Adenosine receptors as drug targets.
Adenosine receptors as drug targets.
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DOI：
10.1016/j.yexcr.2010.02.004
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发表时间：
2010-05-01
影响因子：
3.7
通讯作者：
Fredholm BB
中科院分区：
文献类型：
--
作者：
Fredholm BB
存在四种腺苷受体A1、A2 A、A2 B和A3，它们一起形成G蛋白偶联受体的限定亚组。它们被很好地保存并广泛表达。内源性激动剂腺苷在体液中的浓度最低（20 - 200 nM），足以轻微激活受体，这些受体在基底神经节、脂肪细胞和肾脏中高度表达。在这里腺苷可以发挥生理作用，在这里拮抗剂如咖啡因可以在健康个体中产生影响。腺苷水平在应激和痛苦中升高（在缺血中高达30 μM），并通过增加能量供应和减少细胞工作、刺激血管生成、介导预处理和对免疫活性细胞具有多种作用，倾向于将不良结果的风险降至最低。腺苷的这些病理生理作用也提供了一些潜在的药物靶点，但腺苷受体参与如此多的过程并不能简化药物开发。
There are four adenosine receptors, A1, A2A, A2B and A3, together forming a defined subgroup of G protein coupled receptors. They are well conserved and widely expressed. The endogenous agonist, adenosine, has a minimal concentration in body fluids (20 – 200 nM) that is sufficient to slightly activate the receptors where they are very highly expressed - as in the basal ganglia, on fat cells and in the kidney. Here adenosine can play a physiological role and here antagonists such as caffeine can have effects in healthy individuals. Adenosine levels rise in stress and distress (up to 30 μM in ischemia) and tend to minimize the risk for adverse outcomes by increasing energy supply and decreasing cellular work, by stimulating angiogenesis, mediating preconditioning and having multiple effects on immune competent cells. These pathophysiological roles of adenosine also offer some potential drug targets, but the fact that adenosine receptors are involved in so many processes does not simplify drug development.
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DOI：
10.1073/pnas.0810926105
发表时间：
2008-12-16
影响因子：
11.1
作者：
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DOI：
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发表时间：
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影响因子：
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作者：
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影响因子：
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影响因子：
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