Journal article
Allosteric Modulation of the Dopamine D2 Receptor by Pro-Leu-Gly-NH2 Peptidomimetics Constrained in Either a Polyproline II Helix or a Type II β-Turn Conformation
Abstract
Type II beta-turn mimics and polyproline II helix mimics based upon diastereoisomeric 5.6.5 spiro bicyclic scaffolds have provided two pairs of Pro-Leu-Gly-NH(2) (PLG) peptidomimetics with contrasting dopamine receptor modulating activities. Compounds 1a and 3a were found to be positive allosteric modulators of the dopamine receptor, while the corresponding diastereoisomeric compounds 1b and 3b provided the first PLG peptidomimetics with the …
Authors
Raghavan B; Skoblenick KJ; Bhagwanth S; Argintaru N; Mishra RK; Johnson RL
Journal
Journal of Medicinal Chemistry, Vol. 52, No. 7, pp. 2043–2051
Publisher
American Chemical Society (ACS)
Publication Date
April 9, 2009
DOI
10.1021/jm801575w
ISSN
0022-2623
Associated Experts
Fields of Research (FoR)
Medical Subject Headings (MeSH)
Allosteric RegulationAnimalsBinding, CompetitiveCattleCorpus StriatumCrystallography, X-RayHeterocyclic Compounds, 2-RingIn Vitro TechniquesMSH Release-Inhibiting HormoneMolecular MimicryOligopeptidesPeptidesProtein Structure, SecondaryReceptors, Dopamine D2Spiro CompoundsStereoisomerismStructure-Activity RelationshipThiazolidines