Corticotropin-releasing factor peptide antagonists: Design, characterization and potential clinical relevance

Frontiers in Neuroendocrinology

Volumn 35, Issue 2, 2014, Pages 161-170

  Rivier, Jean E ^a   Rivier, Catherine L ^a  

^a SALK INSTITUTE FOR BIOLOGICAL STUDIES   (United States)

Author keywords

Astressin; Astressin B; CRF antagonists; H rCRF; OCRF

Indexed keywords

5 CHLORO 4 [N (CYCLOPROPYLMETHYL) N PROPYLAMINO] 2 METHYL 6 (2,4,6 TRICHLOROANILINO)PYRIMIDINE; ANTISAUVAGINE 30; ASTRESSIN 2B; ASTRESSIN B; CORTICOTROPIN RELEASING FACTOR ANTAGONIST; CORTICOTROPIN RELEASING FACTOR DERIVATIVE; CORTICOTROPIN RELEASING FACTOR RECEPTOR 1; CORTICOTROPIN RELEASING FACTOR RECEPTOR 2; DEGARELIX; GONADORELIN ANTAGONIST; HORMONE RECEPTOR STIMULATING AGENT; PEPTIDE HORMONE RECEPTOR BLOCKING AGENT; PROTIRELIN DERIVATIVE; SAUVAGINE; SOMATOSTATIN DERIVATIVE; STRESSIN 1; UNCLASSIFIED DRUG; UROTENSIN I; CORTICOTROPIN RELEASING FACTOR; CORTICOTROPIN RELEASING FACTOR RECEPTOR; CYCLO(31-34)(PHENYLALANYL(12)-NORLEUCYL(21,28)-GLUTAMYL(31)-LYSYL(34))ACETYL-CORTICOTROPIN RELEASING FACTOR (4-41); CYCLOPEPTIDE; PEPTIDE FRAGMENT;

BINDING AFFINITY; BRAIN DISEASE; DRUG DESIGN; DRUG DETERMINATION; DRUG POTENCY; DRUG PURIFICATION; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; DRUG TARGETING; HUMAN; IRRITABLE COLON; NONHUMAN; PRIORITY JOURNAL; REVIEW; STRUCTURE ACTIVITY RELATION; AGONISTS; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; PHYSIOLOGICAL STRESS;

ANIMALS; CORTICOTROPIN-RELEASING HORMONE; HUMANS; PEPTIDE FRAGMENTS; PEPTIDES, CYCLIC; RECEPTORS, CORTICOTROPIN-RELEASING HORMONE; STRESS, PHYSIOLOGICAL;

EID: 84896121320     PISSN: 00913022     EISSN: 10956808     Source Type: Journal    
DOI: 10.1016/j.yfrne.2013.10.006     Document Type: Review

References (133)

1. Acheson D., Feifil D., de Wilde S., Mckinney R., Lhor J., Risbrough V. The effect of intranasal oxytocin treatment on conditioned fear extinction and recall in healthy human sample. Psychopharmacology 2013, 229:199-208.
2. Bale, T., Vale, W., 2004. CRF and CRF receptors: role in stress responsivity and other behaviors. In: Cho, A.K. (Ed.), Annual Review of Pharmacology and Toxicology, Annual Reviews, pp. 525-557.
3. Baram T.Z., Mitchell W.G., Haden E. Inhibition of pituitary-adrenal secretion by a corticotropin releasing hormone antagonist in humans. Mol Psychiat. 1996, 1:320-324.
4. Barquist E., Bonaz B., Martinez V., Rivier J., Zinner M., Taché Y. Neuronal pathways involved in abdominal surgery-induced gastric ileus in rats. Am. J. Physiol. 1996, R888-R894.
5. Behan D.P., De Souza E.B., Lowry P.J., Potter E., Sawchenko P., Vale W.W. Corticotropin releasing factor (CRF) binding protein: a novel regulator of CRF and related peptides. Front. Neuroendocrinol. 1995, 16:362-382.
6. Berardis D.D., Marini S., Iasevoli F., Tomassetti C., Bartolomeis A.D., Mazza M., Valchera A., Fornaro M., Cavuto M., Srinivasan V., Sepede G., Martinotti G., Giannantonio M.D. The role of intranasal oxytocin in the treatment of patients with schizophrenia: a systemic review. CNS Neurol. Disord. Drug Targets 2013, 12:252-264.
7. Bethlehem R.A., van Honk J., Auyeung B., Baron-Cohen S. Oxytocin, brain physiology, and functional connectivity: a review of intranasal oxytocin fMRI studies. 2013, 38:962-974.
