Webb T E, Kaplan M G, Barnard E A
Molecular Neurobiology Unit, Royal Free Hospital School of Medicine, London, United Kingdom.
Biochem Biophys Res Commun. 1996 Feb 6;219(1):105-10. doi: 10.1006/bbrc.1996.0189.
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.
我们已经确定了活化鸡T细胞中存在的孤儿G蛋白偶联受体cDNA 6H1的身份，它是P2Y嘌呤受体的一个亚型。这一鉴定首先基于与P2Y受体家族最近克隆成员的序列同一性程度，其次基于药理学特征。6H1受体在COS-7细胞中瞬时表达时，能特异性且高亲和力地结合放射性标记物[35S]dATPαS（解离常数Kd为10 nM）。这种特异性结合可被一系列对P2嘌呤受体有活性的配体竞争性取代，其中ATP活性最强（抑制常数Ki为116 nM）。此类竞争研究确定了以下活性排序：ATP＞ADP＞2-甲硫基ATP＞α,β-亚甲基ATP＞UTP，从而证实6H1是不断增加的P2Y嘌呤受体家族的一员。作为此类被鉴定出的第五个受体，我们建议将其命名为P2Y5。
