorophenyl)-N-((1R)-1-(emethoxyphenyl)ethyl)-1-propanamine] on correcting inactivating mutations in the human calcium-sensing receptor. The Journal of Pharmacology and Experimental Therapeutics 2009, 331:775-786.
104. Ma J.N., Owens M., Gustafsson M., Jensen J., Tabatabaei A., Schmelzer K., Olsson R., Burstein E.S. Characterization of highly efficacious allosteric agonists of the human calcium-sensing receptor. The Journal of Pharmacology and Experimental Therapeutics 2011, 337:275-284.
105. MacLeod J.R., Yano S., Chattopadhyay N., Brown E.M. Extracellular calcium-sensing receptor transactivates the epidermal growth factor receptor by a triple-membrane-spanning signaling mechanism. Biochemical and Biophysical Research Communications 2004, 320:455-460.
106. Mah S.J., Cornell E., Mitchell N.A., Fleck M.W. Glutamate receptor trafficking: Endoplasmic reticulum quality control involves ligand binding and receptor function. The Journal of Neuroscience 2005, 25:2215-2225.
107. Mamillapalli R., VanHouten J., Zawalich W., Wysolmerski J. Switching of G-protein usage by the calcium-sensing receptor reverses its effect on parathyroid hormone-related protein secretion in normal versus malignant breast cells. The Journal of Biological Chemistry 2008, 283:24435-24447.
108. Mancilla E.E., De Luca F., Baron J. Activating mutations of the Ca2+-sensing receptor. Molecular Genetics and Metabolism 1998, 64:198-204.
109. McCormick W.D., Atkinson-Dell R., Campion K.L., Mun H.C., Conigrave A.D., Ward D.T. Increased receptor stimulation elicits differential calcium-sensing receptor(T888) dephosphorylation. The Journal of Biological Chemistry 2010, 285:14170-14177.
110. Mendoza F.J., Lopez I., Canalejo R., Almaden Y., Martin D., Aguilera-Tejero E., Rodriguez M. Direct upregulation of parathyroid calcium-sensing receptor and vitamin D receptor by calcimimetics in uremic rats. American Journal of Physiology. Renal Physiology 2009, 296:F605-F613.
111. Messa P., Alfieri C., Brezzi G. Cinacalcet: Pharmacological and clinical aspects. Expert Opinion on Drug Metabolism and Toxicology 2008, 4:1551-1560.
112. Miedlich S., Gama L., Breitwieser G.E. Calcium sensing receptor activation by a calcimimetic suggests a link between cooperativity and intracellular calcium oscillations. The Journal of Biological Chemistry 2002, 277:49691-49699.
113. Miedlich S.U., Gama L., Seuwen K., Wolf R.M., Breitwieser G.E. Homology modeling of the transmembrane domain of the human calcium sensing receptor and localization of an allosteric binding site. The Journal of Biological Chemistry 2004, 279:7254-7263.
114. Mizobuchi M., Hatamura I., Ogata H., Saji F., Uda S., Shiizaki K., Sakaguchi T., Negi S., Kinugasa E., Koshikawa S., Akizawa T. Calcimimetic compound upregulates decreased calcium-sensing receptor expression level in parathyroid glands of rats with chronic renal insufficiency. Journal of the American Society of Nephrology 2004, 15:2579-2587.
115. Monnier C., Tu H., Bourrier E., Vol C., Lamarque L., Trinquet E., Pin J.-P., Rondard P. Trans-activation between TM domains: Implication in heterodimeric GABAB receptor activation. The EMBO Journal 2011, 30:32-42.
116. Moriyoshi K., Iijima K., Fujii H., Ito H., Cho Y., Nakanishi S. Seven in absentia homolog 1A mediates ubiquitination and degradation of group 1 metabotropic glutamate receptors. Proceedings of the National Academy of Sciences of the United States of America 2004, 101:8614-8619.
117. Murphy J.E., Padilla B.E., Hasdemir B., Cottrell G.S., Bunnett N.W. Endosomes: A legitimate platform for the signaling train. Proceedings of the National Academy of Sciences of the United States of America 2009, 106:17615-17622.
118. Nemeth E.F. Receptor antagonists. The search for calcium receptor antagonists (calcilytics). Journal of Molecular Endocrinology 2002, 29:15-21.
