Biasing the parathyroid hormone receptor: Relating in vitro ligand efficacy to in vivo biological activity

Methods in Enzymology

Volumn 522, Issue , 2013, Pages 229-262

  Appleton, Kathryn M ^a,b   Lee, Mi Hye ^a   Alele, Christian ^a   Alele, Christine ^a   Luttrell, Deirdre K ^a   Peterson, Yuri K ^b   Morinelli, Thomas A ^a,c   Luttrell, Louis M ^a,c  

^a MEDICAL UNIVERSITY OF SOUTH CAROLINA   (United States)

^b MEDICAL UNIVERSITY OF SOUTH CAROLINA   (United States)

^c RALPH H JOHNSON VA MEDICAL CENTER   (United States)

Author keywords

arrestin; biased agonism; G protein coupled receptor; parathyroid hormone; pharmacology

Indexed keywords

CYCLIC AMP; G PROTEIN COUPLED RECEPTOR; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 3; PARATHYROID HORMONE RECEPTOR 1;

ARTICLE; BONE MASS; CALCIUM SIGNALING; CALCIUM TRANSPORT; CELL CULTURE; CELL STRAIN HEK293; GENETIC TRANSFECTION; HUMAN; IN VITRO STUDY; IN VIVO STUDY; INVERSE AGONISM; LUMINESCENCE; MEASUREMENT; NONHUMAN; PREDICTION; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN EXPRESSION; TRANSIENT TRANSFECTION;

EID: 84873326843     PISSN: 00766879     EISSN: 15577988     Source Type: Book Series    
DOI: 10.1016/B978-0-12-407865-9.00013-3     Document Type: Chapter

References (56)

