Biomedical sciences publications
-
Cortical nNOS Neurons Co-Express the NK1 Receptor and are Depolarized by Substance P in Multiple Mammalian Species
To evaluate the degree of co-expression of nNOS and NK1 in the cortex among mammals, we used double immunofluorescence for nNOS and NK1 and determined the anatomical distribution in mouse,…
-
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.
-
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.
-
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.
-
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.
-
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.
-
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…
-
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.
-
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.
-
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.
-
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…
-
N-Glycan Cryptic Antigens as Active Immunological Targets in Prostate Cancer Patients
We report here a carbohydrate microarray analysis of a number of tumor-associated carbohydrates for their serum antibody reactivities and potential immunogenicity in humans