119. Nemeth E.F. Misconceptions about calcimimetics. Annals of the New York Academy of Sciences 2006, 1068:471-476.
120. Nemeth E.F., DelMar E.G., Heaton W.L., Miller M.A., Lambert L.D., Conklin R.L., Gowen M., Gleason J.G., Bhalnagar P.K., Fox J. Calcilytic compounds: Potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. The Journal of Pharmacology and Experimental Therapeutics 2001, 299:323-331.
121. Nemeth E.F., Fox J. Calcimimetic compounds: A direct approach to controlling plasma levels of parathyroid hormone in hyperparathyroidism. Trends in Endocrinology and Metabolism 1999, 10:66-71.
122. Nemeth E.F., Heaton W.H., Miller M., Fox J., Balandrin M.F., Van Wagenen B.C., Colloton M., Karbon W., Scherrer J., Schatzen E., Rishton G., Scully S., Qi M., Harris R., Lacey D., Martin D. Pharmacodynamics of the type II calcimimetic compound cinacalcet HCl. The Journal of Pharmacology and Experimental Therapeutics 2004, 308:627-635.
123. Nemeth E.F., Steffey M.E., Hammerland L.G., Hung B.C., Van Wagenen B.C., DelMar E.G., Balandrin M.F. Calcimimetics with potent and selective activity on the parathyroid calcium receptor. Proceedings of the National Academy of Sciences of the United States of America 1998, 85:4040-4045.
124. Oda Y., Tu C.L., Chang W., Crumrine D., Komuves L., Mauro T., Elias P.M., Bikle D.D. The calcium sensing receptor and its alternatively spliced form in murine epidermal differentiation. The Journal of Biological Chemistry 2000, 275:1183-1190.
125. Oda Y., Tu C.-L., Pillai S., Bikle D.D. The calcium sensing receptor and its alternatively spliced form in keratinocyte differentiation. The Journal of Biological Chemistry 1998, 273:23344-23352.
126. Oh W.J., Wu C.C., Kim S.J., Facchinetti V., Julien L.A., Finlan M., Roux P.P., Su B., Jacinto E. mTORC2 can associate with ribosomes to promote cotranslational phosphorylation and stability of nascent Akt polypeptide. The EMBO Journal 2010, 29:3939-3951.
127. Ohsu T., Amino Y., Nagasaki H., Yamanaka T., Takeshita S., Hatanaka T., Maruyama Y., Miyamura N., Eto Y. Involvement of the calcium-sensing receptor in human taste perception. The Journal of Biological Chemistry 2010, 285:1016-1022.
128. Palmer A.J., Wallace H.M. The polyamine transport system as a target for anticancer drug development. Amino Acids 2010, 38:415-522.
129. Penn A.C., Williams S.R., Greger I.H. Gating motions underlie AMPA receptor secretion from the endoplasmic reticulum. The EMBO Journal 2008, 27:3056-3068.
130. Petrel C., Kessler A., Dauban P., Dodd R.H., Rognan D., Ruat M. Positive and negative allosteric modulators of the Ca2+ sensing receptor interact with overlapping but not identical binding sites in the transmembrane domain. The Journal of Biological Chemistry 2004, 279:18990-18997.
131. Pidasheva S., Grant M., Canaff L., Ercan O., Kumar U., Hendy G.N. Calcium-sensing receptor dimerizes in the endoplasmic reticulum: Biochemical and biophysical characterization of CASR mutants retained intracellularly. Human Molecular Genetics 2006, 15:2200-2209.
132. Piecha G., Kokeny G., Nakagawa K., Koleganova N., Geldyyev A., Berger I., Ritz E., Schmitt C.P., Gross M.-L. Calcimimetic R-568 or calcitriol: Equally beneficial on progress of renal damage in subtotally nephrectomized rats. American Journal of Physiology. Renal Physiology 2008, 294:F748-F757.
133. Revankar C.M., Mitchell H.D., Field A.S., Burai R., Corona C., Ramesh C., Sklar L.A., Arterburn J.B., Prossnitz E.R. Synthetic estrogen derivatives demonstrate the functionality of intracellular GPR30. ACS Chemical Biology 2007, 2:536-544.
134. Reyes-Ibarra A.P., Garcia-Regalado A., Ramirez-Rangel I., Esparza-Silva A.L., Valadez-Sanchez M., Vazquez-Prado J., Reyes-Cruz G. Calcium-sensing receptor endocytosis links extracellular calcium signaling to parathyroid hormone-related peptide secretion via a Rab11a-dependent and AMSH-sensitive mechanism. Molecular Endocrinology 2007, 21:1394-1407.