8. Beyermann M., Fechner K., Furkert J., Krause E., Bienert M. A single-point slight alteration set as a tool for structure-activity relationship studies of ovine corticotropin releasing factor. J. Med. Chem. 1996, 39:3324-3330.
9. Beyermann M., Heinrich N., Fechner K., Furkert J., Zhang W., Kraetke O., Bienert M., Berger H. Achieving signalling selectivity of ligands for the corticotropin-releasing factor type 1 receptor by modifying the agonist's signalling domain. Br. J. Pharmacol. 2007, 151:851-859.
10. Broadbear J.H. Corticotropin-releasing hormone in nonhuman primates. Front. Biosci. 2006, 11:2303-2335.
11. Broadbear J.H., Winger G., Rivier J.E., Rice K.C., Woods J.H. Corticotropin-releasing hormone antagonists, astressin B and antalarmin: differing profiles of activity in rhesus monkeys. Neuropsychopharmacology 2004, 29:1112-1121.
12. Broqua P., Riviere P., Conn P.M., Rivier J.E., Aubert M.K., Junien J.-L. Pharmacological profile of a new, potent and long-acting gonadotropin-releasing hormone antagonist: Degarelix. J. Pharmacol. Exp. Ther. 2002, 301:95-102.
13. Chalmers D.T., Lovenberg T.W., DeSouza E.B. 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. 1995, 15:6340-6350.
14. Chang C.P., Pearse R.V., O'Connell S., Rosenfeld M.G. Identification of a seven transmembrane helix receptor for corticotropin-releasing factor and sauvagine in mammalian brain. Neuron 1993, 11:1187-1195.
15. Chatzaki E., Anton P.A., Million M., Lambropoulou M., Constantinidis T., Kolios G., Tache Y., Grigoriadis D.E. Corticotropin-releasing factor receptor subtype 2 in human colonic mucosa: down-regulation in ulcerative colitis. World J. Gastroenterol. 2013, 19:1416-1423.
16. Chen R., Lewis K.A., Perrin M.H., Vale W.W. Expression cloning of a human corticotropin releasing factor (CRF) receptor. Proc. Natl. Acad. Sci. U.S.A. 1993, 90:8967-8971.
17. Chen Y.W., Rada P.V., Butzler B.P., Leibowitz S.F., Hoebel B.G. Corticotropin-releasing factor in the nucleus accumbens shell induces swim depression, anxiety, and anhedonia along with changes in local dopamine/acetylcholine balance. Neuroscience 2012, 206:155-166.
18. Chou P.Y., Fasman G.D. Empirical predictions of protein conformation. Annu. Rev. Biochem. 1978, 47:251-276.
19. Chou P.Y., Fasman G.D. Prediction of the secondary structure of proteins from their amino acid sequence. Adv. Enzymol. 1987, 47:45-148.
20. Coskun T., Bozkurt A., Alican I., Ozkutlu U., Kurtel H., Yegen B.C. Pathways mediating CRF-induced inhibition of gastric emptying in rats. Regul. Pept. 1997, 69:113-120.
21. Curtis A.L., Grigoriadis D.E., Page M.E., Rivier J., Valentino R.J. Pharmacological comparison of two corticotropin-releasing factor antagonists: in vivo and in vitro studies. J. Pharmacol. Exp. There. 1994, 268:359-365.
22. Curtis A.L., Lechner S.M., Pavcovich L.A., Valentino R.J. Activation of the locus coeruleus noradrenergic system by intracoerulear microinfusion of corticotropin-releasing factor: effects on discharge rate, cortical norepinephrine levels and cortical electroencephalographic activity. J. Pharmacol. Exp. Ther. 1997, 281:163-172.
23. Dautzenberg F.M., Hauger R.L. The CRF peptide family and their receptors: yet more partners discovered. Trends Pharmacol. Sci. 2002, 23:71-77.
24. Dinan T.G. Novel approaches to the treatment of depression by modulating the hypothalamic-pituitary-adrenal axis. Hum. Psychopharmacol. Clin. Exp. 2001, 16:89-93.
25. Farrokhi C.B., Tovote P., Blanchard R.J., Blanchard D.C., Litvin Y., Spiess J. Cortagine: behavioral and autonomic function of the selective CRF receptor subtype 1 agonist. CNS Drug Rev. 2007, 13:423-443.
26. Fisher L., Rivier C., Rivier J., Brown M. Differential antagonist activity of α-helical CRF(9-41) in three bioassay systems. Endocrinology 1991, 129:1312-1316.
