• br Drug design Over the past decades the development of

  2022-05-11

  

  Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst

• In order to study the role of haspin s kinase

  2022-05-10

  

  In order to study the role of haspin’s kinase activity in mitosis (and other cellular processes) and its potential role in cancer, we sought to identify and optimize inhibitors. Utilizing a recently developed time-resolved fluorescence resonance energy transfer (TR-FRET) high throughput screening (H

• To search for potential variants of SLA DOB

  2022-05-10

  

  To search for potential variants of SLA-DOB and CD4 associated with different (percentage) levels of the five (T-lymphocyte subsets, total antibody IgG, interferon alpha (IFN-α), Toll like receptor 3 (TLR3), interleukin 6 (IL-6) in serum and porcine reproductive and respiratory syndrome virus (PRRSV

• Vinblastine sulfate synthesis In summary we have developed a

  2022-05-10

  

  In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ

• One of the main clinical

  2022-05-10

  

  One of the main clinical issues of ABCB1, together with its impact on intestinal absorption, concerns its location at the BBB. Indeed, ABCB1 has been identified in the luminal side of endothelial cells and in the abluminal side of astrocyte endfeet processes of the CNS microvasculature [[36], [37],

• Excessive extracellular glutamate may induce excitotoxic neu

  2022-05-10

  

  Excessive extracellular glutamate may induce excitotoxic neuronal damage in disorders of the CNS (Schwartz et al., 2003). EAATs are considered to contribute to prevention of excitotoxicity by glutamate uptake. Our data revealed that expression levels of membrane EAAT proteins in astrocytes are much

• ICH induced striatal lesion produced a reduction of EAAT exp

  2022-05-10

  

  ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino monocrotaline sale transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain i

• We confirmed a decrease in extracellular glutamate uptake an

  2022-05-10

  

  We confirmed a decrease in extracellular glutamate uptake and the presence of efflux in an endothelial cell model of oxygen-glucose deprivation (OGD), which effectively simulates the inefficient energy supply after brain injury [15], and analysed the function of endothelial EAATs and explored the ro

• The discovery that GLUT in the microvasculature represents a

  2022-05-10

  

  The discovery that GLUT1 in the microvasculature represents an important target of VEGF thereby affecting SANT-1 function is highly relevant. The work of Jais et al. identified VEGF as a determining player in the regulation of cognitive performance and provides an important link to the unfavorable

• Ghrelin is mostly known for its orexigenic properties

  2022-05-09

  

  Ghrelin is mostly known for its orexigenic properties, whereas the role of DAG on feeding is controversial with studies claiming an orexigenic, anorexigenic or no effect (Inhoff et al, 2009, Toshinai et al, 2006). One of these studies was that of Toshinai and colleagues, who found a link between the

• br Ghrelin Ghrelin was purified from rat stomach about twent

  2022-05-09

  

  Ghrelin Ghrelin was purified from rat stomach about twenty years ago as a 28-amino NAD+ octanoylated peptide and shown to be the endogenous ligand of the growth hormone (GH) secretagogue receptor (now termed GHSR1a, Howard et al., 1996, Kojima et al., 1999). GHSR1a is a 7-transmembrane receptor

• E-4031 br Regulation of plasma ghrelin concentration

  2022-05-09

  

  Regulation of plasma ghrelin concentration As described above, ghrelin is primarily produced in the stomach and secreted into the blood stream. Plasma ghrelin does not significantly differ between chronic heart failure (CHF) patients and controls, although plasma ghrelin level is significantly hi

• The observed increase in macroscopic conductance could be du

  2022-05-09

  

  The observed increase in macroscopic conductance could be due to a left shift in the open state probability vs. voltage curve for the high-activity state causing an increase in the open state probability at all potentials. However, an increase of the apparent single channel conductance cannot be ent

• CC is a widespread disorder affecting

  2022-05-09

  

  CC is a widespread disorder affecting up to 20% of people worldwide, which also deteriorates the quality of life of patients and causes a substantial economic burden to society. There are 3 categories of CC: normal-transit constipation, slow-transit constipation and defecatory or rectal evacuation d

• uPAR promotes cell associated proteolysis by binding to uPA

  2022-05-09

  

  uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot

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