1. A.B. Abou-Samra, H. Jüppner, T. Force, M.W. Freeman, X.F. Kong, and E. Schipani Expression cloning of a common receptor for parathyroid hormone and parathyroid hormone-related peptide from rat osteoblast-like cells: A single receptor stimulates intracellular accumulation of both cAMP and inositol trisphosphates and increases intracellular free calcium Proceedings of the National Academy of Sciences of the United States of America 89 1992 2732 2736
2. S. Ahn, S.K. Shenoy, H. Wei, and R.J. Lefkowitz Differential kinetic and spatial patterns of beta-arrestin and G protein-mediated ERK activation by the angiotensin II receptor The Journal of Biological Chemistry 279 2004 35518 35525
3. J.R. Barbier, T.J. Gardella, T. Dean, S. MacLean, Z. Potetinova, and J.F. Whitfield Backbone-methylated analogues of the principle receptor binding region of human parathyroid hormone. Evidence for binding to both the N-terminal extracellular domain and extracellular loop region The Journal of Biological Chemistry 280 2005 23771 23777
4. K.A. Berg, S. Maayani, J. Goldfarb, C. Scaramellini, P. Leff, and W.P. Clarke Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: Evidence for agonist-directed trafficking of receptor stimulus Molecular Pharmacology 54 1998 94 104
5. B.F. Binkowski, F. Fan, and K.V. Wood Luminescent biosensors for real-time monitoring of intracellular cAMP Methods in Molecular Biology 756 2011 263 271
6. A. Bisello, M.J. Horwitz, and A.F. Stewart Parathyroid hormone-related protein: An essential physiological regulator of adult bone mass Endocrinology 145 2004 3551 3553
7. J.W. Black, and P. Leff Operational models of pharmacological agonist Proceedings of the Royal Society London B Biological Sciences 220 1983 141 162
8. M.L. Bouxsein, D.D. Pierroz, V. Glatt, D.S. Goddard, F. Cavat, and R. Rizzoli Beta-arrestin2 regulates the differential response of cortical and trabecular bone to intermittent PTH in female mice Journal of Bone and Mineral Research 20 2005 635 643
9. F.R. Bringhurst, H. Juppner, J. Guo, P. Urena, J.T. Potts Jr., and H.M. Kronenberg Cloned, stably expressed parathyroid hormone (PTH)/PTH-related peptide receptors activate multiple messenger signals and biological responses in LLC-PK1 kidney cells Endocrinology 132 1993 2090 2098
10. H. Dobnig, and R.T. Turner Evidence that intermittent treatment with parathyroid hormone increases bone formation in adult rats by activation of bone lining cells Endocrinology 136 1995 3632 3638
11. F.J. Ehlert Ternary complex model A. Christopolous, Biomedical applications of computer modeling 2000 CRC Press Boca Raton 21 85
12. S.L. Ferrari, V. Behar, M. Chorev, M. Rosenblatt, and A. Bisello Endocytosis of ligand-human parathyroid hormone receptor 1 complexes is protein kinase C-dependent and involves beta-arrestin2. Real-time monitoring by fluorescence microscopy The Journal of Biological Chemistry 274 1999 29968 29975
13. S.L. Ferrari, D.D. Pierroz, V. Glatt, D.S. Goddard, E.N. Bianchi, and F.T. Lin Bone response to intermittent parathyroid hormone is altered in mice null for beta-arrestin2 Endocrinology 146 2005 1854 1862
14. K.W. Figueroa, M.T. Griffin, and F.J. Ehlert Selectivity of agonists for the active state of M1 to M4 muscarinic receptor subtypes The Journal of Pharmacology and Experimental Therapeutics 328 2009 331 342
15. S. Galandrin, and M. Bouvier Distinct signaling profiles of beta1 and beta2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy Molecular Pharmacology 70 2006 1575 1584
16. T.J. Gardella, M.D. Luck, G.S. Jensen, E. Schipani, J.T. Potts Jr., and H. Juppner Inverse agonism of amino-terminally truncated parathyroid hormone (PTH) and PTH-related peptide (PTHrP) analogs revealed with constitutively active mutant PTH/PTHrP receptors Endocrinology 137 1996 3936 3941
17. D. Gesty-Palmer, M. Chen, E. Reiter, S. Ahn, C.D. Nelson, and S. Wang Distinct conformations of the parathyroid hormone receptor mediate G protein and beta-arrestin dependent activation of ERK1/2 The Journal of Biological Chemistry 281 2006 10856 10864
