Toward multivalent signaling across G protein-coupled receptors from poly(amidoamine) dendrimers
Toward multivalent signaling across G protein-coupled receptors from poly(amidoamine) dendrimers
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DOI：
10.1021/bc700327u
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发表时间：
2008-02-01
影响因子：
4.7
通讯作者：
Jacobson, Kenneth A.
中科院分区：
文献类型：
--
作者：
Kim, Yoonkyung;Hechler, Beatrice;Jacobson, Kenneth A.
细胞外腺苷对A（2A）受体（一种G蛋白偶联受体（GPCR））的激活具有抗血小板聚集和抗炎作用。多拷贝的A（2A）激动剂，核苷CGS 21680，共价偶联到PAMAM树枝状聚合物和光谱表征。荧光PAMAM-CGS 21680缀合物5抑制洗涤的人血小板的聚集并被内化。我们设想，与单价GPCR配体相比，我们的多价树枝状聚合物缀合物可以改善整体药理学特征。
Activation of the A(2A) receptor, a G protein-coupled receptor (GPCR), by extracellular adenosine, is antiaggregatory in platelets and anti-inflammatory. Multiple copies of an A(2A) agonist, the nucleoside CGS21680, were coupled covalently to PAMAM dendrimers and characterized spectroscopically. A fluorescent PAMAM-CGS21680 conjugate 5 inhibited aggregation of washed human platelets and was internalized. We envision that our multivalent dendrimer conjugates may improve overall pharmacological profiles compared to the monovalent GPCR ligands.