CRF1 receptor

Overview

The CRF1 receptor, a.k.a. CRHR1, has been cloned from a variety of species ranging from fish to man [1,2,3,4,5,6,7,8,9,10,11]. The CRF₁ receptor is widely expressed in the central nervous system... [read more] with high levels of expression in cortex, cerebellum, hippocampus, basolateral amygdala, bed nucleus of thes stria terminalis, olfactory bulb and anterior pituitary [8,12,13]. In the periphery, CRF₁ receptor mRNA is expressed at low levels in the skin, ovary, testis and adrenal gland [4,8,14].

Binding and functional studies using cell lines recombinantly or endogenously expressing CRF₁ receptors revealed a distinct ligand-selective profile whereby human and ovine CRF, urocortin 1, urotensin I, and sauvagine all bind with high affinity to the mammalian CRF₁ receptor and activate the cyclic AMP signaling pathway [6,15,16,17]. In contrast, urocortin 2 and urocortin 3 do not bind to or activate CRF₁ receptors [18,19,20,21]. Therefore, CRF and urocortin 1 can be classified as the endogenous ligands for mammalian CRF₁ receptors.

References

1. Chen R, Lewis KA, Perrin MH, et al. Expression cloning of a human corticotropin-releasing-factor receptor. Proc Natl Acad Sci USA 1993;90:8967-71.
2. Chang CP, Pearse 2nd RV, O'Connell S, et al. Identification of a seven transmembrane helix receptor for corticotropin-releasing factor and sauvagine in mammalian brain. Neuron 1993;11:1187-95.
3. Perrin MH, Donaldson CJ, Chen R, et al. Cloning and functional expression of a rat brain corticotropin releasing factor (CRF) receptor. Endocrinology 1993;133:3058-61.
4. Vita N, Laurent P, Lefort S, et al. Primary structure and functional expression of mouse pituitary and human brain corticotrophin releasing factor receptors. FEBS Lett 1993;335:1-5.
5. Yu J, Xie LY, Abou-Samra AB. Molecular cloning of a type A chicken corticotropin-releasing factor receptor with high affinity for urotensin I. Endocrinology 1996;137:192-7.
6. Dautzenberg FM, Dietrich K, Palchaudhuri MR, et al. Identification of two corticotropin-releasing factor receptors from Xenopus laevis with high ligand selectivity: unusual pharmacology of the type 1 receptor. J Neurochem 1997;69:1640-9.
7. Myers DA, Trinh JV, Myers TR. Structure and function of the ovine type 1 corticotropin releasing factor receptor (CRF1) and a carboxyl-terminal variant. Mol Cell Endocrinol 1998;144:21-35.
8. Palchaudhuri MR, Wille S, Mevenkamp G, et al. Corticotropin-releasing factor receptor type 1 from Tupaia belangeri--cloning, functional expression and tissue distribution. Eur J Biochem 1998;258:78-84.
9. Arai M, Assil IQ, Abou-Samra AB. Characterization of three corticotropin-releasing factor receptors in catfish: a novel third receptor is predominantly expressed in pituitary and urophysis. Endocrinology 2001;142:446-54.
10. Pohl S, Darlison MG, Clarke WC, et al. Cloning and functional pharmacology of two corticotropin-releasing factor receptors from a teleost fish. Eur J Pharmacol 2001;430:193-202.
11. Oshida Y, Ikeda Y, Chaki S, et al. Monkey corticotropin-releasing factor1 receptor: Complementary DNA cloning and pharmacological characterization. Life Sci 2004;74:1911-1924.
12. Potter E, Sutton S, Donaldson C, et al. Distribution of corticotropin-releasing factor receptor mRNA expression in the rat brain and pituitary. Proc Natl Acad Sci USA 1994;91:8777-81.
13. Chalmers DT, Lovenberg TW, Grigoriadis DE, et al. Corticotrophin-releasing factor receptors: from molecular biology to drug design. Trends Pharmacol Sci 1996;17:166-72.
14. Nappi RE, Rivest S. 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 1995;53:1417-28.
15. Donaldson CJ, Sutton SW, Perrin MH, et al. Cloning and characterization of human urocortin. Endocrinology 1996;137:2167-70.
16. Dautzenberg FM, Py-Lang G, Higelin J, et al. Different binding modes of amphibian and human corticotropin-releasing factor type 1 and type 2 receptors: evidence for evolutionary differences. J Pharmacol Exp Ther 2001;296:113-20.
17. Perrin MH, Sutton SW, Cervini LA, et al. Comparison of an agonist, urocortin, and an antagonist, astressin, as radioligands for characterization of corticotropin-releasing factor receptors. J Pharmacol Exp Ther 1999;288:729-34.
18. Lewis K, Li C, Perrin MH, et al. 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 USA 2001;98:7570-5.
19. Reyes TM, Lewis K, Perrin MH, et al. Urocortin II: a member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc Natl Acad Sci USA 2001;98:2843-8.
20. Hsu SY, Hsueh AJ. Human stresscopin and stresscopin-related peptide are selective ligands for the type 2 corticotropin-releasing hormone receptor. Nat Med 2001;7:605-11.
21. Dautzenberg FM, Gutknecht E, Van der Linden I, et al. Cell type specific calcium signaling by corticotropin-releasing factor type 1 (CRF1) and 2a (CRF2(a)) receptors: Gq coupling in human embryonic kidney 293 but not SK-N-MC neuroblastoma cells. Biochem Pharmacol 2004;68:1833-1844.

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