18. D. Gesty-Palmer, P. Flannery, L. Yuan, L. Corsino, R. Spurney, and R.J. Lefkowitz A beta-Arrestin biased agonist of the parathyroid hormone receptor (PTH1R) promotes bone formation independent of G protein activation Science Translational Medicine 1 2009 1ra1
19. D. Gesty-Palmer, and L.M. Luttrell 'Biasing' the parathyroid hormone receptor: A novel anabolic approach to increasing bone mass? British Journal of Pharmacology 164 2011 59 67
20. K.J. Gregory, N.E. Hall, A.B. Tobin, P.M. Sexton, and A. Christopoulos Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias The Journal of Biological Chemistry 285 2010 7459 7474
21. M.T. Griffin, K.W. Figueroa, S. Liller, and F.J. Ehlert Estimation of agonist activity at G protein-coupled receptors: Analysis of M2 muscarinic receptor signaling through Gi/o, Gs, and G15 The Journal of Pharmacology and Experimental Therapeutics 321 2007 1193 1207
22. S. Hilliker, J.E. Wergedal, H.E. Gruber, P. Bettica, and D.J. Baylink Truncation of the amino terminus of PTH alters its anabolic activity on bone in vivo Bone 19 1996 469 477
23. S.R. Hoare, and T.B. Usdin Tuberoinfundibular peptide (7-39) [TIP(7-39)], a novel, selective, high-affinity antagonist for the parathyroid hormone-1 receptor with no detectable agonist activity The Journal of Pharmacology and Experimental Therapeutics 295 2000 761 770
24. J.M. Hock, and I. Gera Effects of continuous and intermittent administration and inhibition of resorption on the anabolic response of bone to parathyroid hormone Journal of Bone and Mineral Research 7 1992 65 72
25. H. Jouishomme, J.F. Whitfield, B. Chakravarthy, J.P. Durkin, L. Gagnon, and R.J. Isaacs The protein kinase-C activation domain of the parathyroid hormone Endocrinology 130 1992 53 60
26. H. Jouishomme, J.F. Whitfield, L. Gagnon, S. MacLean, R. Isaacs, and B. Chakravarthy Further definition of the protein kinase C activation domain of the parathyroid hormone Journal of Bone and Mineral Research 9 1994 943 949
27. H. Jüppner, A.B. Abou-Samra, M. Freeman, X.F. Kong, E. Schipani, and J. Richards A G protein-linked receptor for parathyroid hormone and parathyroid hormone-related peptide Science 254 1991 1024 1026
28. A. Karlin On the application of "a plausible model" of allosteric proteins to the receptor for acetylcholine Journal of Theoretical Biology 16 1967 306 320
29. T. Kenakin Agonist-receptor efficacy. II. Agonist-trafficking of receptor signals Trends in Pharmacological Sciences 16 1995 232 238
30. T.P. Kenakin 7TM receptor allostery: Putting numbers to shapeshifting proteins Trends in Pharmacological Sciences 30 2009 460 469
31. T. Kenakin, and L.E. Miller Seven transmembrane receptors as shapeshifting proteins: The impact of allosteric modulation and functional selectivity on new drug discovery Pharmacological Reviews 62 2010 265 304
32. E.D. Lederer, S.S. Sohi, and K.R. McLeish Parathyroid hormone stimulates extracellular signal-regulated kinase (ERK) activity through two independent signal transduction pathways: Role of ERK in sodium-phosphate cotransport Journal of American Society of Nephrology 11 2000 222 231
33. M.H. Lee, H.M. EI-Shewy, D.K. Luttrell, and L.M. Luttrell Role of beta-arrestin-mediated desensitization and signaling in the control of angiotensin AT1a receptor-stimulated transcription Journal of Biological Chemistry 283 2008 2088 2097
34. L.M. Luttrell, and D. Gesty-Palmer Beyond desensitization: Physiological relevance of arrestin-dependent signaling Pharmacological Reviews 62 2010 305 330
35. L.M. Luttrell, and T.P. Kenakin Refining efficacy: Allosterism and bias in G protein-coupled receptor signaling Methods in Molecular Biology 756 2011 3 35
36. M.J. Mahon, M. Donowitz, C.C. Yun, and G.V. Segre Na(+)/H(+) exchanger regulatory factor 2 directs parathyroid hormone 1 receptor signaling Nature 417 2002 858 861
37. S. Mohan, S. Kutilek, C. Zhang, H.G. Shen, Y. Kodama, and A.K. Srivastava Comparison of bone formation responses to parathyroid hormone(1-34), (1-31), and (2-34) in mice Bone 27 2000 471 478
38. J. Nasman, J.P. Kukkonen, S. Ammoun, and K.E. Akerman Role of G-protein availability in differential signaling by a2-adrenoceptors Biochemical Pharmacology 62 2001 913 922
