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PNA-Based Multivalent Scaffolds Activate the Dopamine D2 Receptor. | LitMetric

PNA-Based Multivalent Scaffolds Activate the Dopamine D2 Receptor.

ACS Med Chem Lett

Laboratory of Bioorganic Chemistry, NIDDK, and Molecular Neuropharmacology Section, NINDS, National Institutes of Health, Bethesda, Maryland 20892, United States.

Published: April 2015

AI Article Synopsis

Article Abstract

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 each construct was assessed, and the multivalent effects were evaluated.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4394337PMC
http://dx.doi.org/10.1021/ml500478mDOI Listing

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