27. 37]CRF attenuates the acute actions of te highly potent cannabinoid receptor agonist HU-210 on defensive-withdrawal behavior in rats. J. Pharmacol. Exp. Ther. 1996, 276:56-64.
28. Fujino M., Shinagawa S., Yamazaki I., Kobayashi S., Obayashi M., Fukuda T., Nakayama R., White W.F., Rippel R.H. [Des-Gly-NH210, Pro-ethylamide9]-LH-RH: a highly potent analog of luteinizing hormone releasing hormone. Arch. Biochem. Biophys. (Commun.) 1973, 154:488-489.
29. Fukudo S. Role of corticotropin-releasing hormone in irritable bowel syndrome and intestinal inflammation. J. Gastroenterol. 2007, 42(Suppl. 17):48-51.
30. Fukudo S., Nomura T., Hongo M. Impact of corticotropin-releasing hormone on gastrointestinal motility and adrenocorticotropic hormone in normal controls and patients with irritable bowel syndrome. Gut 1998, 42:845-849.
31. Gold P.W., Kling M.A., Khan I., Calabrese J.R., Kalogeras K., Post R.M., Avgerinos P.C., Loriaux D.L., Chrousos G.P. Corticotropin releasing hormone: relevance to normal physiology and to the pathophysiology and differential diagnosis of hypercortisolism and adrenal insufficiency. Hypothalamic Dysfunction in Neuropsychiatric Disorders 1987, 183-200. Raven Press, New York. D. Nerozzi, F.K. Goodwin, E. Costa (Eds.).
32. Goldman M.E., McKee R.L., Caulfield M.P., Reagan J.E., Levy J.J., Gay C.T., DeHaven P.A., Rosenblatt M., Chorev M. A new highly potent parathyroid hormone antagonist: [D-Trp12, Tyr34]bPTH-(7-34)NH2. Endocrinology 1988, 123:2597-2599.
33. Grace C.R.R., Cervini L., Gulyas J., Rivier J., Riek R. Astressin-amide and astressin-acid are structurally different in DMSO. Biopolymers 2007, 87:196-205.
34. Grace C.R.R., Perrin M., Gulyas J., Rivier J., Vale W., Riek R. NMR structure of the first extracellular domain of corticotropin releasing factor receptor 1 (ECD1-CRF-R1) complexed with a high affinity agonist. J. Biol. Chem. 2010, 285:38580-38589.
35. Griebel G., Holsboer F. Neuropeptide receptor ligans as drugs for phsychiatric diseases: the end of the beginning?. Nat. Rev. 2012, 11:462-478.
36. Gulyas J., Rivier C., Perrin M., Koerber S.C., Sutton S., Corrigan A., Lahrichi S.L., Craig A.G., Vale W.W., Rivier J. Potent, structurally constrained agonists and competitive antagonists of corticotropin releasing factor (CRF). Proc. Natl. Acad. Sci. U.S.A. 1995, 92:10575-10579.
37. Habib K.E., Gold P.W., Chrousos G.P. Neuroendocrinology of stress. Endocrinol. Metab. Clin. North Am. 2001, 30:695-728.
38. Hauger R.L., Risbrough V., Brauns O., Dautzenberg F.M. Corticotropin releasing factor (CRF) receptor signaling in the central nervous system: new molecular targets. CNS Neurol. Disord. Drug Targets 2006, 5:453-479.
39. Hauger R.L., Risbrough V., Oakley R.H., Olivares-Reyes J.A., Dautzenberg F.M. Role of CRF receptor signaling in stress vulnerability, anxiety, and depression. Ann. N. Y. Acad. Sci. 2009, 1179:120-143.
40. Hernandez J.-F., Kornreich W., Rivier C., Miranda A., Yamamoto G., Andrews J., Taché Y., Vale W.W., Rivier J.E. Synthesis and relative potencies of new constrained CRF antagonists. J. Med. Chem. 1993, 36:2860-2867.
41. Hoeger C., Galyean R., Boublik J., McClintock R., Rivier J. Preparative reversed phase high performance liquid chromatography. II. Effects of buffer pH on the purification of synthetic peptides. Biochromatography 1987, 2:134-142.
42. Horiuchi N., Holick M.F., Potts J.T., Rosenblatt M. A parathyroid hormone inhibitor in vivo: design and biological evaluation of a hormone analog. Science 1983, 220:1053-1055.
