Identification and characterization of novel somatostatin antagonists

Molecular Pharmacology

Volumn 50, Issue 4, 1996, Pages 709-715

  Bass, Roy T ^a   Buckwalter, Brian L ^a   Patel, Bomi P ^a   Pausch, Mark H ^a   Price, Laura A ^a   Strnad, Joann ^a   Hadcock, John R ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYL 4 NITROPHENYL CYCLO(DEXTRO CYSTEINYLTYROSYL DEXTRO TRYPTOPHANYLLYSYLTHREONYLCYSTEINYL) DEXTRO TYROSINAMIDE; HORMONE RECEPTOR BLOCKING AGENT; RECEPTOR SUBTYPE; SOMATOSTATIN; SOMATOSTATIN RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING COMPETITION; CONTROLLED STUDY; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HUMAN; HUMAN CELL; MOLECULAR CLONING; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; RECEPTOR AFFINITY; RECEPTOR BLOCKING;

AMINO ACID SEQUENCE; ANIMALS; BINDING, COMPETITIVE; CYCLIC AMP; IODINE RADIOISOTOPES; PEPTIDES; RADIOLIGAND ASSAY; RATS; RECEPTORS, SOMATOSTATIN; SACCHAROMYCES CEREVISIAE; SOMATOSTATIN;

EID: 0029859983     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (40)

