Toward multivalent signaling across G protein-coupled receptors from poly(amidoamine) dendrimers.

ABSTRACT: 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.

SUBMITTER: Kim Y 

PROVIDER: S-EPMC10150582 | biostudies-literature | 2008 Feb

REPOSITORIES: biostudies-literature