43. Jiang G., Stalewski J., Galyean R., Dykert J., Schteingart C., Broqua P., Aebi A., Aubert M.L., Semple G., Robson P., Akinsanya K., Haigh R., Riviere P., Trojnar J., Junien J.L., Rivier J.E. GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6. J. Med. Chem. 2001, 44:453-467.
44. Jones D.N.C., Kortekaas R., Hatcher P.D., Middlemiss D.N., White A., Hagan J.J. Influence of peptide CRF receptor antagonists upon the behavioural effects of human/rat CRF. Eur. J. Pharmacol. 1999, 373:141-145.
45. Kandel E.R. Biology and the future of psychoanalysis: a new intellectual framework for psychiatry revisited. Am. J. Psychiat. 1999, 156:505-524.
46. Karten M.J., Rivier J.E. Gonadotropin-releasing hormone analog design. Structure-function studies toward the development of agonists and antagonists: rationale and perspective. Endocr. Rev. 1986, 7:44-66.
47. Karten M.J., Hoeger C.A., Hook W.A., Lindbert M.C., Naqvi R.H. The development of safer GnRH antagonists: strategy and status. Recent Progress on GnRH and Gonadal Peptides 1990, 147-158. Elsevier, Paris, France. P. Bouchard, F. Haour, P. Franchimont, B. Schatz (Eds.).
48. Keller P.A., McCluskey A., Morgan J., O'Connor S.M. The role of the HPA axis in psychiatric disorders and CRF antagonists as potential treatments. Arch. Pharm. (Weinheim) 2006, 339:346-355.
49. Kishimoto T., Pearse R.V., Lin C.R., Rosenfeld M.G. A sauvagine/corticotropin-releasing factor receptor expressed in heart and skeletal muscle. Proc. Natl. Acad. Sci. U.S.A. 1995, 92:1108-1112.
50. Koerber S.C., Gulyas J., Lahrichi S.L., Corrigan A., Craig A.G., Rivier C., Vale W.W., Rivier J. Constrained corticotropin releasing factor (CRF) agonists and antagonists with i-(i+3) Glu-Xaa-DXbb-Lys bridges. J. Med. Chem. 1998, 41:5002-5011.
51. Koob G.F. A role for brain stress systems in addiction. Neuron 2008, 59:11-34.
52. Koob G.F. Corticotropin-releasing factor, neuroplasticity (sensitization), and alcoholism. Proc. Natl. Acad. Sci. U.S.A. 2008, 105:8809-8810.
53. Kornreich W.D., Galyean R., Hernandez J.-F., Craig A.G., Donaldson C.J., Yamamoto G., Rivier C., Vale W.W., Rivier J.E. Alanine series of ovine corticotropin releasing factor (oCRF): a structure-activity relationship study. J. Med. Chem. 1992, 35:1870-1876.
54. Kostich W.A., Chen A., Sperle K., Largent B.L. Molecular identification and analysis of a novel human corticotropin-releasing factor (CRF) receptor: the CRF2gamma receptor. Mol. Endocrinol. 1998, 12:1077-1085.
55. Krohg K., Hageman I., Jorgensen M.B. Corticotropin-releasing factor (CRF) in stress and disease: a review of literature and treatment perspectives with special emphasis on psychiatric disorders. Nord. J. Psych. 2008, 62:8-16.
56. Lau S.H., Rivier J., Vale W., Kaiser E.T., Kezdy F.J. Surface properties of an amphiphilic peptide hormone and of its analog: corticotropin-releasing factor and sauvagine. Proc. Natl. Acad. Sci. U.S.A. 1983, 80:7070-7074.
57. Lederis K., Letter A., McMaster D., Moore G. Complete amino acid sequence of urotensin I, a hypotensive and corticotropin-releasing neuropeptide from Catostomus. Science 1982, 218:162-164.
58. Lee C., Sarna S.K. Central regulation of gastric emptying of solid nutrient meals by corticotropin releasing factor. Neurogastroenterol. Motil. 1997, 9:221-229.
59. Lewis K., Li C., Perrin M.H., Blount A., Kunitake K., Donaldson C., Vaughan J., Reyes T.M., Gulyas J., Fischer W., Bilezikjian L., Rivier J., Sawchenko P.E., Vale W.W. Identification of Urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 2001, 98:7570-7575.
60. Liapakis G., Venihaki M., Margioris A., Grigoriadis D., Gkountelias K. Members of CRF family and their receptors: from past to future. Curr. Med. Chem. 2011, 18:2583-2600.
