Biomedical sciences publications
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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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Alphaviruses: Population Genetics and Determinants of Emergence
This review discusses the ecology, epidemiology and molecular virology of the alphaviruses, then focuses on three of the most important members of the genus.
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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.
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Nociceptin/Orphanin FQ Inhibition with SB612111 Ameliorates Dextran Sodium Sulfate-Induced Colitis
In this study, we asked whether the small molecule N/OFQ antagonist (−)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB612111) would inhibit the development of dextran sodium sulfate-induced colitis in C57BL/6 mice.
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Radiosynthesis of a 125I Analog of a Highly Selective Alpha3beta4 Nicotinic Acetylcholine Receptor Antagonist Ligand for Use in Autoradiography Studies
Our laboratory has discovered a series of very high affinity and highly selective ligands for the α3β4 nAChR subtype. We now report the synthesis of a radiolabeled 125I analog of N-(2-iodophenyl)-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine (AT-1012), a…
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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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Effects of Bacterial and Presystemic Nitroreductase Metabolism of 2-Chloro-5-Nitro-N-Phenylbenzamide on its Mutagenicity and Bioavailability
Studies were initiated to assess its bacterial mutagenicity and pharmacokinetic profile in two animal species prior to subchronic oral toxicity evaluations and the results are reported here.