Calcium agonists in hyperparathyroidism

Expert Opinion on Investigational Drugs

Volumn 13, Issue 3, 2004, Pages 229-244

  Falchetti, Alberto ^a  

^a UNIVERSITY OF FLORENCE   (Italy)

Author keywords

Calcimimetics; Calcium sensing receptor; Chronic renal failure; G protein coupled receptor; Hypercalcaemia; Hyperparathyroidism

Indexed keywords

1 (3 METHOXYPHENYL) N (3 PHENYLPROPYL)ETHYLAMINE; [N [3 (2 CHLOROPHENYL)PROPYL]] ALPHA METHYL 3 METHOXYBENZYLAMINE; ACETYLCHOLINE; CALCIMIMETIC AGENT; CALCITONIN; CALCIUM; CALCIUM CHANNEL STIMULATING AGENT; CALCIUM SENSING RECEPTOR; CINACALCET; G PROTEIN COUPLED RECEPTOR; GENTAMICIN; KANAMYCIN B; LANTHANUM; MAGNESIUM; MEMBRANE RECEPTOR; METABOTROPIC RECEPTOR; N [3 (2 CHLOROPHENYL)PROPYL] 1 (3 METHOXYPHENYL)ETHYLAMINE; NEOMYCIN; PARATHYROID HORMONE; PHOSPHOLIPASE A2; PLACEBO; POLYARGININE; POLYLYSINE; PROTAMINE; R 568; SPERMIDINE; SPERMINE; STREPTOMYCIN; UNCLASSIFIED DRUG; UNINDEXED DRUG; VITAMIN D; VITAMIN D RECEPTOR;

ABDOMINAL PAIN; CALCIUM BLOOD LEVEL; CALCIUM HOMEOSTASIS; CELL PROLIFERATION; CHRONIC KIDNEY FAILURE; CLINICAL PRACTICE; CLINICAL STUDY; CROSS REACTION; DIARRHEA; DOSE RESPONSE; DRUG BINDING; DRUG EFFICACY; DRUG MECHANISM; DRUG SAFETY; EXTRACELLULAR CALCIUM; GASTROINTESTINAL SYMPTOM; HUMAN; HYPERCALCEMIA; HYPERPARATHYROIDISM; HYPOCALCEMIA; IN VITRO STUDY; IN VIVO STUDY; NAUSEA; PALLIATIVE THERAPY; PARATHYROID GLAND; PARATHYROID HORMONE RELEASE; REVIEW; VOMITING;

ANIMALS; CALCIUM; CALCIUM SIGNALING; DRUG INTERACTIONS; HOMEOSTASIS; HUMANS; HYPERPARATHYROIDISM; KIDNEY; NAPHTHALENES; PARATHYROID GLANDS; PARATHYROID NEOPLASMS; RECEPTORS, CALCIUM-SENSING;

EID: 1542708186     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.13.3.229     Document Type: Review

References (166)

1. BOCKAERT J, CLAEYSEN S, BECAMEL C et al.: G protein-coupled receptors: Dominant players in cell-cell communication. Int. Rev. Cytol. (2002) 212:63-132.
2. PIERCE KL, PREMONT RT, LEFKOWITZ RJ: Seven-transmembrane receptors. Nat. Rev. Mol. Cell. Biol. (2002) 3(9):639-650.
3. +-sensing receptor. In: The Principles of Bone Biology (Volume 1, 2nd edn), Bilezikian JP, Raisz LG, Rodan GA (Eds), Academic Press, San Diego, CA, USA (2002): 371-387.
4. COBURN JW, ELANGOVAN L, GOODMAN WG, FRAZAO JM: Calcium-sensing receptor and calcimimetic agents. Kidney Int. Suppl. (1999) 73:S52-S58.
5. 2+)-sensing receptor from bovine parathyroid. Nature (1993) 366(6455):575-580.
6. EMANUEL RL, ADLER GK, KIFOR O et al.: Calcium-sensing receptor expression and regulation by extracellular calcium in the AtT-20 pituitary cell line. Mol. Endocrinol. (1996) 10(5):555-565.
7. BROWN AJ, ZHONG M, FINCH J et al.: Rat calcium-sensing receptor is regulated by vitamin D but not by calcium. Am. J. Physiol. (1996) 270(3, Pt 2):F454-F460.
8. ROGERS KV, DUNN CK, CONKLIN RL et al.: Calcium receptor messenger ribonucleic acid levels in the parathyroid glands and kidney of vitamin D-deficient rats are not regulated by plasma calcium or 1,25-dihydroxyvitamin D3. Endocrinology (1995) 136(2):499-504.
