Evidence that corticotropin-releasing factor receptor type 1 couples to Gs- and Gi-proteins through different conformations of its J-domain

British Journal of Pharmacology

Volumn 149, Issue 7, 2006, Pages 942-947

  Berger, H ^a   Heinrich, N ^a   Wietfeld, D ^a   Bienert, M ^a   Beyermann, M ^a  

^a LEIBNIZ INSTITUT FÜR MOLEKULARE PHARMAKOLOGIE   (Germany)

Author keywords

CRF receptor 1; G protein coupling; Non peptide antagonist; Two domain model

Indexed keywords

ANTALARMIN; CORTICOTROPIN RELEASING FACTOR ANTAGONIST; CORTICOTROPIN RELEASING FACTOR RECEPTOR 1; CORTICOTROPIN RELEASING FACTOR[9-41]; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); INHIBITORY GUANINE NUCLEOTIDE BINDING PROTEIN; SAUVAGINE; STIMULATORY GUANINE NUCLEOTIDE BINDING PROTEIN; SULFUR 35; UROCORTIN;

ALLOSTERISM; ALPHA HELIX; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BINDING ASSAY; COMPETITIVE INHIBITION; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; EMBRYO; EMBRYO CELL; HUMAN; HUMAN CELL; KIDNEY CELL; NONHUMAN; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN PROTEIN INTERACTION; RAT;

ALLOSTERIC REGULATION; BINDING, COMPETITIVE; CELL LINE; CORTICOTROPIN-RELEASING HORMONE; DOSE-RESPONSE RELATIONSHIP, DRUG; GTP-BINDING PROTEIN ALPHA SUBUNITS, GI-GO; GTP-BINDING PROTEIN ALPHA SUBUNITS, GS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HORMONE ANTAGONISTS; HUMANS; MODELS, MOLECULAR; PEPTIDE FRAGMENTS; PEPTIDES; PROTEIN CONFORMATION; PROTEIN STRUCTURE, TERTIARY; PYRIMIDINES; PYRROLES; RECEPTORS, CORTICOTROPIN-RELEASING HORMONE; SIGNAL TRANSDUCTION; TRANSFECTION;

EID: 33845217668     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0706926     Document Type: Article

References (20)

1. Assil IQ, Qi L, Arai M, Shomali M, Abou SA (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. Beyermann M, Rothemund S, Heinrich N, Fechner K, Furkert J, Dathe M et al. (2000). A role for a helical connector between two receptor binding sites of a long-chain peptide hormone. J Biol Chem 275: 5702-5709.
3. Christopoulos A, Kenakin T (2002). G protein-coupled receptor allosterism and complexing. Pharmacol Rev 54: 323-374.
4. Dautzenberg FM, Hauger RL (2002). The CRF peptide family and their receptors: yet more partners discovered. Trends Pharmacol Sci 23: 71-77.
5. Dautzenberg FM, Wille S, Braun S, Hauger RL (2002). GRK3 regulation during CRF- and urocortin-induced CRF1 receptor desensitization. Biochem Biophys Res Commun 298: 303-308.
6. Grammatopoulos DK, Dai YL, Randeva HS, Levine MA, Karteris E, Easton AJ et al. (1999). A novel spliced variant of the type 1 corticotropin-releasing hormone receptor with a deletion in the seventh transmembrane domain present in the human pregnant term myometrium and fetal membranes. Mol Endocrinol 13: 2189-2202.
7. Grammatopoulos DK, Randeva HS, Levine MA, Katsanou ES, Hilhouse EW (2000). Urocortin, but not corticotropin-releasing hormone (CRH), activates the mitogen-activated protein kinase signal transduction pathway in human pregnant myometrium: an effect mediated via R1 alpha and R2 beta CRH receptor subtypes and stimulation of Gq-proteins. Mol Endocrinol 14: 2076-2091.
8. Hillhouse EW, Grammatopoulos DK (2006). The molecular mechanisms underlying the regulation of the biological activity of corticotropin-releasing hormone receptors: Implications for physiology and pathophysiology. Endocr Rev 27: 260-286.
9. Hoare SR, Sullivan SK, Ling N, Crowe PD, Grigoriadis DE (2003). Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists. Mol Pharmacol 63: 751-765.
10. Hoare SR, Sullivan SK, Schwarz DA, Ling N, Vale WW, Crowe PD et al. (2004). Ligand affinity for amino-terminal and juxtamembrane domains of the corticotropin releasing factor type I receptor: regulation by G protein and nonpeptide antagonists. Biochemistry 43: 3996-4011.
11. Jensen AA, Spalding TA (2004). Allosteric modulation of G protein coupled receptors. Eur J Pharm Sci 21: 407-420.
12. Kenakin T (2002). Efficacy at G protein-coupled receptors. Nat Rev Drug Discov 1: 103-110.
13. Liaw CW, Grigoriadis DE, Lorang MT, de Souza EB, Maki RA (1997). Localization of agonist- and antagonist-binding domains of human corticotropin-releasing factor receptors. Mol Endocrinol 11: 2048-2053.
14. Nielsen SM, Nielsen LZ, Hjorth SA, Perrin MH, Vale WW (2000). Constitutive activation of tethered-peptide/corticotropin-releasing factor receptor chimeras. Proc Natl Acad Sci USA 97: 10277-10281.
15. Pradier L, Menager J, Le-Guern J, Bock M-D, Heuillet E, Fardin V et al. (1994). Septide: an agonist for the NK1 receptor acting at a site distinct from substance P. Mol Pharmacol 45: 287-293.
16. Reinhart GJ, Xie Q, Liu XJ, Zhu YF, Fan J, Chen C et al. (2004). Species selectivity of nonpeptide antagonists of the gonadotropin-releasing hormone receptor is determined by residues in extracellular loops II and III and the amino terminus. J Biol Chem 279: 34115-34122.
17. Soudijn W, van-Wijngaarden I, Ijzerman AP (2002). Allosteric modulation of G protein-coupled receptors. Curr Opin Drug Discov Dev 5: 749-755.
18. Strader CD, Fong TM, Tota MR, Underwood D, Dixon RA (1994). Structure and function of G protein-coupled receptors. Annu Rev Biochem 63: 101-132.
19. Wietfeld D, Heinrich N, Furkert J, Fechner K, Beyermann M, Bienert M et al. (2004). Regulation of the coupling to different G proteins of rat corticotropin-releasing factor receptor type 1 in human embryonic kidney 293 cells. J Biol Chem 279: 38386-38394.
20. Zhang G, Huang N, Li YW, Qi X, Marshall AP, Yan XX et al. (2003). Pharmacological characterization of a novel nonpeptide antagonist radioligand, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2, 3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for corticotropin-releasing factor1 receptors. J Pharmacol Exp Ther 305: 57-69.