• 1
    Spiess, J., Rivier, J., Rivier, C. & Vale, W. (1981) Primary structure of corticotropin-releasing factor from ovine hypothalamus. Proc. Natl. Acad. Sci. USA 78, 65176521.
  • 2
    Vale, W., Spiess, J., Rivier, C. & Rivier, J. (1981) Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and β-endorphin. Science 213, 13941397.
  • 3
    Chen, R., Lewis, K.A., Perrin, M.H. & Vale, W.W. (1993) Expression cloning of a human corticotropin-releasing-factor receptor. Proc. Natl. Acad. Sci. USA 90, 89678971.
  • 4
    Vita, N., Laurent, P., Lefort, S., Chalon, P., Lelias, J.M., Kaghad, M., Le Fur, G., Caput, D. & Ferrara, P. (1993) Primary structure and functional expression of mouse pituitary and human brain corticotrophin releasing factor receptors. FEBS Lett. 335, 15.DOI: 10.1016/0014-5793(93)80427-V
  • 5
    Chang, C.P., Pearse, R.V.d., O'Connell, S. & Rosenfeld, M.G. (1993) Identification of a seven transmembrane helix receptor for corticotropin-releasing factor and sauvagine in mammalian brain. Neuron 11, 11871195.
  • 6
    Perrin, M., Donaldson, C., Chen, R., Blount, A., Berggren, T., Bilezikjian, L., Sawchenko, P. & Vale, W. (1995) Identification of a second corticotropin-releasing factor receptor gene and characterization of a cDNA expressed in heart. Proc. Natl. Acad. Sci. USA 92, 29692973.
  • 7
    Yu, J., Xie, L.Y. & Abou-Samra, A.-B. (1996) Molecular cloning of a type A chicken corticotropin-releasing factor receptor with high affinity for urotensin I. Endocrinology 137, 192197.DOI: 10.1210/en.137.1.192
  • 8
    Dautzenberg, F.M., Dietrich, K., Palchaudhuri, M.R. & Spiess, J. (1997) Identification of two corticotropin-releasing factor receptors from Xenopus laevis with high ligand selectivity: unusual pharmacology of the type 1 receptor. J. Neurochem. 69, 16401649.
  • 9
    Lovenberg, T.W., Liaw, C.W., Grigoriadis, D.E., Clevenger, W., Chalmers, D.T., De Souza, E.B. & Oltersdorf, T. (1995) Cloning and characterization of a functionally distinct corticotropin-releasing factor receptor subtype from rat brain. Proc. Natl. Acad. Sci. USA 92, 836840.
  • 10
    Kishimoto, T., Pearse, R.V.N., Lin, C.R. & Rosenfeld, M.G. (1995) A sauvagine/corticotropin-releasing factor receptor expressed in heart and skeletal muscle. Proc. Natl. Acad. Sci. USA 92, 11081112.
  • 11
    Lovenberg, T.W., Chalmers, D.T., Liu, C. & De Souza, E.B. (1995) CRF2 alpha and CRF2 beta receptor mRNAs are differentially distributed between the rat central nervous system and peripheral tissues. Endocrinology 136, 41394142.DOI: 10.1210/en.136.9.4139
  • 12
    Stenzel, P., Kesterson, R., Yeung, W., Cone, R.D., Rittenberg, M.B. & Stenzel-Poore, M.P. (1995) Identification of a novel murine receptor for corticotropin-releasing hormone expressed in heart. Mol. Endocrinol. 9, 637645.DOI: 10.1210/me.9.5.637
  • 13
    De Souza, E.B., Perrin, M.H., Insel, T.R., Rivier, J., Vale, W.W. & Kuhar, M.J. (1984) Corticotropin-releasing factor receptors in rat forebrain: autoradiographic identification. Science 224, 14491451.
  • 14
    De Souza, E.B. (1987) Corticotropin-releasing factor receptors in the rat central nervous system: characterization and regional distribution. J. Neurosci. 7, 88100.
  • 15
    Wynn, P.C., Hauger, R.L., Holmes, M.C., Millan, M.A., Catt, K.J. & Aguilera, G. (1984) Brain and pituitary receptors for corticotropin releasing factor: Localization and differential regulation after adrenalectomy. Peptides 5, 10771084.DOI: 10.1016/0196-9781(84)90174-8
  • 16
    Potter, E., Sutton, S., Donaldson, C., Chen, R., Perrin, M., Lewis, K., Sawchenko, P.E. & Vale, W. (1994) Distribution of corticotropin-releasing factor receptor mRNA expression in the rat brain and pituitary. Proc. Natl. Acad. Sci. USA 91, 87778781.