9. MATHIAS RS, NGUYEN HT, ZHANG MY, PORTALE AA: Reduced expression of the renal calcium-sensing receptor in rats with experimental chronic renal insufficiency. J. Am. Soc. Nephrol. (1998) 9(11):2067-2074.
10. BROWN EM: Physiology and pathophysiology of the extracellular calcium-sensing receptor. Am. J. Med. (1999) 106(2):238-253.
11. 2+ store release. J. Biol. Chem. (1998) 273(33):21267-21275.
12. 2+O-sensing receptor. J. Biol. Chem. (1996) 271(32 ):19537-19545.
13. 2+)-sensing receptor (CaR) activate nonselective cation channels in HEK293 cells stably transfected with the human CaR. Biochem. Biophys. Res. Commun. (1996) 226(2):572-579.
14. +)-sensing, second messengers, and the control of parathyroid hormone secretion. Cell Calcium (1990) 11(5):333-337.
15. AWATA H, HUANG C, HANDLOGTEN ME, MILLER RT: Interaction of the calcium-sensing receptor and filamin, a potential scaffolding protein. J. Biol. Chem. (2001) 276(37):34871-34879.
16. HJALM G, MacLEOD RJ, KIFOR O et al.: Filamin-A binds to the carboxyl-terminal tail of the calcium-sensing receptor, an interaction that participates in CaR-mediated activation of mitogen-activated protein kinase. J. Biol. Chem. (2001) 276(37):34880-34887.
17. KIFOR O, MacLEOD RJ, DIAZ R et al.: Regulation of MAP kinase by calcium-sensing receptor in bovine parathyroid and CaR-transfected HEK293 cells. Am. J. Physiol. Renal. Physiol. (2001) 280(2):F291-F302.
18. McNEIL SE, HOBSON SA, NIPPER V, RODLAND KD: Functional calcium-sensing receptors in rat fibroblasts are required for activation of SRC kinase and mitogen-activated protein kinase in response to extracellular calcium. J. Biol. Chem. (1998) 273(2):1114-11120.
19. GARRETT JE, CAPUANO IV, HAMMERLAND LG et al.: Molecular cloning and functional expression of human parathyroid calcium receptor cDNAs. J. Biol. Chem. (1995) 270(21):12919-12925.
20. 2+)-sensing receptor modulates shark rectal gland function. J. Exp. Biol. (2002) 205(13):1889-1897.
21. CHENG SX, OKUDA M, HALL AE et al.: Expression of calcium-sensing receptor in rat colonic epithelium: Evidence for modulation of fluid secretion. Am. J. Physiol. Gastrointest. Liver Physiol. (2002) 283(1):G240-G250.
22. SPURR NK: Genetics of calcium-sensing-regulation of calcium levels in the body. Curr. Opin. Pharmacol. (2003) 3(3):291-294.
23. 2+ and other ions as extracellular (first) messengers. Physiol. Rev. (1991) 71(2):371-411.
24. BROWN EM, MacLEOD RJ: Extracellular calcium sensing and extracellular calcium signaling. Physiol. Rev. (2001) 81(1):239-297.
25. 2+/polyvalent cation-sensing protein in rat kidney. Am. J. Physiol. (1998) 274(3, Pt 2):F611-F622.
26. CARMELIET G, VAN CROMPHAUT S, DACI E et al.: Disorders of calcium homeostasis. Best Pract. Res. Clin. Endocrinol. Metab. (2003) 17(4):529-546.
27. BROWN EM, POLLAK M, HEBERT SC: The extracellular calcium-sensing receptor: Its role in health and disease. Annual Rev. Med. (1998) 49:15-29.
28. 2+ receptors. Mol. Pharmacol. (1999) 55(4):642-648.
29. MIKI H, MAERCKLEIN PB, FITZPATRICK LA: Spontaneous oscillations of intracellular calcium in single bovine parathyroid cells may be associated with the inhibition of parathyroid hormone secretion. Endocrinology (1995) 136(7):2954-2959.
30. BREITWIESER GE, GAMA L: Calcium-sensing receptor activation induces intracellular calcium oscillations. Am. J. Physiol. Cell. Physiol. (2001) 280(6):C1412-C1421.
31. RICCARDI D, PARK J, LEE WS et al.: Cloning and functional expression of a rat kidney extracellular calcium/polyvalent cation-sensing receptor. Proc. Natl. Acad. Sci. USA (1995) 92(1):131-135.
32. 2+-sensing receptor and PTH/PTHrP receptor in rat kidney. Am. J. Physiol. (1996) 271:F951-F956.
33. PEARCE SH, WILLIAMSON C, KIFOR O et al.: A familial syndrome of hypocalcemia with hypercalciuria due to mutations in the calcium-sensing receptor. N. Engl. J. Med. (1996) 335(15):1115-1122.
