2017
Brain Penetration of the ROS1/ALK Inhibitor Lorlatinib Confirmed by PET
Collier T, Maresca K, Normandin M, Richardson P, McCarthy T, Liang S, Waterhouse R, Vasdev N. Brain Penetration of the ROS1/ALK Inhibitor Lorlatinib Confirmed by PET. Molecular Imaging 2017, 16: 1536012117736669. PMID: 29067878, PMCID: PMC5661750, DOI: 10.1177/1536012117736669.Peer-Reviewed Original ResearchConceptsPositron emission tomographyLung cancerTreatment of non-small-cell lung cancerBrain metastases of patientsNon-small-cell lung cancerPositron emission tomography evaluationNonhuman primatesRodent tumor modelsGoal of clinical translationOptimal therapeutic outcomesMetastasis of patientsBlood-brain barrierBrain metastasesPF-06463922Preclinical modelsClinical trial investigatorsTumor modelMolecular alterationsLorlatinibTherapeutic outcomesCancer therapeuticsBrain penetrationClinical translationEmission tomographyTrial investigators
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