  • 17
    Chalmers, D.T., Lovenberg, T.W. & De Souza, E.B. (1995) Localization of novel corticotropin-releasing factor receptor (CRF2) mRNA expression to specific subcortical nuclei in rat brain: Comparison with CRF1 receptor mRNA expression. J. Neurosci. 15, 63406350.
  • 18
    Nappi, R.E. & Rivest, S. (1995) Stress-induced genetic expression of a selective corticotropin-releasing factor-receptor subtype within the rat ovaries: an effect dependent on the ovulatory cycle. Biol. Reprod. 53, 14171428.
  • 19
    Slominski, A., Ermak, G., Hwang, J., Chakraborty, A., Mazurkiewicz, J.E. & Mihm, M. (1995) Proopiomelanocortin corticotropin-releasing hormone and corticotropin-releasing hormone receptor genes are expressed in human skin. FEBS Lett. 374, 113116.DOI: 10.1016/0014-5793(95)01090-2
  • 20
    Radulovic, J., Sydow, S. & Spiess, J. (1998) Characterization of native corticotropin-releasing factor receptor type 1 (CRFR1) in the rat and mouse central nervous system. J. Neurosci. Res. in press.
  • 21
    Vaughan, J., Donaldson, C., Bittencourt, J., Perrin, M.H., Lewis, K., Sutton, S., Chan, R., Turnbull, A.V., Lovejoy, D., Rivier, C., Rivier, J., Sawchenko, P.E. & Vale, W. (1995) Urocortin, a mammalian neuropeptide related to fish urotensin I and to corticotropin-releasing factor. Nature 378, 287292.DOI: 10.1038/378287a0
  • 22
    Donaldson, C., Sutton, S., Perrin, M.H., Corrigan, A.Z., Lewis, K.A., Rivier, J., Vaughan, J.M. & Vale, W.W. (1996) Cloning and characterization of human urocortin. Endocrinology 137, 21672170.DOI: 10.1210/en.137.5.2167
  • 23
    Liaw, C.W., Lovenberg, T.W., Barry, G., Oltersdorf, T., Grigoriadis, D.E. & De Souza, E.B. (1996) Cloning and characterization of the human corticotropin-releasing factor-2 receptor complementary deoxyribonucleic acid. Endocrinology 137, 7277.DOI: 10.1210/en.137.1.72
  • 24
    Grigoriadis, D.E. & De Souza, E.B. (1988) The brain corticotropin-releasing factor (CRF) receptor is of lower apparent molecular weight than the CRF receptor in anterior pituitary. Evidence from chemical cross-linking studies. J. Biol. Chem. 263, 1092710931.
  • 25
    Grigoriadis, D.E. & De Souza, E.B. (1989) Heterogeneity between brain and pituitary corticotropin-releasing factor receptors is due to differential glycosylation. Endocrinology 125, 18771888.
  • 26
    Webster, E.L., Grigoriadis, D.E. & De Souza, E.B. (1991) Corticotropin-releasing factor receptors in the brain-pituitary-immune axis. In Stress, Neuropeptides, and Systemic Disease (McCubbin, J.A., Kaufmann, P.G. & Nemeroff, C.B., eds), pp. 233260. Academic Press, San Diego.
  • 27
    Castro, M.G., Morrison, E., Perone, M.J., Brown, O.A., Murray, C.A., Ahmed, I., Perkins, A.V., Europe-Finner, G., Lowenstein, P.R. & Linton, E.A. (1996) Corticotrophin-releasing hormone receptor type 1: generation and characterization of polyclonal antipeptide antibodies and their localization in pituitary cells and cortical neurones in vitro. J. Neuroendocrinol. 8, 521531.