34. THAKKER RV: Disorders of the calcium-sensing receptor. Biochem. Biophys. Acta (1996) 1448:166-170.
35. 2+)-sensing receptor in divalent mineral ion homeostasis. J. Exp. Biol. (1997) 200:(2):295-302.
36. VEZZOLI G, TANINI A, FERRUCCI L et al.: Influence of calcium-sensing receptor gene on urinary calcium excretion in stone-forming patients. J. Am. Soc. Nephrol. (2002) 13(10):2517-2523.
37. HEATH H 3rd: Clinical spectrum of primary hyperparathyroidism: Evolution with changes in medical practice and technology. J. Bone Miner. Res. (1991) 6(Suppl. 2):S63-S70.
38. LEIFSSON BG, AHREN B: Serum calcium and survival in a large health screening program. J. Clin. Endocrinol. Metab. (1996) 81(6):2149-2153.
39. SILVERBERG SJ, BILEZIKIAN JP: Evaluation and management of primary hyperparathyroidism. J. Clin. Endocrinol. Metab. (1996) 81(6):2036-2040.
40. WERMERS RA, KHOSLA S, ATKINSON EJ et al.: The rise and fall of primary hyperparathyroidism: A population-based study in Rochester, Minnesota, 1965-1992. Ann. Intern. Med. (1997) 126(6):433-440.
41. URENA P: Use of calcimimetics in uremic patients with secondary hyperparathyroidism: Review. Artif. Organs (2003) 27(9):759-764.
42. IMANISHI Y, TAHARA H, PALANISAMY N et al.: Clonal chromosomal defects in the molecular pathogenesis of refractory hyperparathyroidism of uremia. J. Am. Soc. Nephrol. (2002) 13(6):1490-1498.
43. BROWN EM, WILSON RE, EASTMAN RC et al.: Abnormal regulation of parathyroid release by calcium in secondary hyperparathyroidism due to chronic renal failure. J. Clin. Endocrinol. Metab. (1982) 54:172-179.
44. ARNOLD A: Molecular mechanisms of parathyroid neoplasia. Endocrinol. Metab. Clin. North Am. (1994) 23(1):93-107.
45. HSI ED, ZUKERBERG LR, YANG WI, ARNOLD A: Cyclin D1/PRAD1 expression in parathyroid adenomas: An immunohistochemical study. J. Clin. Endocrinol. Metab. (1996) 81(5):1736-1739.
46. CHANDRASEKHARAPPA SC, GURU SC, MANICKAM P et al.: Positional cloning of the gene for multiple endocrine neoplasia-type 1. Science (1997) 276(5311):404-407.
47. HEPPNER C, KESTER MB, AGARWAL SK et al.: Somatic mutation of the MEN1 gene in parathyroid tumours. Nat. Genet. (1997) 16(4):375-378.
48. CRYNS VL, YI SM, TAHARA H et al.: Frequent loss of chromosome arm 1p DNA in parathyroid adenomas. Genes Chromosomes Cancer (1995) 13(1):9-17.
49. 2+)-sensing receptor gene in human parathyroid tumors. J. Clin. Endocrinol. Metab. (1995) 80(11 ):3107-3110.
50. FALCHETTI A, BECHERINI L, MARTINETI V et al.: Telomerase repeat amplification protocol (TRAP): A new molecular marker for parathyroid carcinoma. Biochem. Biophys. Res. Commun. (1999) 265(1):252-255.
51. MARX SJ: Familial hypocalciuric hypercalcemia. N. Engl. J. Med (1980) 303:810-811.
52. MARX SJ, FRASER D, RAPOPORT A: Familial hypocalciuric hypercalcemia: Mild expression of the gene in heterozygotes and severe expression in homozygotes. Am. J. Med. (1985) 78:15-22.
53. CARLING T, SZABO E, BAI M et al.: Familial hypercalcemia and hypercalciuria caused by a novel mutation in the cytoplasmic tail of the calcium receptor. J. Clin. Endocrinol. Metab. (2000) 85(5):2042-2047.
54. 2+-sensing receptor gene mutation. Nat. Genet. (1994) 8:303-307.
55. FINEGOLD DN, ARMITAGE MM, GALIANI M et al.: Preliminary localization of a gene for autosomal dominant hypoparathyroidism to chromosome 3q13. Pediatr. Res. (1994) 36:414-417.
56. PERRY YM, FINEGOLD DM, ARMITAGE MM et al.: A missense mutation in the Ca-sensing receptor gene causes familial autosomal dominant hypoparathyroidism. Am. J. Hum. Genet. (1994) 55:(Suppl.) (Abstract 17)
57. CHATTOPADHYAY N, MITHAL A, BROWN EM: The calcium-sensing receptor: A window into physiology and pathophysiology of mineral ion metabolism. Endocr. Rev. (1996) 17:289-307.
