Beilstein J. Org. Chem.2013,9, 204–214, doi:10.3762/bjoc.9.24
/bjoc.9.24 Abstract A variety of stable, small-molecule peptidomimetic ligands have been developed to elucidate the mechanism by which the neuropeptide Pro-Leu-Gly-NH2 (PLG) modulates dopaminergic neurotransmission. Photoaffinity labeling ligands based upon PLG peptidomimetics have been used to
changes in the spiro-bicyclic dopamine receptor modulators are capable of causing major changes in the modulatory activity of PLG peptidomimetics.
Keywords: allosteric modulation; dopamine D2 receptor; peptidomimetic; Pro-Leu-Gly-NH2; spiro-bicyclic scaffold; Review
There has been an increasing effort
neuropeptide Pro-Leu-Gly-NH2 (PLG) has been shown to be a positive allosteric modulator of the dopamine D2 receptor [3]. PLG was initially isolated from brain tissue in the search for hypothalamic releasing factors, wherein it was found to inhibit the release of melanocyte stimulating hormone from the
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Graphical Abstract
Figure 1:
PLG peptidomimetic design approach. The Φ2, ψ2, Φ3, and ψ3 torsion angles define the postulated β-t...