  • 28
    Sydow, S., Radulovic, J., Dautzenberg, F.M. & Spiess, J. (1997) Structure-function relationship of different domains of the rat corticotropin-releasing factor receptor. Mol. Brain Res. 52, 182193.DOI: 10.1016/S0169-328X(97)00256-8
  • 29
    Liaw, C.W., Grigoriadis, D.E., Lovenberg, T.W., De Souza, E.B. & Maki, R.A. (1997) Localization of ligand-binding domains of human corticotropin-releasing factor receptor: a chimeric receptor approach. Mol. Endocrinol. 11, 980985.DOI: 10.1210/me.11.7.980
  • 30
    Lee, C., Gardella, T.J., Abou-Samra, A.-B., Nussbaum, S.R., Segre, G.V., Potts, J.J. Jr, Kronenberg, H.M. & Jüppner, H. (1994) Role of the extracellular regions of the parathyroid hormone (PTH)/PTH-related peptide receptor in hormone binding. Endocrinology 135, 14881495.DOI: 10.1210/en.135.4.1488
  • 31
    Lee, C., Luck, M.D., Jüppner, H., Potts, J.J. Jr, Kronenberg, H.M. & Gardella, T.J. (1995) Homolog-scanning mutagenesis of the parathyroid hormone (PTH) receptor reveals PTH-(1-34) binding determinants in the third extracellular loop. Mol. Endocrinol. 9, 12691278.DOI: 10.1210/me.9.10.1269
  • 32
    Spengler, D., Waeber, C., Pantaloni, C., Holsboer, F., Bockaert, J., Seeburg, P.H. & Journot, L. (1993) Differential signal transduction by five splice variants of the PACAP receptor. Nature 365, 170175.DOI: 10.1038/365170a0
  • 33
    Jelinek, L.J., Lok, S., Rosenberg, G.B., Smith, R.A., Grant, F.J., Biggs, S., Bensch, P.A., Kuijper, J.L., Sheppard, P.O., Sprecher, C.A., O'Hara, P.J., Foster, D., Walder, K.M., Chen, L.H.J., McKernan, P.A. & Kindsvogel, W. (1993) Expression cloning and signaling properties of the rat glucagon receptor. Science 259, 16141616.
  • 34
    Rühmann, A., Köpke, A.K.E., Dautzenberg, F.M. & Spiess, J. (1996) Synthesis and characterization of a photoactivatable analog of corticotropin-releasing factor for specific receptor labeling. Proc. Natl. Acad. Sci. USA 93, 1060910613.DOI: 10.1073/pnas.93.20.10609
  • 35
    Chalmers, D.T., Lovenberg, T.W., Grigoriadis, D.E., Behan, D.P. & De Souza, E.B. (1996) Corticotrophin-releasing factor receptors: from molecular biology to drug design. Trends Pharmacol. Sci. 17, 166172.
  • 36
    Oliveira, L., Paiva, A.C., Sander, C. & Vriend, G. (1994) A common step for signal transduction in G protein-coupled receptors. Trends Pharmacol. Sci. 15, 170172.DOI: 10.1016/0165-6147(94)90137-6
  • 37
    Probst, w. C., Snyder, L.A., Schuster, D.I., Brosius, J. & Sealfon, S.C. (1992) Sequence alignment of the G-protein coupled receptor superfamily. DNA Cell Biol. 11, 120.
  • 38
    Segre, G.V. & Goldring, S.R. (1993) Receptors for secretin calcitonin. parathyroid hormone (PTH)/PTH-related peptide, vasoactive intestinal peptide, glucagonlike peptide 1, growth hormone-releasing hormone, and glucagon belong to a newly discovered G-protein-linked receptor family. Trends Endocrinol. Metab. 4, 309314.DOI: 10.1016/1043-2760(93)90071-L
  • 39
    Frielle, T., Daniel, K.W., Caron, M.G. & Lefkowitz, R.J. (1988) Structural basis of β-adrenergic receptor subtype specificity studied with chimeric β1/β2-adrenergic receptors. Proc. Natl. Acad. Sci. USA 85, 94949498.
  • 40
    Fong, T.M., Huang, R.-R.C. & Strader, C.D. (1992) Localization of agonist and antagoist binding domains of the human neurokinin-1 receptor. J. Biol. Chem. 267, 2566425667.
  • 41
    Gether, U., Johansen, T.E., Snider, R.M., Lowe, J.A. III Nakanishi, S. & Schwartz, T.W. (1993) Different binding epitopes on the NK1 receptor for substance P and a non-peptide antagonist, Nature 362, 345348.DOI: 10.1038/362345a0
  • 42
    Sachais, B.S., Snider, R.M., Lowe, J.A. III & Krause, J.E. (1993) Molecular basis for the species selectivity of the substance P antagonist CP-96,345. J. Biol. Chem. 268, 23192323.