58. BROWN E: Mutations in the calcium-sensing receptor and their clinical implications. Horm. Res. (1997) 48:199-208.
59. MARX SJ, AGARWAL SK, KESTER MB et al.: Germline and somatic mutation of the gene for multiple endocrine neoplasia Type 1 (MEN1). J. Intern. Med. (1998) 243(6):447-453.
60. FARNEBO F, TEH BT, KYTOLA S et al.: Alterations of the MEN1 gene in sporadic parathyroid tumors. J. Clin. Endocrinol. Metab. (1998) 83(8):2627-2630.
61. BROWN EM: The pathophysiology of primary hyperparathyroidism. J. Bone Miner. Res. (2002) 17(Suppl.2):N24-N29.
62. YANO S, SUGIMOTO T, TSUKAMOTO T et al.: Association of decreased calcium-sensing receptor expression with proliferation of parathyroid cells in secondary hyperparathyroidism. Kidney Int. (2000) 58(5):1980-1986.
63. BROWN AJ, RITTER CS, FINCH JL, SLATOPOLSKY EA: Decreased calcium-sensing receptor expression in hyperplastic parathyroid glands of uremic rats: Role of dietary phosphate. Kidney Int. (1999) 55(4):1284-1292.
64. YANO S, SUGIMOTO T, TSUKAMOTO T et al.: Decrease in vitamin D receptor and calcium-sensing receptor in highly proliferative parathyroid adenomas. Eur. J. Endocrinol. (2003) 148(4):403-411.
65. LLACH F: Hyperphosphatemia in end-stage renal disease patients: Pathophysiological consequences. Kidney Int. (1999) 73:S31-S37.
66. SLATOPOLSKY E, DUSSO A, BROWN AJ: The role of phosphorus in the development of secondary hyperparathyroidism and parathyroid cell proliferation in chronic renal failure. Am. J. Med. Sci. (1999) 317(6):370-376.
67. LJUNGHALL S, HELLMAN P, RASTAD J, AKERSTROM G: Primary hyperparathyroidism: Epidemiology, diagnosis and clinical picture. World J. Surg. (1991) 15(6):681-687.
68. THOMPSON NW: Multiple endocrine neoplasia Type I. Surgical therapy. Cancer Treat. Res. (1997) 89:407-419.
69. HOOGHE L, KINNAERT P: Secondary hyperparathyroidism and parathyroid autotransplantation. Acta Chir. Belg. (1994) 94(5):297-298.
70. NUSSBAUM SR, THOMPSON AR, HUTCHESON KA, GAZ RD, WANG CA: Intraoperative measurement of parathyroid hormone in the surgical management of hyperparathyroidism. Surgery. (1988) 104(6):1121-1127.
71. DAVIES C, DEMEURE MJ, ST JOHN A, EDIS AJ: Study of intact (1-84) parathyroid hormone secretion in patients undergoing parathyroidectomy. World J. Surg. (1990) 14(3):355-359.
72. BERGENFELZ A, NORDEN NE, AHREN B: Intraoperative fall in plasma levels of intact parathyroid hormone after removal of one enlarged parathyroid gland in hyperparathyroid patients. Eur. J. Surg. (1991) 157(2):109-112.
73. RYAN MF, JONES SR, BARNES AD: Clinical evaluation of a rapid parathyroid hormone assay. Ann. Clin. Biochem. (1992) 29(1):48-51.
74. DUQUENNE M, WERYHA G, KAMINSKY P et al.: Serum parathormone profile during surgical treatment of hyperfunctioning parathyroid adenoma: A multicompartmental model. J. Bone Miner. Res. (1994) 9(9):1371-1375.
75. LOCCHI F, TOMMASI M, BRANDI ML et al.: The importance of the unsuppressed glands in the study of intact parathyroid hormone disappearance after parathyroid adenomectomy. Eur. J. Endocrinol. (2001) 144(4):353-362.
76. LEVIN KE, CLARK OH: The reasons for failure in parathyroid operations. Arch. Surg. (1989) 124(8):911-914.
77. LUMB GA, STANBURY SW: Parathyroid function in human vitamin D deficiency and vitamin D deficiency in primary hyperparathyroidism. Am. J. Med. (1974) 56(6):833-839.
78. CARROLL MF, SCHADE DS: A practical approach to hypercalcemia. Am. Fam. Physician (2003) 67(9):1959-1966.
79. REASNER CA, STONE MD, HOSKING DJ et al.: Acute changes in calcium homeostasis during treatment of primary hyperparathyroidism with risedronate. J. Clin. Endocrinol. Metab. (1993) 77(4):1067-1071.
80. ROSSINI M, GATTI D, ISAIA G et al.: Effects of oral alendronate in elderly patients with osteoporosis and mild primary hyperparathyroidism. J. Bone Miner. Res. (2001) 16(1):113-119.