135. Riccardi D., Hall A.E., Chattopadhyay N., Xu J.Z., Brown E.M., Hebert S.C. Localization of the extracellular Ca2+/polyvalent cation-sensing protein in rat kidney. American Journal of Physiology. Renal Physiology 1998, 274:F611-F622.
136. Riccardi D., Traebert M., Ward D.T., Kaissling B., Biber J., Hebert S.C., Murer H. Dietary phosphate and parathyroid hormone alter the expression of the calcium-sensing receptor (CaR) and the Na+-dependent Pi transporter (NaPi-2) in the rat proximal tubule. Pflügers Archiv 2000, 441:379-387.
137. Rothe H., Mayer G. Clinical importance of calcium-sensing receptor gene polymorphism Arg990Gly in the age of calcimimetic therapy. Current Pharmacogenomics 2006, 4:153-156.
138. Rothe H.M., Shapiro W.B., Sun W.Y., Chou S.Y. Calcium-sensing receptor gene polymorphism Arg990Gly and its possible effect on response to cinacalcet HCl. Pharmacogenetics and Genomics 2005, 15:29-34.
139. Rus R., Haag C., Bumke-Vogt C., Bahr V., Mayr B., Mohlig M., Schulze E., Frank-Raue K., Raue F., Schofl C. Novel inactivating mutations of the calcium-sensing receptor: The calcimimetic NPS R-568 improves signal transduction of mutant receptors. The Journal of Clinical Endocrinology and Metabolism 2008, 93:4797-4803.
140. Ryan Z.C., Craig T.A., Venyaminov S.Y., Thompson J.R., Kumar R. Biophysical properties of the extra-cellular domain of the calcium-sensing receptor. Biochemical and Biophysical Research Communications 2006, 349:339-344.
141. Saidak Z., Boudot C., Abdoune R., Petit L., Brazier M., Mentaverri R., Kamel S. Extracellular calcium promotes the migration of breast cancer cells through the activation of the calcium sensing receptor. Experimental Cell Research 2009, 315:2072-2080.
142. Saidak Z., Mentaverri R., Brown E.M. The role of the calcium-sensing receptor in the development and progression of cancer. Endocrine Reviews 2009, 30:178-195.
143. Sallette J., Pons S., Devillers-Thiery A., Soudant M., de Carvalho L.P., Changeaux J.P., Corringer P.J. Nicotine upregulates its own receptors through enhanced intracellular maturation. Neuron 2005, 46:595-607.
144. Sanders J.L., Chattopadhyay N., Kifor O., Yamaguchi T., Brown E.M. Ca2+-sensing receptor expression and PTHrP secretion in PC-3 human prostate cancer cells. American Journal of Physiology. Endocrinology and Metabolism 2001, 281:E1267-E1274.
145. Sato B.K., Schulz D., Do P.H., Hampton R.Y. Misfolded membrane proteins are specifically recognized by the transmembrane domain of the Hrd1p ubiquitin ligase. Molecular Cell 2009, 34:212-222.
146. Schwartz G.G., John E.M., Rowland G., Ingles S.A. Prostate cancer in African-American men and polymorphism in the calcium-sensing receptor. Cancer Biology & Therapy 2010, 9:994-999.
147. Scott G.K., Gu F., Crump C.M., Thomas L., Wan L., Xiang Y., Thomas G. The phosphorylation state of an autoregulatory domain controls PACS-1-directed protein traffic. The EMBO Journal 2003, 22:6234-6244.
148. Skatch W.R. Cellular mechanisms of membrane protein folding. Nature Structural and Molecular Biology 2009, 16:606-612.
149. Smajilovic S., Tfelt-Hansen J. Calcium acts as a first messenger through the calcium-sensing receptor in the cardiovascular system. Cardiovascular Research 2007, 75:457-467.
150. Soda K. Polyamine intake, dietary pattern, and cardiovascular disease. Medical Hypotheses 2010, 75:299-301.
151. Srinivasan R., Pantoja R., Moss F.J., Mackey E.D.W., Son C.D., Miwa J., Lester H.A. Nicotine up-regulates α4β2 nicotinic receptors and ER exit sites via stoichiometry-dependent chaperoning. The Journal of General Physiology 2010, 137:59-79.