  • 43
    Perrin, M.H., Sutton, S., Bain, D.L., Berggren, W.T. & Vale, W.W. (1998) The first extracellular domain of corticotropin releasing factor-R1 contains major binding determinants for urocortin and astressin. Endocrinology 139, 566570.DOI: 10.1210/en.139.2.566
  • 44
    Cao, Y.J., Gimpl, G. & Fahrenholz, F. (1995) The amino-terminal fragment of the adenylate cyclase activating polypeptide (PACAP) receptor functions as a high affinity PACAP binding domain. Biochem. Biophys. Res. Commun. 212, 673680.
  • 45
    Hashimoto, H., Ogawa, N., Hagihara, N., Yamamoto, K., Imanishi, K., Nogi, H., Nishino, A., Fujita, T., Matsuda, T., Nagata, S. & Baba, A. (1997) Vasoactive intestinal polypeptide and pituitary adenylate cyclase- activating polypeptide receptor chimeras reveal domains that determine specificity of vasoactive intestinal polypeptide binding and activation. Mol. Pharmacol. 52, 128135.
  • 46
    Strader, C.D., Candelore, M.R., Hill, W.S., Sigal, I.S. & Dixon, R.A.F. (1989) Identification of two serine residues involved in agonist activation of the β-adrenergic receptor. J. Biol. Chem. 264, 1357213578.
  • 47
    Barak, L.S., Ménard, L., Ferguson, S.S.G., Colapietro, A.-M. & Caron, M.G. (1995) The conserved seven-transmembrane sequence NP(X)2,3Y of the G-protein-coupled receptor superfamily regulates multiple properties of the β2-adrenergic receptor. Biochemistry 34, 1540715414.
  • 48
    Wess, J., Blin, N., Mutschler, E. & Blüml, K. (1995) Muscarinic acetylcholine receptors: structural basis of ligand binding and G protein coupling. Life Sci. 56, 915912.DOI: 10.1016/0024-3205(95)00028-5
  • 49
    Walker, P., Munoz, M., Martinez, R. & Peitsch, M.C. (1994) Acidic residues in extracellular loops of the human Y1 neuropeptide Y receptor are essential for ligand binding. J. Biol. Chem. 269, 28632869.
  • 50
    Flanagan, C.A., Becker, I.I., Davidson, J.S., Wakefield, I.K., Zhou, W., Sealfon, S.C. & Millar, R.P. (1994) Glutamate 301 of the mouse gonadotropin-releasing hormone receptor confers specifictiy for arginine 8 of mammalian gonadotropin-releasing hormone. J. Biol. Chem. 268, 2263622641.
  • 51
    Chini, B., Mouillac, B., Ala, Y., Balestre, M., Trumpp-Kallmeyer, S., Hoflack, J., Elands, J., Hibert, M., Manning, M., Jard, S. & Barberis, C. (1995) Tyr 115 is the key residue for determining agonist selectivity in the V1A vasopressin receptor. EMBO J. 14, 21762182.
  • 52
    Gardella, T.J., Jüppner, H., Wilson, A.K., Keutmann, H.T., Abou-Samra, A.-B., Segre, G.V., Bringhurst, F.R., Potss, J.T.J., Nussbaum, S.R. & Kronenberg, H.M. (1994) Determinants of [Arg2]PTH-(1-34) binding and signaling in the transmembrane region of the parathyroid hormone receptor. Endocrinology 135, 11861194.DOI: 10.1210/en.135.3.1186
  • 53
    Jüppner, H., Schipani, E., Bringhurst, F.R., McClure, I., Keutmann, H.T., Potts, J.T.J., Kronenberg, H.M., Abou-Samra, A.-B., Segre, G.V. & Gardella, T.J. (1994) The extracellular, amino-terminal region of the PTH/PTHrP receptor determines the binding affinity for carboxy-terminal fragments of PTH(1-34), Endocrinology 134, 879884.DOI: 10.1210/en.134.2.879
  • 54
    Kim, J., Jiang, Q., Glashofer, M., Yehle, S., Wess, J. & Jacobson, K.A. (1996) Glutamate residues in the second extracellular loop of the human A2a adenosine receptor are required for ligand recognition. Mol. Pharmacol. 49, 683691.