81. KHAN AA, BILEZIKIAN JP, KUNG AWC et al.: A double blind randomized placebo controlled trial of alendronate in primary hyperparathyroidism. J. Bone Mineral Res. (2001) 16(Suppl. 1):S226.
82. HASSANI S, BRAUNSTEIN GD, SEIBEL MJ et al.: Alendronate therapy of primary hyperparathyroidism. Endocrinologist (2001) 11:459-464.
83. SELBY PL, PEACOCK M: Ethinyl estradiol and norethindrone in the treatment of primary hyperparathyroidism in postmenopausal women. N. Engl. J. Med. (1986) 314(23):1481-1485.
84. MARCUS R: Estrogens and progestins in the management of primari hyperparathyroidism. J. Bone Mineral Res. (1991) 16(Suppl. 2):S125-S129.
85. ARNOLD A, BROWN EM, URENA P et al.: Monoclonality of parathyroid tumors in chronic renal failure. J. Clin. Invest. (1995) 95:2047-2053.
86. DRUEKE TB: Parathyroid gland hyperplasia in uremia. Kidney Int. (2001) 59:1182-1183.
87. 3 receptor density is associated with a more severe form of parathyroid hyperplasia in chronic uremic patients. J. Clin. Invest. (1993) 92:1436-1443.
88. GOGUSEV J, DUCHAMBON P, HORY B et al.: Depressed expression of calcium receptor in parathyroid gland tissue of patients with hyperparathyroidism. Kidney Int. (1997) 51:328-336.
89. 3 in the parathyroid in vivo. J. Clin. Invest. (1990) 86:1968-1975.
90. SZABO A, MERKE J, BEIER E et al.: 1,25(OH)2 vitamin D3 inhibits parathyroid cell proliferation in experimental uremia. Kidney Int. (1989) 35:1049-1056.
91. LOGHMAN-ADHAM M: Safety of new phosphate binders for chronic renal failure. Drug Saf. (2003) 26(15):1093-1115.
92. SLATOPOLSKY E, WEERTS C, NORWOOD K et al.: Long-term effects of calcium carbonate and 2.5 mEq/liter calcium dialysate on mineral metabolism. Kidney Int. (1989) 36(5):897-903.
93. INDRIDASON OS, QUARLES LD: Comparison of treatments for mild secondary hyperparathyroidism in hemodialysis patients. Durham Renal Osteodystrophy Study Group. Kidney Int. (2000) 57(1):282-292.
94. RUDNICKI M, HOJSTED J, PETERSEN LJ et al.: Oral calcium effectively reduces parathyroid hormone levels in hemodialysis patients. Nephron (1993) 65:369-374.
95. HSU CH: Are we mismanaging calcium and phosphate metabolism in renal failure? Am. J. Kidney Dis. (1997) 29(4):641-649.
96. CUNNINGHAM J: What is the optimal regimen for vitamin D? Kidney Int. (1999) 56:S59-S64.
97. QUARLES LD, YOHAY DA, CARROLL BA et al.: Prospective trial of pulse oral versus intravenous calcitriol treatment of hyperparathyroidism in ESRD. Kidney Int. (1994) 45(6):1710-1721.
98. GOODMAN WG, RAMIREZ JA, BELIN TR et al.: Development of adynamic bone in patients with secondary hyperparathyroidism after intermittent calcitriol therapy. Kidney Int. (1994) 46(4):1160-1166.
99. BLOCK GA, PORT FK: Re-evaluation of risks associated with hyperphosphatemia and hyperparathyroidism in dialysis patients: recommendations for a change in management. Am. J. Kidney Dis. (2000) 35(6):1226-1237.
100. BLOCK GA, HULBERT-SHEARON TE, LEVIN NW, PORT FK: Association of serum phosphorus and calcium x phosphate product with mortality risk in chronic hemodialysis patients: A national study. Am. J. Kidney Dis. (1998) 31(4):607-617.
101. GANESH SK, STACK AG, LEVIN NW et al.: Association of elevated serum PO(4), Ca x PO(4) product, and parathyroid hormone with cardiac mortality risk in chronic hemodialysis patients. J. Am. Soc. Nephrol. (2001) 12(10):2131-2138.
102. GUERIN AP, LONDON GM, MARCHAIS SJ, METIVIER F: Arterial stiffening and vascular calcifications in end-stage renal disease. Nephrol. Dial. Transplant. (2000) 15(7):1014-1021.
103. GOODMAN WG, GOLDIN J, KUIZON BD et al. Coronary-artery calcification in young adults with end-stage renal disease who are undergoing dialysis. N. Engl. J. Med. (2000) 342(20):1478-1483.