61. Lovenberg T.W., Liaw C.W., Grigoriadis D.E., Clevenger W., Chalmers D.T., DeSouza E.B., Oltersdorf T. Cloning and characterization of a functionally distinct corticotropin-releasing factor receptor subtype from rat brain. Proc. Natl. Acad. Sci. U.S.A. 1995, 92:836-840.
62. Lowery E.G., Thiele T.E. Pre-clinical evidence that corticotropin-releasing factor (CRF) receptor antagonists are promising targets for pharmacological treatment of alcoholism. CNS Neurol. Disord. Frug Targets 2010, 9:77-86.
63. Macey D.J., Koob G.F., Markou A. CRF and urocortin decreased brain stimulation reward in the rat: reversal by a CRF receptor antagonist. Brain Res. 2000, 866:82-91.
64. Märki W., Spiess J., Taché Y., Brown M., Rivier J.E. Total solid phase synthesis of porcine gut gastrin releasing peptide (GRP), a mammalian bombesin. J. Am. Chem. Soc. 1981, 103:3178-3185.
65. Martinez V., Barquist E., Rivier J., Taché Y. Central CRF inhibits gastric empyting of a nutrient solid meal in rats: the role of CRF2 receptors. Am. J. Physiol. 1998, 274:G965-G970.
66. Martinez V., Rivier J., Tache Y. Peripheral injection of a new corticotropin-releasing factor (CRF) antagonist, astressin, blocks peripheral CRF- and abdominal surgery-induced delayed gastric emptying in rats. J. Pharmacol. Exp. There. 1999, 290:629-634.
67. Mazur A.W., Wang F., Tscheiner M., Donnelly E., Isfort R.J. Sauvagine analogs selective for corticotropin releasing factor 2 receptor: effect of substitutions at positions 35 and 39 on CRF2R selectivity. Peptides 2005, 26:887-891.
68. Menzaghi F., Howard R.L., Heinrichs S.C., Vale W., Rivier J., Koob G.F. Characterization of a novel and potent corticotropin-releasing factor antagonist in rats. J. Pharmacol. Exp. Ther. 1994, 269:564-572.
69. Miller C., Rivier J. Peptide chemistry: development of high-performance liquid chromatography and capillary zone electrophoresis. Biopolym. Pept. Sci. 1996, 40:265-317.
70. Miranda A., Koerber S.C., Gulyas J., Lahrichi S., Craig A.G., Corrigan A., Hagler A., Rivier C., Vale W.W., Rivier J.E. Conformationally restricted competitive antagonists of human/rat corticotropin-releasing factor. J. Med. Chem. 1994, 37:1450-1459.
71. Moeser A.J., Ryan K.A., Nighot P.K., Blikslager A.T. Gastrointestinal dysfunction induced by early weaning is attenuated by delayed weaning and mast cell blockade in pigs. Am. J. Physiol. Gastrointest. Liver Physiol. 2007, 293:G413-G421.
72. Monahan M., Amoss M., Anderson H., Vale W. Synthetic analogs of the hypothalamic luteinizing hormone releasing factor with increased agonist or antagonist properties. Biochemistry 1973, 12:4616-4620.
73. Montecucchi P.C., Gozzini L. Secondary structure prediction of sauvagine, a novel biologically active polypeptide from a frog. Int. J. Pept. Protein Res. 1982, 20:139-143.
74. Montecucchi P.C., Henschen A. Amino acid composition and sequence analysis of sauvagine, a new active peptide from skin of Phyllomedusa sauvagei. Int. J. Pept. Protein Res. 1981, 18:113-120.
75. Overman E., Rivier J., Moeser A. CRF induces intestinal epithelila barrier injury via the release of mast cell proteases and TNF-alpha. PLoS One 2012, 7:1-9.
76. Pallai P.V., Mabilia M., Goodman M., Vale W., Rivier J. Structural homology of corticotropin-releasing factor, sauvagine, and urotensin I: circular dichroism and prediction studies. Proc. Natl. Acad. Sci. U.S.A. 1983, 80:6770-6774.
77. Pecoraro N., Dallman M.F., Warne J.P., Ginsberg A.B., Laugero K.D., la Fleur S.E., Houshyar H., Gomez F., Bhargava A., Akana S.F. From Malthus to motive: how the HPA axis engineers the phenotype, yoking needs to wants. Prog. Neurobiol. 2006, 79:247-340.
78. Perrin M.H., Donaldson C., Chen R., Blount A., Berggren T., Bilezikjian L., Sawchenko P., Vale W.W. Identification of a second corticotropin-releasing factor receptor gene and characterization of a cDNA expressed in heart. Proc. Natl. Acad. Sci. U.S.A. 1995, 92:2969-2973.
