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Research Centers: Recent submissions
Now showing items 141-160 of 241
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Neuronal Glud1 (Glutamate Dehydrogenase 1) Over-Expressing Mice: Increased Glutamate Formation and Synaptic Release, Loss of Synaptic Activity, and Adaptive Changes in Genomic Expression
(Elsevier, 2011-09)Glutamate dehydrogenase 1 (GLUD1) is a mitochondrial enzyme expressed in all tissues, including brain. Although this enzyme is expressed in glutamatergic pathways, its function as a regulator of glutamate neurotransmitter ... -
Mechanism of the asymmetric activation of the MinD ATPase by MinE
(Wiley, 2012-07)MinD is a component of the Min system involved in the spatial regulation of cell division. It is an ATPase in the MinD/ParA/Mrp deviant Walker A motif family which is within the P loop GTPase superfamily. Its ATPase activity ... -
Discrimination of soluble and aggregation-prone proteins based on sequence information
(Royal Society of Chemistry, 2013-04-05)Understanding the factors governing protein solubility is a key to grasp the mechanisms of protein solubility and may provide insight into protein aggregation and misfolding related diseases such as Alzheimer’s disease. ... -
Production, purification, and characterization of recombinant hFSH glycoforms for functional studies
(Elsevier, 2015-04-15)Previously, our laboratory demonstrated the existence of a β-subunit glycosylation-deficient human FSH glycoform, hFSH21. A third variant, hFSH18, has recently been detected in FSH glycoforms isolated from purified pituitary ... -
Drug Repurposing for Gastrointestinal Stromal Tumor
(American Association for Cancer Research, 2013-07)Despite significant treatment advances over the past decade, metastatic gastrointestinal stromal tumor (GIST) remains largely incurable. Rare diseases, such as GIST, individually affect small groups of patients but ... -
Structure Fluctuations and Conformational Changes in Protein Binding
(World Scientific Publishing, 2012-04)Structure fluctuations and conformational changes accompany all biological processes involving macromolecules. The paper presents a classification of protein residues based on the normalized equilibrium fluctuations of the ... -
Identification of human presequence protease (hPreP) agonists for the treatment of Alzheimer’s disease
(Elsevier, 2014-04-09)Amyloid-β (Aβ), a neurotoxic peptide, is linked to the onset of Alzheimer’s disease (AD). Increased Aβ content within neuronal cell mitochondria is a pathological feature in both human and mouse models with AD. This ... -
Open Access High Throughput Drug Discovery in the Public Domain: A Mount Everest in the Making
(Bentham Science Publishers, 2010-11-11)High throughput screening (HTS) facilitates screening large numbers of compounds against a biochemical target of interest using validated biological or biophysical assays. In recent years, a significant number of drugs in ... -
A phase I study of intraperitoneal nanoparticulate paclitaxel (Nanotax®) in patients with peritoneal malignancies
(Springer Verlag, 2015-05)PURPOSE: This multicenter, open-label, dose-escalating, phase I study evaluated the safety, tolerability, pharmacokinetics and preliminary tumor response of a nanoparticulate formulation of paclitaxel (Nanotax®) administered ... -
Constrained TRPV1 agonists synthesized via silver-mediated intramolecular azo-methine ylide cycloaddition of α-iminoamides
(Elsevier, 2014-02-01)As part of an effort to identify agonists of TRPV1, a peripheral sensory nerve ion channel, high throughput screening of the NIH Small Molecule Repository (SMR) collection identified MLS002174161, a pentacyclic benzodiazepine. ... -
Molecular landscape of the ribosome pre-initiation complex during mRNA scanning: structural role for eIF3c and its control by eIF5
(Elsevier, 2017-04-06)During eukaryotic translation initiation, eIF3 binds the solvent-accessible side of the 40S ribosome and recruits the gate-keeper protein eIF1 and eIF5 to the decoding center. This is largely mediated by the N-terminal ... -
Age-associated changes in synaptic lipid raft proteins revealed by two-dimensional fluorescence difference gel electrophoresis
(Elsevier, 2008-12-31)Brain aging is associated with a progressive decline in cognitive function though the molecular mechanisms remain unknown. Functional changes in brain neurons could be due to age-related alterations in levels of specific ... -
Probing Chemical Space with Alkaloid-Inspired Libraries
(Nature Publishing Group, 2014-01-19)Screening of small molecule libraries is an important aspect of probe and drug discovery science. Numerous authors have suggested that bioactive natural products are attractive starting points for such libraries, due to ... -
Discovery, Synthesis, and Optimization of Diarylisoxazole-3- carboxamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore
(Wiley, 2015-10)The mitochondrial permeability transition pore (mtPTP) is a Ca2+-requiring mega-channel which, under pathological conditions, leads to the deregulated release of Ca2+ and mitochondrial dysfunction, ultimately resulting in ... -
Reconfiguration of the proteasome during chaperone-mediated assembly
(Nature Publishing Group, 2013-05-23)The proteasomal ATPase ring, comprising Rpt1-Rpt6, associates with the heptameric α ring of the proteasome core particle (CP) in the mature proteasome, with the Rpt C-terminal tails inserting into pockets of the α ring1–4. ... -
Synthesis of a quinolone library from ynones
(Elsevier, 2009-11-25)A library of 72 quinolones was synthesized from substituted anthranilic acids, using ynone intermediates. These masked β-dicarbonyl synthons allowed cyclization under milder conditions than previously reported quinolone syntheses. -
Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 2CL Protease
(American Chemical Society, 2016-03-10)Human noroviruses are the primary causative agents of acute gastroenteritis and a pressing public health burden worldwide. There are currently no vaccines or small molecule therapeutics available for the treatment or ... -
Synthesis of a Family of Spirocyclic Scaffolds; Building Blocks for the Exploration of Chemical Space
(American Chemical Society, 2013-07-05)This report describes the preparation of a series of 17 novel racemic spirocyclic scaffolds that are intended for the creation of compound libraries by parallel synthesis for biological screening. Each scaffold features ... -
Evidence that histidine protonation of receptor-bound anthrax protective antigen is a trigger for pore formation
(ACS, 2010-08-24)The protective antigen (PA) component of the anthrax toxin forms pores within the low pH environment of host endosomes, through mechanisms that are poorly understood. It has been proposed that pore formation is dependent ... -
Structural and Inhibitor Studies of Norovirus 3C-like Proteases
(Elsevier, 2013-09-17)Noroviruses have a single-stranded, positive sense 7–8 kb RNA genome, which encodes a polyprotein precursor processed by a virus-encoded 3C-like cysteine protease (3CLpro) to generate mature non-structural proteins. Because ...
