Can I read The ligand‐selective Domains of Corticotropin‐Releasing Factor Type 1 and Type 2 Receptor Reside in Different Extracellular Domains: Generation of Chimeric Receptors with a Novel Ligand‐Selective Profile on EtoBox?

The ligand‐selective Domains of Corticotropin‐Releasing Factor Type 1 and Type 2 Receptor Reside in Different Extracellular Domains: Generation of Chimeric Receptors with a Novel Ligand‐Selective Profile by Frank M. Dautzenberg; Gavin J. Kilpatrick; Sandra Wille; Richard L. Hauger is a Neuroscience article available to read on EtoBox.

What is The ligand‐selective Domains of Corticotropin‐Releasing Factor Type 1 and Type 2 Receptor Reside in Different Extracellular Domains: Generation of Chimeric Receptors with a Novel Ligand‐Selective Profile about?

Abstract : The nonselective human corticotropin‐releasing factor (hCRF) receptor 1 (hCRFR1) and the ligand‐selective __Xenopus__ CRFR1 (xCRFR1), xCRFR2, and hCRFR2α were compared. To understand the interactions of hCRF, ovine CRF (oCRF), rat urocortin (rUcn), and sauvagine, ligands with different affinities for type 1 and type 2 CRFRs, chimeric and mutant receptors of hCRFR1, xCRFR1, hCRFR2α, and xCRFR2 were constructed. In cyclic AMP stimulation and CRF‐binding assays, it was established that different extracellular regions of CRFR1 and CRFR2 conferred their ligand selectivities. The ligand selectivity of xCRFR1 resided in five N‐terminal amino acids, whereas the N‐terminus of both CRFR2 proteins did not contribute to their ligand selectivities. Chimeric receptors in which the first extracellular domain of hCRFR1 replaced that of hCRFR2α or xCRFR2 showed a similar pharmacological profile to the two parental CRFR2 molecules. Chimeric receptors carrying the N‐terminal domain of xCRFR1 linked to hCRFR2α or xCRFR2 displayed a novel pharmacological profile. hCRF, rUcn, and sauvagine were bound with high affinity, whereas oCRF was bound with low affinity. Furthermore, when three or five

Who reads The ligand‐selective Domains of Corticotropin‐Releasing Factor Type 1 and Type 2 Receptor Reside in Different Extracellular Domains: Generation of Chimeric Receptors with a Novel Ligand‐Selective Profile?

Author

Frank M. Dautzenberg; Gavin J. Kilpatrick; Sandra Wille; Richard L. Hauger

Publisher

John Wiley and Sons; Wiley (Blackwell Publishing); Blackwell Publishing Inc.; Wiley (ISSN 0022-3042)

Published

1999

Language

EN

Field

Neuroscience (Life Sciences)