79. Perrin M.H., Sutton S.W., Cervini L., Rivier J.E., Vale W.W. Comparison of an agonist, urocortin, and an antagonist, astressin, as radioligands for characterization of CRF receptors. J. Pharmacol. Exp. Ther. 1999, 288:729-734.
80. Potter E., Sutton S., Donaldson C., Chen R., Perrin M., Lewis K., Sawchenko P.E., Vale W.W. Distribution of corticotropin-releasing factor receptor mRNA expression in the rat brain and pituitary. Proc. Natl. Acad. Sci. U.S.A. 1994, 91:8777-8781.
81. Risbrough V.B., Hauger R.L., Roberts A., Vale W.W., Geyer M.A. CRF receptors CRF1 and CRF2 exert both additive and opposing influences on defensive startle behavior. J. Neurosci. 2004, 24:6545-6552.
82. Rivier, J., McClintock, R., 1989. Isolation and characterization of biologically active peptides and proteins using reversed-phase HPLC. The Use of HPLC in Receptor Biochemistry. Alan R. Liss, Inc., pp. 77-105.
83. Rivier, J., Burgus, R., Vale, W., 1971. 3-methyl-TRF, a synthetic analogue with specific activity greater than that of TRF. In: The Endocrine Society Meeting, Endocrinology.
84. Rivier C., Vale W., Guillemin R. An in vivo corticotropin-releasing factor (CRF) assay based on plasma levels of radio-immunoassayable ACTH. Proc. Soc. Exp. Biol. Med. 1973, 142:842-845.
85. Rivier J., Vale W., Burgus R., Ling N., Amoss M., Blackwell R., Guillemin R. Synthetic luteinizing hormone releasing factor analogs. Series of short-chain amide LRF homologs converging to the amino terminus. J. Med. Chem. 1973, 16:545-549.
86. Rivier J., Amoss M., Rivier C., Vale W. Synthetic luteinizing hormone releasing factor. Short chain analogs. J. Med. Chem. 1974, 17:230-233.
87. 8]-somatostatin: an analog of somatostatin more potent than the native molecule. Biochem. Biophys. Res. Commun. 1975, 65:746-751.
88. Rivier C., Brownstein M., Spiess J., Rivier J., Vale W. In vivo CRF-induced secretion of ACTH, β-endorphin and corticosterone. Endocrinology 1982, 110:272-278.
89. Rivier C., Rivier J., Vale W. Inhibition of adrenocorticotropic hormone secretion in the rat by immunoneutralization of corticotropin-releasing factor. Science 1982, 218:377-379.
90. Rivier, J., McClintock, R., Eksteen, R., Karger, B.L., 1982c. Reversed phase HPLC semipreparative purification of unprotected biologically active peptides: application to synthetic mixtures. In: Proceedings of the 1982 FDA-USP Workshop on Drug and Reference Standards for Insulins, Somatropins and Thyroid-axis Drugs. The United States Pharmacopeial Convention Inc., Rockville, MD, pp. 554-564.
91. Rivier C., Vale W., Rivier J. Effects of gonadotropin releasing hormone/agonists and antagonists on reproductive functions. J. Med. Chem. 1983, 26:1545-1550.
92. Rivier J., Spiess J., Vale W. Characterization of rat hypothalamic corticotropin-releasing factor. Proc. Natl. Acad. Sci. U.S.A. 1983, 80:4851-4855.
93. Rivier J., Rivier C., Vale W. Synthetic competitive antagonists of corticotropin releasing factor: effect on ACTH secretion in the rat. Science 1984, 224:889-891.
94. Rivier J., Rivier C., Galyean R., Miranda A., Miller C., Craig A.G., Yamamoto G., Brown M., Vale W. Single point D-substituted corticotropin releasing factor analogues: effects on potency and physicochemical characteristics. J. Med. Chem. 1993, 36:2851-2859.
95. Rivier J., Gulyas J., Corrigan A., Craig A.G., Martinez V., Taché Y., Vale W., Rivier C. Astressin analogues (CRF antagonists) with extended duration of action in the rat. J. Med. Chem. 1998, 41:5012-5019.
96. Rivier J.E., Kirby D.A., Lahrichi S.L., Corrigan A., Vale W.W., Rivier C.L. Constrained corticotropin releasing factor (CRF) antagonists (Astressin analogues) with long duration of action in the rat. J. Med. Chem. 1999, 42:3175-3182.