104. CHERTOW GM, BURKE SK, RAGGI P: Sevelamer attenuates the progression of coronary and aortic calcification in hemodialysis patients. Kidney Int. (2002) 62(1):245-252.
105. GOODMAN WG, RAMIREZ JA, BELIN TR et al.: Development of adynamic bone in patients with secondary hyperparathyroidism after intermittent calcitriol therapy. Kidney Int. (1994) 46(4):1160-1166.
106. INDRIDASON OS, QUARLES LD: Prevention and management of renal osteodystrophy in dialysis patients. In: Renal Osteodystrophy. Bushinski DA (Ed.), Philadelphia, Lippincott-Raven, Philadelphia, PA, USA (1997):445-472.
107. FLORIO T, YAO H, CAREY KD et al.: Somatostatin activation of mitogen-activated protein kinase via somatostatin receptor 1 (SSTR1). Mol. Endocrinol. (1999) 13(1):24-37.
108. ALDERTON F, HUMPHREY PP, SELLERS LA: High-intensity p38 kinase activity is critical for p21 (cip1) induction and the antiproliferative function of G(i) protein-coupled receptors. Mol. Pharmacol. (2001) 59(5):1119-1128.
109. SAKAGUCHI K: Acidic fibroblast growth factor autocrine system as a mediator of calcium-regulated parathyroid cell growth. J. Biol. Chem. (1992) 267(34):24554-24562.
110. KANESAKA Y, TOKUNAGA H, IWASHITA K et al.: Endothelin receptor antagonist prevents parathyroid cell proliferation of low calcium diet-induced. hyperparathyroidism in rats. Endocrinology (2001) 142(1):407-413.
111. MATSUSHITA H, HARA M, ENDO Y et al.: Proliferation of parathyroid cells negatively correlates with expression of parathyroid hormone-related protein in secondary parathyroid hyperplasia. Kidney Int. (1999) 55(1):130-138.
112. COZZOLINO M, LU Y, FINCH J et al.: P21WAF1 and TGF-α mediate parathyroid growth arrest by vitamin D and high calcium. Kidney Int. (2001) 60(6):2109-2117.
113. WADA M, NAGANO N: Control of parathyroid cell growth by calcimimetics. Nephrol, Dial. Transplant. (2003) 18(Suppl. 3):iIi13-iii17.
114. COHEN A, TILVERBERG SJ: Calcimimetics: therapeutic potential in hyperparathyroidism. Curr. Opin. Pharmacol. (2002) 2(6):734-739.
115. NEMETH EF, STEFFEY ME, FOX J: The parathyroid calcium receptor: A novel therapeutic target for treating hyperparathyroidism. Pediatr. Nephrol. (1996) 10(3):275-279.
116. 2+ receptor. J. Biol. Chem. (2002) 277(21):18908-18913.
117. NEMETH EF, STEFFEY ME, HAMMERLAND LG et al.: Calcimimetics with potent and selective activity on the parathyroid calcium receptor. Proc. Natl. Acad. Sci. USA (1998) 95(7):4040-4045.
118. 2+ receptor expressed in Xenopus laevis oocytes by NPS 467 or NPS 568. Mol. Pharmacol. (1998) 53(6):1083-1088.
119. OTT SM: Calcimimetics - new drugs with the potential to control hyperparathyroidism. J. Clin. Endocrinol. Metab. (1998) 83(4):1080-1082.
120. MIEDLICH S, GAMA L, BREITWIESER GE: Calcium sensing receptor activation by a calcimimetic suggests a link between cooperativity and intracellular calcium oscillations. J. Biol. Chem. (2002) 277(51):49691-49699.
121. ZHANG Z, JIANG Y, QUINN SJ et al.: L-phenylalanine and NPS R-467 synergistically potentiate the function of the extracellular calcium-sensing receptor through distinct sites. J. Biol. Chem. (2002) 277(37):33736-33741.
122. LI YC, AMLING M, PIRRO AE et al.: Normalization of mineral ion homeostasis by dietary means prevents hyperparathyroidism, rickets, and osteomalacia, but not alopecia in vitamin D receptor-ablated mice. Endocrinology (1998) 139(10): 4391-4396.
123. WADA M, NAGANO N, FURUYA Y et al.: Calcimimetic NPS R-568 prevents parathyroid hyperplasia in rats with severe secondary hyperparathyroidism. Kidney Int. (2000) 57(1):50-58.
124. ANTONSEN JE, SHERRARD DJ, ANDRESS DL: A calcimimetic agent acutely suppresses parathyroid hormone levels in patients with chronic renal failure. Rapid communication. Kidney Int. (1998) 53(1):223-227.
125. NEMETH EF: Calcium receptors as novel drug targets, In: Principles of Bone Biology (1st edn), Bilezikian JP, Raisz LG, Rodan GA (Eds). San Diego, CA, USA Academic Press (1996):1019-1035.
