Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists

Molecular Pharmacology

Volumn 63, Issue 3, 2003, Pages 751-765

  Hoare, Sam R J ^a   Sullivan, Sue K ^a   Ling, Nicholas ^a   Crowe, Paul D ^a   Grigoriadis, Dimitri E ^a  

^a NEUROCRINE BIOSCIENCES INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 CHLORO 4 [N (CYCLOPROPYLMETHYL) N PROPYLAMINO] 2 METHYL 6 (2,4,6 TRICHLOROANILINO)PYRIMIDINE; 8 (2,4 DICHLOROPHENYL) 4 [2 METHOXY 1 (METHOXYMETHYL)ETHYLAMINO] 2,7 DIMETHYLPYRAZOLO[1,5 A][1,3,5]TRIAZINE; ANTALARMIN; ASTRESSIN; CORTICOTROPIN RELEASING FACTOR ANTAGONIST; CORTICOTROPIN RELEASING FACTOR RECEPTOR; G PROTEIN COUPLED RECEPTOR; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); LIGAND; NBI 35965; SAUVAGINE; UNCLASSIFIED DRUG; UROCORTIN;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; COMPETITIVE INHIBITION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DISSOCIATION; DRUG BINDING SITE; DRUG RECEPTOR BINDING; IC 50; MOUSE; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; BINDING SITES; CORTICOTROPIN-RELEASING HORMONE; HUMANS; PEPTIDE FRAGMENTS; PEPTIDES; PYRAZOLES; RATS; RECEPTORS, CORTICOTROPIN-RELEASING HORMONE; TRIAZINES; TRITIUM;

EID: 0037334023     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.63.3.751     Document Type: Article

References (34)

