Molecular identification and analysis of a novel human corticotropin-releasing factor (CRF) receptor: the CRF2gamma receptor

We report the discovery of a new CRF2 receptor splice isoform found in human brain, which we have termed the CRF2gamma receptor. The CRF2gamma cDNA encodes for a 397-amino acid receptor that has an amino terminus with no significant homology to the already reported alpha- and beta-termini. When expr...

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Bibliographic Details
Published in:Molecular endocrinology (Baltimore, Md.) Md.), 1998-08, Vol.12 (8), p.1077-1085
Main Authors: Kostich, W A, Chen, A, Sperle, K, Largent, B L
Format: Article
Language:English
Subjects:
Amino Acid Sequence
Amygdala - metabolism
Base Sequence
Brain - metabolism
Central Nervous System - metabolism
Cloning, Molecular
Corticotropin-Releasing Hormone - metabolism
Corticotropin-Releasing Hormone - pharmacology
Humans
Isomerism
Molecular Sequence Data
Receptors, Corticotropin-Releasing Hormone - drug effects
Receptors, Corticotropin-Releasing Hormone - genetics
Receptors, Corticotropin-Releasing Hormone - metabolism
RNA, Messenger
Tissue Distribution
Urocortins
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Summary:We report the discovery of a new CRF2 receptor splice isoform found in human brain, which we have termed the CRF2gamma receptor. The CRF2gamma cDNA encodes for a 397-amino acid receptor that has an amino terminus with no significant homology to the already reported alpha- and beta-termini. When expressed in 293-EBNA (Epstein-Barr nuclear antigen) cells, the CRF2gamma receptor responds in a dose-dependent manner to CRF and related peptides with a rank order of potency of urocortin > or = sauvagine>urotensin>r/h CRF, with EC50 values more similar to CRF2alpha than CRF2beta. Equilibrium saturation isotherm analysis with radiolabeled sauvagine reveals a two site/state model for binding to CRF2gamma with a 60 pM Kd high-affinity site and a 5 nM Kd low-affinity site. Analysis of CRF2gamma RNA expression in human brain demonstrates expression in septum and hippocampus, with weaker but detectable expression in amygdala, nucleus accumbens, midbrain, and frontal cortex.
ISSN:0888-8809