Identification of 6H1 as a P2Y purinoceptor: P2Y5.
Identification of 6H1 as a P2Y purinoceptor: P2Y5.
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6H1 鉴定为 P2Y 嘌呤受体：P2Y5。
DOI：
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发表时间：
1996
期刊：
影响因子：
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通讯作者：
E. Barnard
中科院分区：
文献类型：
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作者：
T. E. Webb;Mark G. Kaplan;E. Barnard
我们已经确定了存在于激活的鸡T细胞中的孤儿G蛋白偶联受体cDNA6H1是P2Y嘌呤受体的一种亚型。这种鉴定首先基于与最近克隆的P2Y受体家族成员的序列同源性程度，其次基于药理学特征。6H1受体在COS-7细胞中瞬时表达时，与放射性标记[35S]dATPαS特异性结合，并具有高亲和力(Kd，10 nM)。这种特异性结合可以被一系列活跃在P2嘌呤受体上的配体竞争性地取代，其中ATP是最活跃的(K(I))，116 nM。这样的竞争研究已经建立了以下活性等级顺序：ATPADP2-甲硫基三磷酸腺苷α，β-亚甲基三磷酸腺苷，UTP，从而证实6H1是正在成长的P2Y嘌呤受体家族的成员。作为第五个被鉴定的该类型受体，我们建议将其命名为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.