152. Steir C., Veis A. Casein kinase localization in the endoplasmic reticulum of the ROS 17/2.8 cell line. Journal of Bone and Mineral Research 1995, 10:607-615.
153. Stepanchick A., Breitwieser G.E. The cargo receptor p24A facilitates calcium sensing receptor maturation and stabilization in the early secretory pathway. Biochemical and Biophysical Research Communications 2010, 395:136-140.
154. Stepanchick A., McKenna J., McGovern O., Huang Y., Breitwieser G.E. Calcium sensing receptor mutations implicated in pancreatitis and idiopathic epilepsy syndrome disrupt an arginine-rich retention motif. Cellular Physiology and Biochemistry 2010, 26:363-374.
155. Sun J., Murphy E. Calcium-sensing receptor: A sensor and mediator of ischemic preconditioning in heart. American Journal of Physiology. Heart and Circulatory Physiology 2010, 299:1309-1317.
156. Tang C.M., Insel P.A. Genetic variation in G-protein-coupled receptors-Consequences for G-protein-coupled receptors as drug targets. Expert Opinion on Therapeutic Targets 2005, 9:1247-1265.
157. Tantini B., Fiumana E., Cetrullo S., Pignatti C., Bonavita F., Shantz L.M., Giordano E., Muscari C., Flamigni F., Guarnieri C., Stefanelli C., Caldarera C.M. Involvement of polyamines in apoptosis of cardiac myoblasts in a model of simulated ischemia. Journal of Molecular and Cellular Cardiology 2006, 40:775-782.
158. Tfelt-Hansen J., Brown E.M. The calcium-sensing receptor in normal physiology and pathophysiology: A review. Critical Reviews in Clinical Laboratory Sciences 2005, 42:35-70.
159. Tfelt-Hansen J., MacLeod R.J., Chattopadhyay N., Yano S., Quinn S., Ren X., Terwilliger E.F., Schwarz P., Brown E.M. Calcium-sensing receptor stimulates PTHrP release by pathways dependent on PKC, p38 MAPK, JNK, and ERK1/2 in H-500 cells. American Journal of Physiology. Endocrinology and Metabolism 2003, 285:E329-E337.
160. Thompson M.D., Burnham W.M., Cole D.E. The G protein-coupled receptors: Pharmacogenetics and disease. Critical Reviews in Clinical Laboratory Sciences 2005, 42:311-392.
161. Timmers H.J., Karperien M., Hamdy N.A., de Boer H., Hermus A.R. Normalization of serum calcium by cinacalcet in a patient with hypercalcaemia due to a de novo inactivating mutation of the calcium-sensing receptor. Journal of Internal Medicine 2006, 260:177-182.
162. Tu C.-L., Chang W., Bikle D.D. The role of the calcium sensing receptor in regulating intracellular calcium handling in human epidermal keratinocytes. The Journal of Investigative Dermatology 2007, 127:1074-1083.
163. Ulloa-Aguirre A., Conn P.M. Targeting of G protein-coupled receptors to the plasma membrane in health and disease. Frontiers in Bioscience 2009, 14:973-994.
164. Urwyler S. Allosteric modulation of family C G-protein-coupled receptors: From molecular insights to therapeutic perspectives. Pharmacological Reviews 2011, 63:59-126.
165. Van Craenenbroeck K., Clark S.D., Cox M.J., Oak J.N., Liu F., Van Tol H.H.M. Folding efficiency is rate-limiting in dopamine D4 receptor biogenesis. The Journal of Biological Chemistry 2005, 280:19350-19357.
166. Vaniotis G., Del Duca D., Trieu P., Rohlicek C.V., Hebert T.E., Allen B.G. Nuclear β-adrenergic receptors modulate gene expression in adult rat heart. Cellular Signalling 2011, 23:89-98.
167. Vargas-Poussou R., Huang C., Hulin P., Houillier P., Jeunemaitre X., Paillard M., Planelles G., Dechaux M., Miller R.T., Antignac C. Functional characterization of a calcium-sensing receptor mutation in severe autosomal dominant hypocalcemia with a Bartter-like syndrome. Journal of the American Society of Nephrology 2002, 13:2259-2266.
168. Vizard T.N., O'Keeffe G.W., Gutierrez H., Kos C.H., Riccardi D., Davies A.M. Regulation of axonal and dendritic growth by the extracellular calcium-sensing receptor. Nature Neuroscience 2008, 11:285-291.