97. Rivier J., Gulyas J., Kirby D., Low W., Perrin M.H., Kunitake K., DiGruccio M., Vaughan J., Reubi J.C., Waser B., Koerber S.C., Martínez V., Wang L.X., Taché Y., Vale W. Potent and long acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists. J. Med. Chem. 2002, 45:4737-4747.
98. 1)-selective peptide agonist. J. Med. Chem. 2007, 50:1668-1674.
99. Rizo J., Sutton R.B., Breslau J., Koerber S.C., Porter J., Hagler A.T., Rivier J., Gierasch L.M. A novel conformation in a highly potent, constrained gonadotropin releasing hormone antagonist. J. Am. Chem. Soc. 1996, 118:970-976.
100. Rosenblatt M., Segre G.V., Potts J.T. Synthesis of a fragment of parathyroid hormone, bPTH-(28-48): an inhibitor of hormone cleavage in vivo. Biochemistry 1977, 16:2811-2816.
101. Rosenblatt M., Shepard G.L., Tyler G.A., Potts J.T. Modification of the arginines in parathyroid hormone: effect on biological activity. Biochemistry 1978, 17:3188-3191.
102. Rühmann A., Bonk I., Lin C.R., Rosenfeld M.G., Spiess J. Structural requirements for peptidic antagonists of the corticotropin-releasing factor receptor (CRFR): Development of CRFR2β-selective antisauvagine-30. Proc. Natl. Acad. Sci. U.S.A. 1998, 95:15264-15269.
103. Sapolsky R.M. Stress hormones: good and bad. Neurobiol. Dis. 2000, 7:540-542.
104. Slattery D.A., Hudson A.L., Nutt D.J. Invited review: the evolution of antidepressant mechanisms. Fund. Clin. Pharmacol. 2004, 18:1-21.
105. Slominski A., Zbytek B., Zmijewski M., Slominski R.M., Kauser S., Wortsman J., Tobin D.J. Corticotropin releasing hormone and the skin. Front. Biosci. 2006, 11:2230-2248.
106. Slominski, A.T., Zmijewski, M.A., Zbytek, B., Tobin, D.J., Theoharides, T.C., Rivier, J., 2013. Key role of CRF in the skin stress response system. Endocr. Rev. (in press).
107. Smith G.W., Aubry J.-M., Dellu F., Contarino A., Bilezikjian L.M., Gold L., Chen R., Marchuk Y., Hauser C., Bentley C.A., Sawchenko P.E., Koob G.F., Vale W., Lee K.-F. Corticotropin releasing factor receptor 1-deficient mice display decreased anxiety, an impaired stress response and aberrant neuroendocrine development. Neuron 1998, 20:1093-1102.
108. Smith F., Clark J.E., Overman B.L., Tozel C.C., Huang J.H., Rivier J.E., Blisklager A.T., Moeser A.J. Early weaning stress impairs development of mucosal barrier function in the porcine intestine. Am. J. Physiol. Gastrointest. Liver Physiol. 2010, 298:G352-G363.
109. Spiess J., Rivier J., Rivier C., Vale W. Primary structure of corticotropin-releasing factor from ovine hypothalamus. Proc. Natl. Acad. Sci. U.S.A. 1981, 78:6517-6521.
110. Spiess J., Rivier J., Vale W. Sequence analysis of rat hypothalamic corticotropin-releasing factor with the o-phthalaldehyde strategy. Biochemistry 1983, 22:4341-4346.
111. Spiess J., Dautzenberg F.M., Sydow S., Hauger R.L., Rühmann A., Blank T., Radulovic J. Molecular properties of the CRF receptor. Trends Endocrinol. Metabol. 1998, 9:140-145.
112. Stengel A., Tache Y. Corticotropin-releasing factor signaling and visceral response to stress. Exp. Biol. Med. (Maywood) 2010, 235:1168-1178.
113. Stenzel P., Kasterson R., Yeung W., Cone R.D., Rittenberg M.B., Stenzel-Poore M.P. Identification of a novel murine receptor for corticotropin-releasing hormone expressed in the heart. Mol. Endocrinol. 1995, 9:637-645.
114. Sternberg E.M. Emotions and disease: from balance of humors to balance of molecules. Nat. Med. 1997, 3:264-267.
115. Taché Y. Corticotropin releasing factor receptor antagonists: potential future therapy in gastroenterology?. Gut 2004, 53:919-921.
116. Taché Y., Perdue M.H. Role of peripheral CRF signalling pathways in stress-related alterations of gut motility and mucosal function. Neurogastroenterol. Motil. 2004, 16(Suppl. 1):137-142.
