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Medicinal Chemistry Scholarly Works: Recent submissions
Now showing items 221-240 of 255
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(4R,4aR,6S,7S,7aS)-6-Hydroxy-7-hy- droxymethyl-4-methylperhydrocyclo- penta[c]pyran-1-one chloroform solvate from Valeriana laxiflora
(International Union of Crystallography, 2004)The structure of an iridolactone isolated from Valeriana laxiflora was established as (4R,4aR,6S,7S,7aS)-6-hydroxy-7-hydroxymethyl-4-methylperhydrocyclopenta[c]pyran-1-one chloroform solvate, C10H16O4·CHCl3. The ... -
Development of a Cell-Based, High-Throughput Screening Assay for Cholesterol Efflux Using a Fluorescent Mimic of Cholesterol
(Mary Ann Liebert, Inc., 2011-04)Reverse cholesterol transport is the process by which extrahepatic cells, including macrophage-derived foam cells in arterial atherosclerotic plaque, transport excessive cholesterol back to the liver for bile acid synthesis ... -
Lethal Mutagenesis of Poliovirus Mediated by a Mutagenic Pyrimidine Analogue
(American Society for Microbiology, 2007-10)Lethal mutagenesis is the mechanism of action of ribavirin against poliovirus (PV) and numerous other RNA viruses. However, there is still considerable debate regarding the mechanism of action of ribavirin against a variety ... -
Synthetic mimics of mammalian cell surface receptors: prosthetic molecules that augment living cells
(Royal Society of Chemistry, 2005-09-08)Specific receptors on the surface of mammalian cells actively internalize cell-impermeable ligands by receptor-mediated endocytosis. To mimic these internalizing receptors, my laboratory is studying artificial cell surface ... -
High-Throughput Screen of Natural Product Libraries for Hsp90 Inhibitors
(Multidisciplinary Digital Publishing Institute, 2014-03-03)Hsp90 has become the target of intensive investigation, as inhibition of its function has the ability to simultaneously incapacitate proteins that function in pathways that represent the six hallmarks of cancer. While a ... -
Parallel solid-phase synthesis of diaryltriazoles
(Beilstein-Institut, 2012-07-06)A series of substituted diaryltriazoles was prepared by a solid-phase-synthesis protocol using a modified Wang resin. The copper(I)- or ruthenium(II)-catalyzed 1,3-cycloaddition on the polymer bead allowed a rapid synthesis ... -
Automated three-component synthesis of a library of γ-lactams
(Beilstein-Institut, 2012-10-19)A three-component method for the synthesis of γ-lactams from commercially available maleimides, aldehydes, and amines was adapted to parallel library synthesis. Improvements to the chemistry over previous efforts include ... -
Hydrophobic analogues of rhodamine B and rhodamine 101: potent fluorescent probes of mitochondria in living C. elegans
(Beilstein-Institu, 2012-12-11)Mitochondria undergo dynamic fusion and fission events that affect the structure and function of these critical energy-producing cellular organelles. Defects in these dynamic processes have been implicated in a wide range ... -
Synthetic probes for the study of biological function
(Beilstein-Institut, 2013-01-15) -
Inhibiting heat-shock protein 90 reverses sensory hypoalgesia in diabetic mice
(Portland Press Limited, 2010-07-14)Increasing the expression of Hsp70 (heat-shock protein 70) can inhibit sensory neuron degeneration after axotomy. Since the onset of DPN (diabetic peripheral neuropathy) is associated with the gradual decline of sensory ... -
Biophysical Mechanisms of the Neutralization of Endotoxins by Lipopolyamines
(Bentham Open, 2013-09-30)Endotoxins (lipopolysaccharides, LPS) are one of the strongest immunostimulators in nature, responsible for beneficial effects at low, and pathophysiological effects at high concentrations, the latter frequently leading ... -
GlycomicsDB - A Data Integration Platform for Glycans and their Structures
(Bentham Open, 2011-04-19)Glycomics is a discipline of biology that deals with the structure and function of glycans (or carbohydrates). Analytical techniques such as mass spectrometry (MS) and nuclear magnetic resonance (NMR) are having a significant ... -
A cell based high-throughput screening approach for the discovery of new inhibitors of respiratory syncytial virus
(BioMed Central, 2013-01-10)Background: Human respiratory syncytial virus (hRSV) is a highly contagious pathogen and is the most common cause of bronchiolitis and pneumonia for infants and children under one year of age. Worldwide, greater than 33 ... -
Characterization of a Cdc42 Protein Inhibitor and Its Use as a Molecular Probe
(The American Society for Biochemistry and Molecular Biology, 2013-02-04)Cdc42 plays important roles in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. Overactive Cdc42 has been implicated in the pathology of cancers, immune diseases, and neuronal ... -
Decreased APOE-containing HDL subfractions and cholesterol efflux capacity of serum in mice lacking Pcsk9.
(Strangor, 2013-07-24)Background Studies in animals showed that PCSK9 is involved in HDL metabolism. We investigated the molecular mechanism by which PCSK9 regulates HDL cholesterol concentration and also whether Pcsk9 inactivation might affect ... -
Potent Adjuvanticity of a Pure TLR7-Agonistic Imidazoquinoline Dendrimer
(Public Library of Science, 2012-08-28)Engagement of toll-like receptors (TLRs) serve to link innate immune responses with adaptive immunity and can be exploited as powerful vaccine adjuvants for eliciting both primary and anamnestic immune responses. TLR7 ... -
Mitochondrial Targeted Coenzyme Q, Superoxide, and Fuel Selectivity in Endothelial Cells
(Public Library of Science, 2009-01-22)Background Previously, we reported that the “antioxidant” compound “mitoQ” (mitochondrial-targeted ubiquinol/ubiquinone) actually increased superoxide production by bovine aortic endothelial (BAE) cell mitochondria ... -
Sensitivity of Mitochondrial Transcription and Resistance of RNA Polymerase II Dependent Nuclear Transcription to Antiviral Ribonucleosides
(Public Library of Science, 2012-11-15)Ribonucleoside analogues have potential utility as anti-viral, -parasitic, -bacterial and -cancer agents. However, their clinical applications have been limited by off target effects. Development of antiviral ribonucleosides ... -
Turmeric inhibits parathyroid hormone-related protein (PTHrP) secretion from human rheumatoid synoviocytes
(BioMed Central, 2012-06-12)Excessive production of parathyroid hormone-related protein (PTHrP) by tumor-like synoviocytes contributes to joint destruction in rheumatoid arthritis (RA). Having previously demonstrated that curcuminoid-only and essential ... -
Structural analysis of inhibition of E. coli methionine aminopeptidase: implication of loop adaptability in selective inhibition of bacterial enzymes
(BioMed Central, 2007-12-19)Background: Methionine aminopeptidase is a potential target of future antibacterial and anticancer drugs. Structural analysis of complexes of the enzyme with its inhibitors provides valuable information for structure-based ...
