Biomedical sciences publications
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Trace Amine-Associated Receptor 1 Partial Agonism Reveals Novel Paradigm for Neuropsychiatric Therapeutics
Here we report on the identification and characterization of the first selective and potent TAAR1 partial agonist.
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Comparative Analysis of the Substrate Preferences of Two Post-Proline Cleaving Endopeptidases, Prolyl Oligopeptidase and Fibroblast Activation Protein Alpha
Post-proline cleaving peptidases are promising therapeutic targets for neurodegenerative diseases, psychiatric conditions, metabolic disorders, and many cancers.
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Lead Optimization of Antimalarial Propafenone Analogues
Careful examination of the bioavailability, pharmacokinetics, toxicology, and efficacy of this series of compounds using rodent models revealed orally bioavailable compounds that are nontoxic and suppress parasitemia in vivo.
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Fyn Promotes Th17 Differentiation by Regulating the Kinetics of RORγt and Foxp3 Expression
In this study, we show evidence that the Src family tyrosine kinase Fyn helps regulate this Th17/TREG balance.
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Discovery and Optimization of Benzotriazine Di-N-Oxides Targeting Replicating and Nonreplicating Mycobacterium Tuberculosis
These data along with measurements of the physiochemical properties and pharmacokinetic profile demonstrate that BTOs have the potential to be developed into a new class of antitubercular drugs.
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Anterograde Episodic Memory in Korsakoff Syndrome
In this review we highlight the historical studies that examined anterograde episodic memory processes in KS, present a timeline and evidence supporting the myriad theories proffered to account for this…
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The Stereoselective Sulfate Conjugation of 4′-Methoxyfenoterol Stereoisomers by Sulfotransferase Enzymes
The presystemic sulfate conjugation of the stereoisomers of 4′-methoxyfenoterol, (R,R′)-MF, (S,S′)-MF, (R,S′)-MF, and (S,R′)-MF, was investigated using commercially available human intestinal S9 fractions, a mixture of sulfotransferase (SULT) enzymes.
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Genome-Wide Meta-analyses of Smoking Behaviors in African Americans
Here we report results of the first genome-wide association study meta-analysis of smoking behavior in African Americans in the Study of Tobacco in Minority Populations Genetics Consortium.
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Synthesis of a 35S-Labeled Dinucleoside Phosphorothioate Prodrug, an Orally Bioavailable Anti-HBV Agent
The 35S-labeled, dinucleoside phosphorothioate 1, an orally available agent against hepatitis B virus, was prepared in eight steps with high specific activity and radiochemical purity.
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Smoking and Genetic Risk Variation Across Populations of European, Asian, and African American Ancestry–a Meta-Analysis of Chromosome 15q25
We demonstrate association between smoking quantity and markers in the chromosome 15q25 region across all three populations, and narrow the region of association.
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Metabolism, Pharmacokinetics, Tissue Distribution, and Stability Studies of the Prodrug Analog of an Anti-Hepatitis B Virus Dinucleoside Phosphorothioate
The preferential distribution of the dinucleotide 1 and its prodrug 2 into liver may be attributed to the presence of nucleoside phosphorothioate backbone because phosphorothioate oligonucleotides also reveal a similar…
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Bulged DNA Substrates for Identifying Poxvirus Resolvase Inhibitors
We report an assay for resolvase cleavage activity based on fluorescence polarization (FP) for high-throughput screening and mechanistic studies.