117. Tache Y., Martinez V., Million M., Wang L. Stress and the gastrointestinal tract III. Stress-related alterations of gut motor function: role of brain corticotropin-releasing factor receptors. Am. J. Physiol. Gastrointest. Liver Physiol. 2001, 280:G173-G177.
118. Taché Y., Brunnhuber S. From Hans Selye's discovery of biological stress to the identification of corticotropin-releasing factor signaling pathways: implication in stress-related functional bowel diseases. Ann. N.Y. Acad. Sci. 2008, 1148:29-41.
119. Tache Y., Kiank C., Stengel A. A role for corticotropin-releasing factor in functional gastrointestinal disorders. Curr. Gastroenterol. Rep. 2009, 11:270-277.
120. Tazi A., Dantzer R., LeMoal M., Rivier J., Vale W., Koob G.F. Corticotropin releasing factor antagonist blocks stress-induced fighting in rats. Regul. Pept. 1987, 18:37-42.
121. Tichomirowa M.A., Keck M.E., Schneider H.J., Paez-Pereda M., Renner U., Holsboer F., Stalla G.K. Endocrine disturbances in depression. J. Endocrinol. Invest. 2005, 28:89-99.
122. Vale W., Grant G., Amoss M., Blackwell R., Guillemin R. Culture of enzymatically dispersed anterior pituitary cells. Functional validation of a method. Endocrinology 1972, 91:562-572.
123. Vale W., Grant G., Rivier J., Monahan M., Amoss M., Blackwell R., Burgus R., Guillemin R. Synthetic polypeptide antagonists of the hypothalamic luteinizing hormone releasing factor. Science 1972, 176:933-934.
124. Vale W., Rivier C., Brown M., Leppaluoto J., Ling N., Monahan M., Rivier J. Pharmacology of hypothalamic regulatory peptides. Clin. Endocrinol. 1976, 5:261s-273s.
125. Vale W., Spiess J., Rivier C., Rivier J. Characterization of a 41-residue ovine hypothalamic peptide that stimulates the secretion of corticotropin and β-endorphin. Science 1981, 213:1394-1397.
126. Van Pett K., Viau V., Bittencourt J.C., Chan R.K.W., Li H.-Y., Arias C., Prins G.S., Perrin M., Vale W., Sawchenko P.E. Distribution of mRNAs encoding CRF receptors in brain and pituitary of rat and mouse. J. Comp. Neurol. 2000, 428:191-212.
127. Vita N., Laurent P., Lefort S., Chalon P., Lelias J.M., Kaghad M., Le F.G., Caput D., Ferrara P. Primary structure and functional expression of mouse pituitary and human brain corticotropin releasing factor receptors. FEBS Lett. 1993, 335:1-5.
128. Vulliémoz N.R., Xiao E., Xia-Zhang L., Rivier J., Ferin M. Astressin B, a nonselective corticotropin-releasing hormone receptor antagonist, prevents the inhibitory effect of ghrelin on luteinizing hormone pulse frequency in the ovariectomized rhesus monkey. Endocrinology 2008, 149:869-874.
129. Xiao E., Xia-Zhang L., Vulliemoz N., Rivier J., Ferin M. Astressin B, a corticotropin-releasing hormone receptor antagonist, accelerates the return to normal luteal function after an inflammatory-like stress challenge in the rhesus monkey. Endocrinology 2007, 148:841-848.
130. Yamada Y., Mizutani K., Mizusawa Y., Hantani Y., Tanaka M., Tanaka Y., Tomimoto M., Sugawara M., Imai N., Yamada H., Okajima N., Haruta J. New class of corticotropin-releasing factor (CRF) antagonists: small peptides having high binding affinity for CRF receptor. J. Med. Chem. 2004, 47:1075-1078.
131. Zhu J., Jiang Y., Xu G., Liu X. Intranasal administration: a potential solution for cross-BBB delivering neurotrophic factors. Histol. Histopathol. 2012, 27:537-548.
132. Zislis G., Desai T.V., Prado M., Shah H.P., Bruijnzeel A.W. Effects of the CRF receptor antagonist D-Phe CRF(12-41) and the alpha2-adrenergic receptor agonist clonidine on stress-induced reinstatement of nicotine-seeking behavior in rats. Neuropharmacology 2007, 53:958-966.
133. Zorrilla E.P., Koob G.F. Progress in corticotropin-releasing factor-1 antagonist development. Drug Discov. Today 2010, 15:371-383.