PNA-Based Multivalent Scaffolds Activate the Dopamine D2 Receptor.
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ABSTRACT:
SUBMITTER: Dix AV
PROVIDER: S-EPMC4394337 | biostudies-literature | 2015 Apr
REPOSITORIES: biostudies-literature
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PNA-Based Multivalent Scaffolds Activate the Dopamine D2 Receptor.
Dix Andrew V AV Conroy Jennie L JL George Rosenker Kara M KM Sibley David R DR Appella Daniel H DH
ACS medicinal chemistry letters 20150313 4
Peptide nucleic acid scaffolds represent a promising tool to interrogate the multivalent effects of ligand binding to a membrane receptor. Dopamine D2 receptors (D2R) are a class of G-protein coupled receptors (GPCRs), and the formation of higher-ordered structures of these receptors has been associated with the progression of several neurological diseases. In this Letter, we describe the synthesis of a library of ligand-modified PNAs bearing a known D2R agonist, (±)-PPHT. The D2R activity for e ...[more]
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