2020
Design, Synthesis, and Characterization of Benzimidazole Derivatives as Positron Emission Tomography Imaging Ligands for Metabotropic Glutamate Receptor 2
Yuan G, Qu X, Zheng B, Neelamegam R, Afshar S, Iyengar S, Pan C, Wang J, Kang H, Ondrechen M, Poutiainen P, Fakhri G, Zhang Z, Brownell A. Design, Synthesis, and Characterization of Benzimidazole Derivatives as Positron Emission Tomography Imaging Ligands for Metabotropic Glutamate Receptor 2. Journal Of Medicinal Chemistry 2020, 63: 12060-12072. PMID: 32981322, PMCID: PMC8629109, DOI: 10.1021/acs.jmedchem.0c01394.Peer-Reviewed Original ResearchConceptsPotential positron emission tomographyBenzimidazole derivativesPositron emission tomography imaging ligandsExcellent selectivityImaging ligandsPositive allosteric modulatorsRadiochemical yieldBinding affinityMetabotropic glutamate receptor 2C]methyl iodideMolar activityLigandDerivativesRadiochemical purityGlutamate receptor 2Brain regionsAllosteric modulatorsPositron emission tomographyC]methylationRadiochemicalIodideBrain uptakeMGluR subtypesCompoundsBinding
2016
Discovery of a Highly Selective Glycogen Synthase Kinase‐3 Inhibitor (PF‐04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging
Liang S, Chen J, Normandin M, Chang J, Chang G, Taylor C, Trapa P, Plummer M, Para K, Conn E, Lopresti‐Morrow L, Lanyon L, Cook J, Richter K, Nolan C, Schachter J, Janat F, Che Y, Shanmugasundaram V, Lefker B, Enerson B, Livni E, Wang L, Guehl N, Patnaik D, Wagner F, Perlis R, Holson E, Haggarty S, Fakhri G, Kurumbail R, Vasdev N. Discovery of a Highly Selective Glycogen Synthase Kinase‐3 Inhibitor (PF‐04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging. Angewandte Chemie International Edition 2016, 55: 9601-9605. PMID: 27355874, PMCID: PMC4983481, DOI: 10.1002/anie.201603797.Peer-Reviewed Original ResearchConceptsGlycogen synthase kinase-3Tau phosphorylationPET neuroimagingPET imaging studiesModulation of tau phosphorylationNon-human primatesRegulate multiple cellular processesModulates tau phosphorylationMultiple cellular processesBrainBrain permeabilityImaging studiesCellular processesDisplaceable bindingKinase-3