P2Y nucleotide receptors: promise of therapeutic applications.

P2Y nucleotide receptors: promise of therapeutic applications.
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DOI:
10.1016/j.drudis.2010.05.011
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发表时间:
2010-07
影响因子:
7.4
通讯作者:
Boeynaems, Jean-Marie
Boeynaems, Jean-Marie
中科院分区:
医学2区
文献类型:
--
作者:
Jacobson, Kenneth A.;Boeynaems, Jean-Marie

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细胞外核苷酸,例如 ATP 和 UTP,通过一类 G 蛋白偶联受体(称为 P2Y)具有独特的信号传导作用。然而,受体配体通常是体内生物利用度和稳定性较低的带电分子。 P2Y 受体选择性激动剂和拮抗剂的开发以及基因敲除小鼠研究的最新进展导致基于这些受体的新药物概念的产生。该领域的快速进展已经产生了治疗囊性纤维化、干眼病和血栓形成的候选药物。心血管疾病、炎症性疾病和神经退行性疾病的新疗法即将出现。
Extracellular nucleotides, such as ATP and UTP, have distinct signaling roles through a class of G protein-coupled receptors, termed P2Y. However, the receptor ligands are typically charged molecules of low bioavailability and stability in vivo. Recent progress in the development of selective agonists and antagonists for P2Y receptors and study of knockout mice have led to new drug concepts based on these receptors. The rapidly accelerating progress in this field has already resulted in drug candidates for cystic fibrosis, dry eye disease, and thrombosis. On the horizon are novel treatments of cardiovascular diseases, inflammatory diseases, and neurodegeneration.
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