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1: Bioconjug Chem. 2008 Feb;19(2):406-11. Epub 2008 Jan 5.
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Toward multivalent signaling across G protein-coupled receptors from poly(amidoamine) dendrimers.

Kim Y, Hechler B, Klutz AM, Gachet C, Jacobson KA.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.

Activation of the A2A receptor, a G protein-coupled receptor (GPCR), by extracellular adenosine, is antiaggregatory in platelets and anti-inflammatory. Multiple copies of an A2A 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.

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PMID: 18176997 [PubMed - indexed for MEDLINE]