Molecular cloning and pharmacological characterization of bovine calcitonin receptor-like receptor from bovine aortic endothelial cells

Biochem Pharmacol. 2002 Jun 1;63(11):1949-59. doi: 10.1016/s0006-2952(02)00990-5.

Abstract

A complementary DNA encoding calcitonin receptor-like receptor (CRLR) was isolated from a bovine aortic endothelial cell library. The bovine CRLR has 462 amino acids and 92% homology with the human CRLR. In a reverse transcriptase-polymerase chain reaction assay, bovine CRLR was found to be widely distributed, including in the heart and lungs. Stable transfection of bovine CRLR in human embryonic kidney cells (HEK-293) resulted in specific high-affinity [125I] rat adrenomedulin (rADM)-binding (dissociation constant=145+/-15 pM). ADM-stimulated adenylyl cyclase activity with an EC50 value of 5.0+/-1.2 nM. The human ADM receptor antagonist hADM(22-52) inhibited [125I]rADM-binding and ADM-stimulated adenylyl cyclase activity. Interactions between bovine CRLR and individual receptor activity modifying proteins (RAMPs) were also investigated. Transient co-transfection of bovine CRLR cDNA with human receptor activity modifying protein 1 (hRAMP1) cDNA in HEK-293 cells resulted in the expression of a CRLR that displayed high-affinity binding to calcitonin gene-related peptide. Co-transfection of bovine CRLR with human RAMP2 or RAMP3 cDNAs in HEK-293 cells displayed high-affinity ADM receptors. These observations suggest that in the absence of exogenous RAMPs heterologous expression of bovine CRLR results in an ADM receptor phenotype.

MeSH terms

  • Adrenomedullin
  • Amino Acid Sequence
  • Animals
  • Aorta / cytology
  • Calcitonin Receptor-Like Protein
  • Cattle
  • Cells, Cultured
  • Cloning, Molecular
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / metabolism*
  • Humans
  • Intracellular Signaling Peptides and Proteins
  • Membrane Proteins / metabolism
  • Molecular Sequence Data
  • Peptides / pharmacology
  • Receptor Activity-Modifying Protein 2
  • Receptor Activity-Modifying Protein 3
  • Receptor Activity-Modifying Proteins
  • Receptors, Adrenomedullin
  • Receptors, Calcitonin / genetics*
  • Receptors, Calcitonin / metabolism
  • Receptors, Peptide / drug effects
  • Receptors, Peptide / metabolism*
  • Reverse Transcriptase Polymerase Chain Reaction
  • Sequence Homology, Amino Acid

Substances

  • CALCRL protein, human
  • Calcitonin Receptor-Like Protein
  • Calcrl protein, rat
  • Intracellular Signaling Peptides and Proteins
  • Membrane Proteins
  • Peptides
  • RAMP2 protein, human
  • RAMP3 protein, human
  • Ramp2 protein, rat
  • Ramp3 protein, rat
  • Receptor Activity-Modifying Protein 2
  • Receptor Activity-Modifying Protein 3
  • Receptor Activity-Modifying Proteins
  • Receptors, Adrenomedullin
  • Receptors, Calcitonin
  • Receptors, Peptide
  • Adrenomedullin