Molecular identification and pharmacological profile of the bovine kinin B1 receptor.
To support the study of kinin pharmacology in bovine models of cultured endothelial cells (ECs), the Bovine Genome Project was searched for a B1 receptor (B1R) gene ortholog (BDKRB1). A contig complementary to an intronless coding nucleotide sequence was found. The sequence was amplified from bovine EC DNA, further cloned into pcDNA3 and expressed in COS-1 cells. The bovine B1R sequence was confirmed and extended. A putative Zn2+-binding motif HEXXH is not present (replaced by HDAWP). The receptor binds [3H]Lys-des-Arg9-bradykinin in a saturable manner (K(d) 0.36 nM) and exhibits a pharmacological profile similar to that of human B(1)R.
Morissette
Guillaume
G
Centre de Recherche en Rhumatologie et Immunologie, Centre Hospitalier Universitaire de Québec, Québec City G1V 4G2, Canada.
Marceau
François
F
D000595:Amino Acid Sequence; D000818:Animals; D001667:Binding, Competitive; D001920:Bradykinin / Q000494:pharmacology*; D019556:COS Cells; D002417:Cattle; D002478:Cells, Cultured; D002522:Chlorocebus aethiops; D003001:Cloning, Molecular; D042783:Endothelial Cells / Q000187:drug effects; D006801:Humans; D008969:Molecular Sequence Data; D011485:Protein Binding; D043783:Receptor, Bradykinin B1 / Q000187:drug effects* / Q000235:genetics* / Q000378:metabolism
D043783:Receptor, Bradykinin B1; D001920:Bradykinin