126. COBURN JW, BARRI T, TURNER SA et al.: Single doses of the calcimimetic AMG 073 reduce parathyroid hormone levels in a dose dependent manner in hemodialysis patients with secondary hyperparathyroidism. J. Am. Soc. Nephrol. (2000) 11:573.
127. GOODMAN WG, TURNER SA, BLAISDELL PW et al.: Multiple doses of the calcimimetic AMG 073 reduce parathyroid hormone levels in a dose dependent manner in hemodialysis patients with secondary hyperparathyroidism. J. Am. Soc. Nephrol, (2000) 11:576.
128. LINDBERG JS, MOE SM, GOODMAN WG et al.: The calcimimetic AMG 073 reduce parathyroid hormone (PTH), phosphorus, and calcium x phosphorus product in patients with ESRD and secondary hyperparathyroidism. J. Am. Soc. Nephrol. (2000) 11:578A.
129. STEFFEY ME, FOX J, VANWAGENEN BC et al.: Calcimimetics: structurally and mechanistically novel compounds that inhibit hormone secretion from parathyroid cells. J. Bone Mineral Res. (1993) 8(Suppl. 1):S175.
130. FOX JA LOWE SH, PETTY BA, NEMETH EF: 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. (1999) 290(2):473-479.
131. FOX J, LOWE SH, CONKLIN RL et al.: Calcimimetic compound NPS R-568 stimulates calcitonin secretion but selectively targets parathyroid gland Ca(2+) receptor in rats. J. Pharmacol. Exp. Ther. (1999) 290(2):480-486.
132. WADA M, FURUYA Y, SAKIYAMA J et al.: The calcimimetic compound NPS R-568 suppresses parathyroid cell proliferation in rats with renal insufficiency. Control of parathyroid cell growth via a calcium receptor. J. Clin. Invest. (1997) 100(12):2977-2983.
133. CHIN J, MILLER SC, WADA M et al.: Activation of the calcium receptor by a calcimimetic compound halts the progression of secondary hyperparathyroidism in uremic rats. J. Am. Soc. Nephrol. (2000) 11(5):903-911.
134. WADA M, ISHII H, FURUYA Y et al.: NPS R-568 halts or reverses osteitis fibrosa in uremic rats. Kidney Int. (1998) 53(2):448-453.
135. ISHII H, WADA M, FURUYA Y et al.: Daily intermittent decreases in serum levels of parathyroid hormone have an anabolic-like action on the bones of uremic rats with low-turnover bone and osteomalacia. Bone (2000) 26(2):175-182.
136. HEATH HI, SANGUINETTI EL, OGELSBY S, MARRIOTT TB: Inhibition of human parathyroid hormone secretion in vivo by NPS R-568, a calcimimetic drug that targets the parathyroid cell-surface calcium receptor. Bone (1995) 16:85S.
137. SILVERBERG SJ, BONE HG 3rd, MARRIOTT TB et al.: Short-term inhibition of parathyroid hormone secretion by a calcium-receptor agonist in patients with primary hyperparathyroidism. N. Engl. J. Med. (1997) 337(21):1506-1510.
138. AKIZAWA T, SUZUKI M, TOMINAGA Y et al.: Acute effects of calcimimetic agent (CA) on hemodialysis (HD) patients with secondary hyperparathyroidism (2HPT). Am. J. Soc. Nephrol. (1998) 9:561 (Abstract).
139. GOODMAN WG, FRAZAO JM, GOODKIN DA et al.: A calcimimetic agent lowers plasma parathyroid hormone levels in patients with secondary hyperparathyroidism. Kidney Int. (2000) 58(1):436-445.
140. GOODMAN WG: Recent developments in the management of secondary hyperparathyroidism. Kidney Int. (2001) 59(3):1187-1201.
141. COBURN JW, MAUNG HM: Calcimimetic agents and the calcium-sensing receptor. Curr. Opin. Nephrol. Hypertens. (2000) 9(2):123-132.
142. FRANCESCHIAI N, JOY MS, KSHIRSAGAR A: Cinacalcet HCl: a calcimimetic agent for the management of primary and secondary hyperparathyroidism. Expert Opin. Investig. Drugs (2003) 12(8):1413-1421.
143. RACKE FK, NEMETH EF: Protein kinase C modulates hormone secretion regulated by extracellular polycations in bovine parathyroid cells. J. Physiol. (1993) 468:163-176.
144. RACKE FK, NEMETH EF: Cytosolic calcium homeostasis in bovine parathyroid cells and its modulation by protein kinase C. J. Physiol. (1993) 468:141-162.
145. NEMETH EF, HEATON WH, MILLER M et al.: Pharmacodynamics of the Type II Calcimimetic Compound, Cinacalcet HCl. J. Pharmacol. Exp. Ther. (2003) 308(2):627-635.
