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The structure and function of A1 and A2B adenosine receptors.

机译:A1和A2B腺苷受体的结构和功能。

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Of the four G protein coupled adenosine receptor (AR) subtypes, the A1 is best suited for studies of reconstitution with G proteins. Recombinant A1 receptors extended with hexahistidine and FLAG have been purified to near homogeneity. In reconstitution assays using pure recombinant G protein subunits, the composition of the gamma subunit influences coupling to purified A1ARs. The least well characterized AR is the A2B. New data indicate that A(2B)ARs can trigger the degranulation of canine and human mast cell lines. Recombinant human A(2B)ARs are blocked by the anti-asthma drugs theophylline and enprofylline at concentrations that are used therapeutically to treat asthma. Although A(2B)ARs have long been known to stimulate adenylyl cyclase, they also can activate phospholipase C and mobilize Ca2+ by signaling through Gq/11. There is great potential for new therapies based on compounds that selectively target individual AR subtypes.
机译:在四种G蛋白偶联的腺苷受体(AR)亚型中,A1最适合用于G蛋白的重组研究。用六组氨酸和FLAG延伸的重组A1受体已纯化至接近均一。在使用纯重组G蛋白亚基的重组测定中,γ亚基的组成影响与纯化A1AR的偶联。表征最差的AR是A2B。新数据表明,A(2B)ARs可以触发犬和人肥大细胞系的脱粒。重组人A(2B)ARs被抗哮喘药物茶碱和Enprofylline所阻断,其浓度可用于治疗哮喘。尽管早就知道A(2B)ARs会刺激腺苷酸环化酶,但它们也可以激活磷脂酶C并通过Gq / 11发出信号来动员Ca2 +。基于选择性靶向单个AR亚型的化合物的新疗法具有巨大潜力。

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