P2Y11 Receptors: Properties, Distribution and Functions
P2Y11 Receptors: Properties, Distribution and Functions
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DOI：
10.1007/5584_2017_89
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发表时间：
2017-01-01
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影响因子：
--
通讯作者：
Kennedy, Charles
中科院分区：
文献类型：
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作者：
Kennedy, Charles
P2 Y（11）受体是一种G蛋白偶联受体，受内源性嘌呤核苷酸（特别是ATP）刺激。在P2 Y受体中，它具有几个独特的性质;（1）它是唯一在编码序列中含有内含子的人类P2 Y受体基因;（2）该基因似乎不存在于啮齿动物基因组中;（3）它与磷脂酶C和腺苷酸环化酶的刺激偶联。由于在小鼠和大鼠中缺乏它，沿着有限的选择性药理学工具，阻碍了我们对其性质和功能的认识和理解的发展。尽管如此，通过谨慎使用可用工具、使用siRNA抑制受体表达和SNP遗传筛选的组合，已经在多种人类细胞和组织中鉴定了天然P2 Y（11）受体的可能功能。许多是在参与炎症反应的血细胞中，这与细胞外ATP是免疫系统中与损伤相关的信号分子相一致。因此，提出的潜在治疗应用主要涉及急性和慢性炎症反应的调节。
The P2Y(11) receptor is a G protein-coupled receptor that is stimulated by endogenous purine nucleotides, particularly ATP. Amongst P2Y receptors it has several unique properties; (1) it is the only human P2Y receptor gene that contains an intron in the coding sequence; (2) the gene does not appear to be present in the rodent genome; (3) it couples to stimulation of both phospholipase C and adenylyl cyclase. Its absence in mice and rats, along with a limited range of selective pharmacological tools, has hampered the development of our knowledge and understanding of its properties and functions. Nonetheless, through a combination of careful use of the available tools, suppression of receptor expression using siRNA and genetic screening for SNPs, possible functions of native P2Y(11) receptors have been identified in a variety of human cells and tissues. Many are in blood cells involved in inflammatory responses, consistent with extracellular ATP being a damage-associated signalling molecule in the immune system. Thus proposed potential therapeutic applications relate, in the main, to modulation of acute and chronic inflammatory responses.