146. SHOBACK DM, FIREK AF, MIMS RB et al.: An evaluation of the calcimimetic AMG 073 in patients with hypercalcemia and primary hyperparathyroidism (PHPT). J. Bone Mineral Res. (2001) 16(Suppl. 1):S503.
147. PEACOCK M, SHOBACK DM, GRETH E et al.: The calcimimetic AMG-073 reduces serum calcium (Ca) in patients with primary hyperparathyroidism. J. Bone Mineral Res. (2001) 16(Suppl. 1):S163.
148. LINDBERG JS, MOE SM, GOODMAN WG et al.: The calcimimetic AMG 073 reduces parathyroid hormone and calcium x phosphorus in secondary hyperparathyroidism. Kidney Int. (2003) 63(1):248-254.
149. QUARLES LD, SHERRARD, DJ, ADLER S et al.: The calcimimetic AMG 073 as a potential treatment for secondary hyperparathyroidism of end-stage renal disease. J. Am. Soc. Nephrol. (2003) 14(3):575-583.
150. GOODMAN WG, HLADIK GA, TURNER SA et al.: The calcimimetic agent AMG 073 lowers plasma parathyroid hormone levels in hemodialysis patients with secondary hyperparathyroidism. J. Am. Soc. Nephrol. (2002) 13(4):1017-1024.
151. BLOCK GA, COYNE DW, GOODMAN WG et al.: The calcimimetic AMG 073: A potential novel therapy for secondary hyperparathyroidism (SHPT). J. Am. Soc. Nephrol. (2002) 13:572A.
152. QUARLES LD, SPIEGEL DM, CURZI M et al.: The effect of one-year treatment with the calcimimetic AMG 073 on bone health in ESRD patients with secondary hyperparathyroidism (SHPT). J. Am. Soc. Nephrol. (2002) 13:572A-573A.
153. MOE SM, SPRAGUE SM, ADLER S et al.: Two-years treatment with the calcimimetic AMG 073 in hemodialysis patients with secondary hyperparathyroidism (SHPT). J. Am. Soc. Nephrol. (2002) 13:572A.
154. DRUEKE T, CUNNINGAM J, GOODMAN WG et al.: Short-term treatment of secondary hyperparathyroidism (SHPT) with the calcimimetic agent AMG 073. J. Am. Soc. Nephrol.(2001) 12:764A.
155. COLLINS MT, SKARULIS MC, BILEZIKIAN JP et al.: Treatment of hypercalcemia secondary to parathyroid carcinoma with a novel calcimimetic agent. J. Clin. Endocrinol. Metab. (1998) 83(4):1083-1088.
156. PEACOCK M: Normalization of hypercalcemia with the calcimimetic AMG 073 in a patient with metastatic parathyroid cancer. J. Bone Mineral Res. (2002) 17:S381.
157. SILVERBERG SJ, FAIMAN C, BILEZIKIAN JP et al.: The effects of cinacalcet HCl (AMG 073) on serum calcium levels in patients with parathyroid carcinoma or recurrent primary HPT after PTX. J. Bone Mineral Res. (2003) 18(Suppl. 1):S171.
158. RUBIN M, SLINEY J, McCARY LC et al.: Effective management of severe hypercalcemia with the calcimimetic cinacalcet HCl in patients with parathyroid carcinoma. J. Bone Mineral Res. (2003) 18(Suppl. 2):S392.
159. URENA P: Parathyroid gland, calcium receptor and calcimimetics. Nephrologie (2002) 23(4):151-164.
160. OLGAARD K, LEWIN E: Prevention of uremic bone disease using calcimimetic compounds. Ann. Rev Med. (2001) 52:203-220.
161. QUARLES LD, SHERRARD DJ, ADLER S et al.: The calcimimetic AMG 073 reduces PTH and Ca x P in patients with secondary hyperparathyroidism (SHPT). J. Am. Soc. Nephrol. (2001) 12:771A.
162. WADA M, NAGANO N, FURUYA Y et al.: Calcimimetic NPS R-568 prevents parathyroid hyperplasia in rats with severe secondary hyperparathyroidism. Kidney Int. (2000) 57(1):50-58.
163. URENA P, FRAZAORJM: Calcimimetic agents: review and perspectives. Kidney Int. (2003) 85:S91-S96.
164. DREWS J: DAug discovery: a historical perspective. Science (2000) 287(5460):1960-1964.
165. MA P, ZEMMEL R: Value of novelty? Nat. Rev. Drug Discov. (2002) 1(8):571-572.
166. FANG Y, LAHIRI J, PICARD L: G protein-coupled receptor microarrays for drug discovery. Drug Discovery (2003) 8(16):755-761.