Identification of 6H1 as a P2Y purinoceptor: P2Y5.
We have determined the identity of the orphan G-protein coupled receptor cDNA, 6H1, present in activated chicken T cells, as a subtype of P2Y purinoceptor. This identification is based on first on the degree of sequence identity shared with recently cloned members of the P2Y receptor family and second on the pharmacological profile. Upon transient expression in COS-7 cells the 6H1 receptor bound the radiolabel [35S]dATP alpha S specifically and with high affinity (Kd, 10 nM). This specific binding could be competitively displaced by a range of ligands active at P2 purinoceptors, with ATP being the most active (K (i)), 116 nM). Such competition studies have established the following rank order of activity: ATP ADP 2-methylthioATP alpha, beta-methylene ATP, UTP, thus confirming 6H1 as a member of the growing family of P2Y purinoceptors. As the fifth receptor of this type to be identified we suggest that it be named P2Y5.
Webb
T E
TE
Molecular Neurobiology Unit, Royal Free Hospital School of Medicine, London, United Kingdom.
Kaplan
M G
MG
Barnard
E A
EA
D000595:Amino Acid Sequence; D000818:Animals; D001667:Binding, Competitive; D002460:Cell Line; D002462:Cell Membrane / Q000378:metabolism; D002645:Chickens; D002522:Chlorocebus aethiops; D017124:Conserved Sequence; D003838:Deoxyadenine Nucleotides / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D008213:Lymphocyte Activation; D008969:Molecular Sequence Data; D010802:Phylogeny; D011869:Radioligand Assay; D011956:Receptors, Cell Surface / Q000096:biosynthesis / Q000235:genetics / Q000378:metabolism*; D043562:Receptors, G-Protein-Coupled; D018048:Receptors, Purinergic P2 / Q000096:biosynthesis / Q000235:genetics / Q000378:metabolism*; D011994:Recombinant Proteins / Q000096:biosynthesis / Q000378:metabolism; D017386:Sequence Homology, Amino Acid; D013462:Sulfur Radioisotopes; D013601:T-Lymphocytes / Q000276:immunology / Q000378:metabolism; D013873:Thionucleotides / Q000378:metabolism; D014162:Transfection; D049368:Receptors, Lysophosphatidic Acid
D003838:Deoxyadenine Nucleotides; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D018048:Receptors, Purinergic P2; D011994:Recombinant Proteins; D013462:Sulfur Radioisotopes; D013873:Thionucleotides; C082320:LPAR4 protein, human; D049368:Receptors, Lysophosphatidic Acid; C015109:2'-deoxyadenosine 5'-O-(1-thiotriphosphate)