169. Wallace H.M., Duthie J., Evans D.M., Lamond S., Nicoll D.M., Heys S.D. Alterations in polyamine catabolic enzymes in human breast cancer tissue. Clinical Cancer Research 2000, 6:3657-3661.
170. Wan L., Molloy S.S., Thomas L., Liu G., Xiang Y., Rybak S.L., Thomas G. PACS-1 defines a novel gene family of cytosolic sorting proteins required for trans-Golgi network localization. Cell 1998, 94:205-216.
171. Wang M., Yao Y., Kuang D., Hampson D.R. Activation of family C G-protein-coupled receptors by the tripeptide glutathione. The Journal of Biological Chemistry 2006, 281:8864-8870.
172. White E., McKenna J., Cavanaugh A., Breitwieser G.E. Pharmacochaperone-mediated rescue of calcium-sensing receptor loss-of-function mutants. Molecular Endocrinology 2009, 23:1115-1123.
173. Whitfield J.F. Calcium, calcium-sensing receptor and colon cancer. Cancer Letters 2009, 275:9-16.
174. Wright C.D., Chen Q., Baye N.L., Huang Y., Healy C.L., Kasinathan S., O'Connell T.D. Nuclear α1-adrenergic receptors signal activated ERK localization to caveolae in adult cardiac myocytes. Circulation Research 2008, 103:992-1000.
175. Wuller S., Siesner B., Loffler A., Furkert J., Krause G., Hermosilla R., Schaefer M., Schulein R., Rosenthal W., Okshe A. Pharmacochaperones post-translationally enhance cell surface expression by increasing conformational stability of wild-type and mutant vasopressin V2 receptors. The Journal of Biological Chemistry 2004, 279:47254-47263.
176. Xie L., Xiao K., Whalen E.J., Forrester M.T., Freeman R.S., Fong G., Gygi S.P., Lefkowitz R.J., Stamler J.S. Oxygen-regulated β2-adrenergic receptor hydroxylation by EGLN3 and ubiquitylation by pVHL. Science Signaling 2009, 2:ra33.
177. Yamaguchi T., Yamaguchi M., Sugimoto T., Chauhan D., Anderson K.C., Brown E.M., Chihara K. The extracellular calcium (Ca2+o)-sensing receptor is expressed in myeloma cells and modulates cell proliferation. Biochemical and Biophysical Research Communications 2002, 299:532-538.
178. Yang Y., Nishimura I., Imai Y., Takahashi R., Lu B. Parkin suppresses dopaminergic neuron-selective neurotoxicity induced by Pael-R in Drosophila. Neuron 2003, 37:911-924.
179. Yano S., MacLeod R.J., Chattopadhyay N., Tfelt-Hansen J., Kifor O., Butters R.R., Brown E.M. Calcium-sensing receptor activation stimulates parathyroid hormone-related protein secretion in prostate cancer cells: Role of epidermal growth factor receptor transactivation. Bone 2004, 35:664-672.
180. Yano S., Sugimoto T., Tsukamoto T., Chihara K., Kobayashi A., Kitazawa S., Maeda S., Kitazawa R. Decrease in vitamin D receptor and calcium-sensing receptor in highly proliferative parathyroid adenomas. European Journal of Endocrinology 2003, 148:403-411.
181. Yoshida M., Mori A., Inaba A., Makino H., Yamaguchi M., Fujita H., Kawamoto T., Goto M., Kimura H., Baba A., Yasuma T. Synthesis and structure-activity relationship of tetrahydropyrazolopyrimidine derivatives-A novel structural class of potent calcium-sensing receptor antagonists. Bioorganic & Medicinal Chemistry 2010, 18:8501-8511.
182. Young S.H., Rozengurt E. Amino acids and Ca2+ stimulate different patterns of Ca2+ oscillations through the Ca2+-sensing receptor. American Journal of Physiology. Cell Physiology 2002, 282:C1414-C1422.
183. Yun F.H., Wong B.Y., Chase M., Shuen A.Y., Canaff L., Thongthai K., Siminovitch K., Hendy G.N., Cole D.E. Genetic variation at the calcium-sensing receptor (CASR) locus: Implications for clinical molecular diagnostics. Clinical Biochemistry 2007, 40:551-561.
184. Zhang M., Breitwieser G.E. High affinity interaction with filamin A protects against calcium-sensing receptor degradation. The Journal of Biological Chemistry 2005, 280:11140-11146.