• The two competitive bivalent GlxI inhibitors polyBHG nM and

  2022-05-30

  

  The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit

• The dramatic increase in the

  2022-05-30

  

  The dramatic increase in the development of EAAT inhibitors and substrates over the last several years can likely be attributed to a number of experimental advances. Firstly, the isolation of the individual EAAT clones allowed each subtype to be selectively examined in well-characterized expression

• br BA induced activation of TGR

  2022-05-27

  

  BA-induced activation of TGR5 TGR5 is a membrane-bound G protein-coupled receptor for BAs and its activation is dependent on cAMP formation and further stimulation of protein kinase A [53], [31]. The receptor is expressed in the enterochromaffin cells, smooth muscles, immune cells and more import

• br Application of TIRFM to visualizing

  2022-05-27

  

  Application of TIRFM to visualizing exocytosis TIRFM was first used to visualize exocytosis from large secretory granules from chromaffin read 108 (Steyer et al., 1997). Before that, visualization of secretory organelle was strictly limited to a few exceptions, such as mast cell of mutant mice,

• br Conflict of interest br

  2022-05-27

  

  Conflict of interest Author contributions Introduction 2-Quinolones [quinoline-2(1H)-ones], while less prominent than the isomeric 4-quinolones, nevertheless enjoy significant attention as scaffolds in compounds exhibiting a variety of biological activities. These include: 4-aryl-6-chloroqu

• This study has some limitations

  2022-05-27

  

  This study has some limitations. The RDS technique was not effective for the population of MSM from Natal, as it has not reached the sample size initially calculated. Few seeds had enough waves to disperse the sample and make it closer to a probabilistic sample, even with all efforts from the resear

• Maillard reaction also known as non enzymatic browning

  2022-05-27

  

  Maillard reaction, also known as non-enzymatic browning reaction, is a complex chemical reaction between carbonyl groups of reducing sugars and free amino groups of amino acids, peptides, proteins or some other nitrogen containing compounds. Maillard reaction plays an important role in food industry

• br Introduction Histamine was generally accepted as

  2022-05-27

  

  Introduction Histamine was generally accepted as a neurotransmitter in 1984, when histamine was first identified to be located in tuberomamillary nucleus (TM) of the brain (Watanabe et al., 1984). In mammals, histaminergic neurons play an important role in regulating multiple physiological activi

• There were hub genes identified by WGCNA among

  2022-05-27

  

  There were 11 hub genes identified by WGCNA among which KIBRA was the hub gene of the black module. The bioinformatics method is an effective and powerful tool to analyze mRNA Pirfenidone profiles and the related pathways. For instance, the lung cancer risk modules that were closely related to lung

• Our data indicate that curcumin reduced MDA and LOOH

  2022-05-27

  

  Our data indicate that curcumin reduced MDA and LOOH formation in plasma and kidney induced by gentamicin treatment. The results demonstrate the protective effect of this compound against oxidative damage to these membranes. Moreover, the ability of curcumin to reduce the formation of LOOH induced b

• GSK can function in regulating insulin

  2022-05-27

  

  GSK-3 can function in regulating insulin signaling and glucose metabolism. Inactivation of GSK-3 activity results in dephosphorylation and activation of GS that leads to improved glucose tolerance. However, there are additional mechanisms that can lead to increases in GS activity and improve insulin

• br Results and discussion br

  2022-05-27

  

  Results and discussion Conclusions In summary, we generated analogues of the hit compounds 1–3, studied their structure–activity relationships, and created a series of highly potent GPR55 agonists. The most potent agonists among the series were 17a-b, 17e, 17g and 17l with EC50 values below 10

• br STAR Methods br Introduction

  2022-05-26

  

  STAR★Methods Introduction Glycosylation is one of the most prevalent post-translational modifications of proteins. It not only plays major roles in folding, transport and localization of proteins [1], but also regulates various biological processes such as cell growth, viral replication and im

• Because AM had limited efficacy on rodent GPR

  2022-05-26

  

  Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to

• To study the effects of GPR at the whole

  2022-05-26

  

  To study the effects of GPR40 at the whole-animal level, GPR40 mice have been generated in two different genetic backgrounds [18], [19]. GPR40 mice from both backgrounds were apparently healthy with no overt signs of metabolic or other abnormalities. As expected, pancreatic islets taken from GPR40 m

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