1. Brazeau, P., W. Vale, R. Burgus, N. Ling, M. Butcher, J. Rivier, and R. Guillemin, R. Hypothalamic polypeptide that inhibits the secretion of immunoreactive pituitary growth hormone. Science (Washington, D. C.) 129:77-79 (1973).
2. Reisine, T., and G. I. Bell. Molecular biology of somatostatin receptors. Trends Neurosci. 16:34-38 (1993).
3. Bruno, J. F., Y. Xu, J. Song, and M. Berelowitz. Molecular cloning and functional expression of a brain-specific somatostatin receptor. Proc. Natl. Acad. Sci. USA 89:11151-11155 (1992).
4. Kluxen, F.-W., C. Bruns, and H. Lubbert. Expression cloning of a rat brain somatostatin receptor. Proc. Natl. Acad. Sci. USA 89:4618-4622 (1992).
5. Li, X.-J., M. Forte, R. A. North, C. A. Ross, and S. H. Snyder. Cloning and expression of a rat somatostatin receptor enriched in the brain. J. Biol. Chem. 267:21307-21312 (1992).
6. Meyerhof, W., H.-J. Paust, C. Schonrock, and D. Richter. Cloning of a cDNA encoding putative G protein-coupled receptor expressed in specific rat brain regions. DNA Cell Biol. 10:689-694 (1991).
7. O'Carrol, O. M., S. J. Lolait, M. Konig, and L. Mahan. Molecular cloning and expression of a pituitary somatostatin receptor with preferential affinity for somatostatin-28. Mol. Pharmacol. 42:939-946 (1992).
8. Yamada, Y., S. Post, K. Wang, H. S. Tager, G. I. Bell, and S. Seino. Cloning and functional characterization of a family of human and mouse somatostatin receptors expressed in brain, gastrointestinal tract, and kidney. Proc. Natl. Acad. Sci. USA 89:251-255 (1992).
9. Yasuda, K., S. Rens-Domiano, C. D. Breder, S. F. Law, C. B. Saper, T. Reisine, and G. I. Bell. Cloning of a novel somatostatin receptor, SSTR3, coupled to adenylate cyclase. J. Biol. Chem. 28:20422-20428 (1992).
10. Heisler, S., T. D. Reisine, V. Y. H. Hook, and J. Axelrod. Somatostatin inhibits multireceptor stimulation of cyclic AMP formation and corticotropin secretion in mouse pituitary tumor cells. Proc. Natl. Acad. Sci. USA 79:6502-6506 (1982).
11. Hou, C., R. L. Gilbert, and D. L. Barber. Subtype-specific signaling mechanisms of somatostatin receptors SSTR1 and SSTR2. J. Biol. Chem. 269: 10357-10362 (1994).
12. Lewis, D. L., F. F. Weight, and A. Luini. A guanine nucleotide-binding protein mediates the inhibition of voltage-dependent calcium channel current by somatostatin in pituitary cell line. Proc. Natl. Acad. Sci. USA 83:9035-9039 (1986).
13. Liebow, C., C. Reilly, M. Serrano, and A. V. Schally. Somatostatin analogs inhibit growth of pancreatic cancer by stimulating tyrosine phosphatase. Proc. Natl. Acad. Sci. USA 86:2003-2007 (1989).
14. 3). Cell Calcium 5:223-226 (1984).
15. Strnad, J., C. Eppler, M. Corbett, and J. R. Hadcock. The rat SSTR2 receptor subtype is coupled to inhibition of cyclic AMP accumulation. Biochem. Biophys. Res. Commun. 191:968-976 (1993).
16. Tatsumi, H., M. Costa, M. Schimerlik, and R. A. North. Potassium conductance increased by noradrenaline, opioids, somatostatin, and G-protein: whole-cell recording from guinea pig submucous neurons. J. Neurosci. 10:1675-1682 (1990).
17. + channels through protein dephosphorylation. Nature (Lond.) 351:570-573 (1991).
18. Yamashita, N., N. Shibuya, and E. Ogata. Hyperpolarization of the membrane potential caused by somatostatin in dissociated human pituitary adenoma cells that secrete growth hormone. Proc. Natl. Acad. Sci. USA 83:6198-6202 (1986).
19. Veber, D. E. Design and discovery in the development of peptide analogs, in Proceedings of the Twelfth American Peptide Symposium (J. A. Smith and J. E. Rivier, eds.). ESCOM, Leiden, the Netherlands, 3-14 (1992).
20. Bauer, W., U. Briner, W. Doepfner, R. Haller, R. Huguenin, P. Marbach, T. J. Petcher, and J. Pless. SMS 201-995: A very potent and selective octapeptide analogue of somatostatin with prolonged action. Life Sci. 31: 1133-1140 (1982).
21. Cai, R.-Z., B. Szoke, R. Lu, D. Fu, T. W. Redding, and A. V. Schally. Synthesis and biological activity of highly potent octapeptide analogs of somatostatin. Proc. Natl. Acad. Sci. USA, 83:1896-1900 (1986).
22. Murphy, W. A., M. L. Heiman, V. Lance, I. Mezo, and D. H. Coy, D. Octapeptide analogs of somatostatin exhibiting greatly enhance in vivo amd in vitro inhibition of growth hormone secretion in the rat. Biochem. Biophys. Res. Commun. 132:922-928 (1985).
23. Wynants, C., D. H. Coy, and G. Van Binst. Conformational study of superactive analogues of somatostatin with reduced ring size by. 1H NMR. Tetrahedron 44:941-973 (1988).
24. Raynor, K., W. A. Murphy, D. H. Coy, J. H. Taylor, J.-P. Moreau, K. Yasuda, G. I. Bell, and T. Reisine. Cloned somatostatin receptors: identification of subtype selective peptides and demonstration of high affinity binding of linear peptides. Mol. Pharmacol. 43:838-844 (1993).
25. Tarn, J. P., C.-R. Wu, W. Liu, and J.-W. Zhang. A highly selective and effective reagent for disulfide bond formation in peptide synthesis and protein folding, in Proceedings of the Twelfth American Peptide Symposium (J. A. Smith and J. E. Rivier, eds.). ESCOM, Leiden, the Netherlands, 499-500 (1992).
26. Ellman, G. L. A Colorometric method for determining low concentration of mercaptans. Arch. Biochem. Biophys. 74:443-450 (1958).
27. Hadcock, J. R., J. Strnad, and C. Eppler. The rat SSTR1 somatostatin receptor couples to G-proteins and inhibition of cyclic AMP accumulation. Mol. Pharmacol. 45:410-416 (1994).
28. Ozenberger, B. A., and J. R. Hadcock. A single amino acid substitution in the somatostatin receptor subtype five increases affinity for somatostatin-14. Mol. Pharmacol. 47:82-87 (1995)
29. Hadcock, J. R., and J. Strnad. Somatostatin receptor coupling to G proteins. Methods Neurosci. 29:120-132 (1996).
30. Hadcock, J. R., M. Ros, and C. C. Malbon. Agonist regulation of β-adrenergic receptor mRNA: analysis in S49 mouse lymphoma mutants. J. Biol. Chem. 264:13956-13961 (1989).
31. Price, L. A., E. M. Kajkowski, J. R. Hadcock, B. A. Ozenberger, and M. H. Pausch. Functional coupling of a mammalian somatostatin receptor to the yeast pheromone response pathway. Mol. Cell. Biol. 15:6188-6195 (1995).
32. 50) of an enzymatic reaction. Biochem. Pharmacol. 22:3099-3108 (1973).
33. Hruby, V. J. Implications of the X-ray structure of deamino-oxytocin to agonist/antagonist-receptor interactions. Trends Pharmacol. Sci. 8:336-339 (1987).
34. Pelton, J. T., W. Kazmierski, K. Gulya, H. I. Yamamura, and V. J. Hruby. Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for μ opioid receptors. J. Med. Chem. 29:2370-2375 (1986).
35. Walker, J. M., W. D. Bowen, S. T. Atkins, M. K. Hemstreet, and D. H. Coy. μ-Opiate binding and morphine antagonism by octapeptide analogs of somatostatin. Peptide Res. 8:869-875 (1987).
36. Orbuch, M., J. E. Taylor, D. H. Coy, J. E. Mrozinski, Jr., S. A. Mantey, J. F. Battey, J.-P. Moreau, and R. T. Jensen. Discovery of a novel class of neuromedin B receptor antagonists, substituted somatostatin analogues. Mol. Pharmacol. 44:841-850 (1993).
37. Nicolaou, K. C., J. M. Salvine, K. Raynor, S. Pietranico, T. Reisine, R. M. Freidinger, and R. Hirschmann. Design and synthesis of peptidomimetic employing a β-D-glucose for scaffolding, in Proceedings of the Eleventh American Peptide Symposium (J. E. Rivier and G. R. Marshall, eds.). ESCOM, Leiden, the Netherlands, 881-884 (1990).
38. He, Y.-B., Z. Huang, K. Raynor, T. Reisine, and M. Goodman. Synthesis and conformations of somatostatin-related cyclic hexapeptides incorporating specific α- and β-methylated residues. J. Am. Chem. Soc. 115:8066-8072 (1993).
39. Veber, D. A., R. Saperstein, R. F. Nutt, R. M. Freidinger, S. F. Brady, P. Curley, D. S. Perlow, W. J. Paleveda, C. D. Colton, A. G. Zacchei, D. J. Tocco, D. R. Hoff, R. L. Vandlen, J. E. Gerich, L. Hall, L. Mandarino, E. H. Cordes, P. S. Anderson, and R. Hirschmann, R. A super active cyclic hexapeptide analog of somatostatin. Life Sci. 34:1372-1378 (1984).
40. Eppler, C. M., J. R. Zysk, M. Corbett, and H. M. Shieh. Purification of a pituitary receptor for somatostatin. The utility of biotinylated somatostatin analogs. J. Biol. Chem. 267:15603-15612 (1992).