39. S.R. Nussbaum, M. Rosenblatt, and J.T. Potts Jr. Parathyroid hormone - Renal receptor interactions. Demonstration of two receptor-binding domains The Journal of Biological Chemistry 255 1980 10183 10187
40. M. Pines, A.E. Adams, S. Stueckle, R. Bessalle, V. Rashti-Behar, and M. Chorev Generation and characterization of human kidney cell lines stably expressing recombinant human PTH/PTHrP receptor: Lack of interaction with a C-terminal human PTH peptide Endocrinology 135 1994 1713 1716
41. L. Qin, L.J. Raggatt, and N.C. Partridge Parathyroid hormone: A double-edged sword for bone metabolism Trends in Endocrinology and Metabolism 15 2004 60 65
42. S. Rajagopal, S. Ahn, D.H. Rominger, W. Gowen-MacDonald, C.M. Lam, and S.M. Dewire Quantifying ligand bias at seven-transmembrane receptors Molecular Pharmacology 80 2011 367 377
43. S. Rajagopal, K. Rajagopal, and R.J. Lefkowitz Teaching old receptors new tricks: biasing seven-transmembrance receptors Nature Reviews Drug Discovery 9 2010 373 386
44. I. Schmidt, H. Dobnig, and R. Turner Intermittent parathyroid hormone treatment increases osteoblast number, steady state messenger ribonucleic acid levels for osteocalcin, and bone formation in tibial metaphysis of hypophysectomized female rats Endocrinology 136 1995 5127 5134
45. G.V. Segre, M. Rosenblatt, B.L. Reiner, J.E. Mahaffey, and J.T. Potts Jr. Characterization of parathyroid hormone receptors in canine renal cortical plasma membranes using a radioiodinated sulfur-free hormone analogue. Correlation of binding with adenylate cyclase activity The Journal of Biological Chemistry 254 1979 6980 6986
46. W.B. Sneddon, A. Bisello, C.E. Magyar, G.E. Willick, C.A. Syme, and F. Galbiati Ligand-selective dissociation of activation and internalization of the parathyroid hormone receptor. Conditional efficacy of PTH peptide fragments Endocrinology 145 2004 2815 2823
47. A.F. Stewart, R.L. Cain, D.B. Burr, D. Jacob, C.H. Turner, and J.M. Hock Six-month daily administration of parathyroid hormone and parathyroid hormone-related protein peptides to adult ovariectomized rats markedly enhances bone mass and biomechanical properties: A comparison of human parathyroid hormone 1-34, parathyroid hormone-related protein 1-36, and SDZ-parathyroid hormone 893 Journal of Bone and Mineral Research 15 2000 1517 1525
48. H. Takasu, and F.R. Bringhurst Type-1 parathyroid hormone (PTH)/PTH-related peptide (PTHrP) receptors activate phospholipase C in response to carboxyl-truncated analogs of PTH(1-34) Endocrinology 139 1998 4293 4299
49. H. Takasu, T.J. Gardella, M.D. Luck, J.T. Potts, and F.R. Bringhurst Amino-terminal modifications of human parathyroid hormone (PTH) selectively alter phospholipase C signaling via the type 1 PTH receptor: Implications for design of signal-specific PTH ligands Biochemistry 38 1999 13453 13460
50. H. Takasu, J. Guo, and F.R. Bringhurst Dual signaling and ligand selectivity of the human PTH/PTHrP receptor Journal of Bone and Mineral Research 14 1999 11 20
51. C.D. Thron On the analysis of pharmacological experiments in terms of an allosteric receptor model Molecular Pharmacology 9 1973 1 9
52. M.H. Verheijen, and L.H. Defize Parathyroid hormone inhibits mitogen-activated protein kinase activation in osteosarcoma cells via a protein kinase A-dependent pathway Endocrinology 136 1995 3331 3337
53. M.H. Verheijen, M. Karperien, U. Chung, M. van Wijuen, H. Heystek, and J.A. Hendriks Parathyroid hormone-related peptide (PTHrP) induces parietal endoderm formation exclusively via the type I PTH/PTHrP receptor Mechanisms of Development 81 1999 151 161
54. J.F. Whitfield, and P. Morley Small bone-building fragments of parathyroid hormone: New therapeutic agents for osteoporosis Trends in Pharmacological Sciences 16 1995 382 386
55. X. Zhu, S. Gilbert, M. Birnbaumer, and L. Birnbaumer Dual signaling potential is common among Gs-coupled receptors and dependent on receptor density Molecular Pharmacology 46 1994 460 469
56. B. Zimmerman, M. Simaan, M.-H. Lee, L.M. Luttrell, and S.A. Laporte c-Src-mediated phosphorylation of AP-2 reveals a general mechanism for receptors internalizing through the clathrin pathway Cellular Signalling 21 2009 103 110