1. Assil IQ, Qi LJ, Arai M, Shomali M, and Abou-Samra AB (2001) Juxtamembrane region of the amino terminus of the corticotropin releasing factor receptor type 1 is important for ligand interaction. Biochemistry 40:1187-1195.
2. Chen C, Dagnino R Jr, De Souza EB, Grigoriadis DE, Huang CQ, Kim KI, Liu Z, Moran T, Webb TR, Whitten JP, et al. (1996) Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 receptor antagonists. J Med Chem 39:4358-4360.
3. Chen R, Lewis KA, Perrin MH, and Vale WW (1993) Expression cloning of a human corticotropin-releasing-factor receptor. Proc Natl Acad Sci USA 90:8967-8971.
4. Chen YL, Mansbach RS, Winter SM, Brooks E, Collins J, Corman ML, Dunaiskis AR, Faraci WS, Gallaschun RJ, Schmidt A, et al. (1997) Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor 1 receptor antagonist. J Med Chem 40:1749-1754.
5. 50) of an enzymatic reaction, Biochem Pharmacol 22:3099-3108.
6. Dautzenberg FM and Hauger RL (2002) The CRF peptide family and their receptors: yet more partners discovered. Trends Pharmacol Sci 23:71-77.
7. Dautzenberg FM, Wille S, Lohmann R, and Spiess J (1998) Mapping of the ligand-selective domain of the Xenopus laevis corticotropin-releasing factor receptor 1: implications for the ligand-binding site. Proc Natl Acad Sci USA 95:4941-4946.
8. Ehlert FJ (1988) Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods. Mol Pharmacol 33:187-194.
9. Gilligan PJ, Robertson DW, and Zaczek R (2000) Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents. J Med Chem 43:1641-1660.
10. Grigoriadis D, Liaw CW, Oltersdorf T, and DeSouza EB (1994) Pharmacological characterization of rat and human corticotropin-releasing factor (CRF) receptors expressed in stable cell lines. Soc Neurosci Abstr 20:1345.
11. 1) receptor antagonist for the potential treatment of depression and anxiety-related disorders. Soc Neurosci Abstr 26:2148.
12. Grigoriadis DE, Haddach M, Ling N, and Saunders J (2001) The CRF receptor: structure, function and potential for therapeutic intervention. Curr Med Chem Central Nerv Syst Agents 1:63-97.
13. 1 receptor antagonist. J Med Chem 43:449-456.
14. Hofmann BA, Sydow S, Jahn O, van Werven L, Liepold T, Eckart K, and Spiess J (2001) Functional and protein chemical characterization of the N-terminal domain of the rat corticotropin-releasing factor receptor 1. Protein Sci 10:2050-2062.
15. Holsboer F (1999) The rationale for corticotropin-releasing hormone receptor (CRH-R) antagonists to treat depression and anxiety. J Psychiatr Res 33:181-214.
16. Kenakin T (2002) Drug efficacy at G protein-coupled receptors. Annu Rev Pharmacol Toxicol 42:349-379.
17. Lazareno S and Birdsall NJ (1995) Detection, quantitation and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors. Mol Pharmacol 48:362-378.
18. Leppik RA and Birdsall NJ (2000) Agonist binding and function at the human α(2A)-adrenoceptor: allosteric modulation by amilorides. Mol Pharmacol 58:1091-1099.
19. Liaw CW, Grigoriadis DE, Lorang MT, De Souza EB, and Maki RA (1997a) Localization of agonist- and antagonist-binding domains of human corticotropin-releasing factor receptors. Mol Endocrinol 11:2048-2053.
20. Liaw CW, Grigoriadis DE, Lovenberg TW, De Souza EB, and Maki RA (1997b) Localization of ligand-binding domains of human corticotropin-releasing factor receptor: a chimeric receptor approach. Mol Endocrinol 11:980-985.
21. Miranda A, Koerber SC, Gulyas J, Lahrichi SL, Craig AG, Corrigan A, Hagler A, Rivier C, Vale W, and Rivier J (1994) Conformationally restricted competitive antagonists of human/rat corticotropin-releasing factor. J Med Chem 37:1450-1459.
22. Nielsen SM, Nielsen LZ, Hjorth SA, Perrin MH, and Vale WW (2000) Constitutive activation of tethered-peptide/corticotropin-releasing factor receptor chimeras. Proe Natl Acad Sci USA 97:10277-10281.
23. Perrin MH, Fischer WH, Kunitake KS, Craig AG, Koerber SC, Cervini LA, Rivier JE, Groppe JC, Greenwald J, Moller Nielsen S, et al. (2001) Expression, purification and characterization of a soluble form of the first extracellular domain of the human type 1 corticotropin releasing factor receptor. J Biol Chem 276:31528- 31534.
24. Perrin MH, Sutton S, Bain DL, Berggren WT, and Vale WW (1998) The first extracellular domain of corticotropin releasing factor-R1 contains major binding determinants for urocortin and astressin. Endocrinology 139:566-570.
25. Perrin MH and Vale WW (1999) Corticotropin releasing factor receptors and their ligand family. Ann NY Acad Sci 885:312-328.
26. Rivier C and Vale W (1983) Modulation of stress-induced ACTH release by corticotropin-releasing factor, catecholamines and vasopressin. Nature (Lond) 305:325-327.
27. Rivier J, Rivier C, and Vale W (1984) Synthetic competitive antagonists of corticotropin-releasing factor: effect on ACTH secretion in the rat. Science (Wash DC) 224:889-891.
28. Stockton JM, Birdsall NJ, Burgen AS, and Hulme EC (1983) Modification of the binding properties of muscarinic receptors by gallamine. Mol Pharmacol 23:551-557.
29. Sydow S, Flaccus A, Fischer A, and Spiess J (1999) The role of the fourth extracellular domain of the rat corticotropin-releasing factor receptor type 1 in ligand binding. Eur J Biochem 259:55-62.
30. Trankle C, Weyand O, Schroter A, and Mohr K (1999) Using a radioalloster to test predictions of the cooperativity model for gallamine binding to the allosteric site of muscarinic acetylcholine M(2) receptors. Mol Pharmacol 56:962-965.
31. Vale W, Spiess J, Rivier C, and Rivier J (1981) Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and β-endorphin. Science (Wash DC) 213:1394-1397.
32. Webster EL, Lewis DB, Torpy DJ, Zachman EK, Rice KC, and Chrousos GP (1996) In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRH) receptor antagonist: suppression of pituitary ACTH release and peripheral inflammation. Endocrinology 137:5747-5750.
33. Wille S, Sydow S, Palchaudhuri MR, Spiess J, and Dautzenberg FM (1999) Identification of amino acids in the N-terminal domain of corticotropin-releasing factor receptor 1 that are important determinants of high-affinity ligand binding. J Neurochem 72:388-395.
34. 1 receptor antagonist. Soc Neurosci Abstr 23:1763.