Toward Multivalent Signaling across G Protein-Coupled Receptors from Poly(amidoamine) Dendrimers

详细信息    查看全文

• 作者：Yoonkyung Kim ; B&#xe9 ; atrice Hechler ; Athena M. Klutz ; Christian Gachet ; Kenneth A. Jacobson
• 刊名：Bioconjugate Chemistry
• 出版年：2008
• 出版时间：February 2008
• 年：2008
• 卷：19
• 期：2
• 页码：406 - 411
• 全文大小：700K
• 年卷期：v.19,no.2(February 2008)
• ISSN：1520-4812

文摘

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.