• The two competitive bivalent GlxI inhibitors polyBHG nM

  2022-01-28

  

  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

• br Materials and methods br Results br Discussion The glucos

  2022-01-28

  

  Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast DiscoveryProbe™ Inhibitor Library by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 o

• Our own search towards aryl imidazole derived GSMs led

  2022-01-27

  

  Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,

• br STAR Methods br Acknowledgments We would

  2022-01-27

  

  STAR★Methods Acknowledgments We would like to thank V. Gladyshev (Harvard), H. Kornblum (UCLA), L. Greene (Columbia), and J. Baraban (Johns Hopkins) for constructive comments to the project and manuscript. We thank L. Gross and A. Kumar for assistance with editing. We thank L.M. Gerber and Z.

• The F P concentration reported for a

  2022-01-27

  

  The F6-P concentration reported for a resting rabbit muscle [20] reduced the KAapp for aldolase–FBPase complex more than 50 times compared to KAapp for aldolase–FBPase in the absence of effectors (Fig. 1b and Table 1). A standard assay for determination of FBPase activity in a complex with aldolase

• br Materials and methods br

  2022-01-27

  

  Materials and methods Results and discussion To analyze the dependence of lysosomal exocytosis on Cu we exposed HeLa Physcion mg to fresh buffer containing normal levels of free Ca (1mM) and measured β-hex levels in the extracellular medium, followed by measuring β-hex content in the total ce

• br Materials and methods br Results br Discussion mmLDL is

  2022-01-27

  

  Materials and methods Results Discussion mmLDL is an important risk factor for cardiovascular disease, but its mechanism is still unclear. Previously, we co-cultured mmLDL with the coronary artery and basilar artery and found that mmLDL could upregulate ETB receptor expression in both [16],

• DIS used standard methods for locating and contacting

  2022-01-27

  

  DIS used standard methods for locating and contacting persons for interview, including the use of phone calls, letters, in person contact, and contact through social media. During this time period, contacts of persons with diagnosed HIV (first-generation contacts) were tested for HIV and, regardless

• It is not established if ONOO also

  2022-01-27

  

  It is not established if ONOO− also induces tyrosine nitration of ANT and affects VDAC1 and ANT interaction, as well as the interaction of VDAC1 with HK II, all of which are events that may lead to altered mitochondrial and cellular function. Thus, in this study we examined tyrosine nitration of bot

• Hypoxia has been shown to affect miR expression that

  2022-01-27

  

  Hypoxia has been shown to affect miR-155 expression that can induce autophagy in nasopharyngeal and cervical carcinoma cells [334]. Suppression of miR-155 inhibited hypoxia-induced autophagy. miR-155 targeted mRNAs involved in the PI3K/PTEN/Akt/mTORC1 pathway including: Ras homolog enriched in dpp-i

• Considering the fact that OCL

  2022-01-27

  

  Considering the fact that OCL induced depletion of T Phos-tag Biotin receptor in non-stimulated cultures, the only possible explanation of this effect is the elevated mortality of these cells. It was found that OCL at the higher concentration induced the apoptosis of CD4+ and CD8+ T cells. These re

• The advent of next generation sequencing NGS has shown that

  2022-01-27

  

  The advent of next-generation sequencing (NGS) has shown that considerable variation in human genome is still undiscovered and therefore a considerable number of rare variations that are related to disease susceptibility may still be unknown. NGS has allowed to strengthen the association between los

• br Discussion Agonist and antagonist action

  2022-01-27

  

  Discussion Agonist and antagonist action at the GluN1/GluN3 C527 is known to be complex [4], [10]. Recombinant GluN1/GluN3 receptors produce only small excitatory currents in response to glycine, likely because of a combination of activation via GluN3 and desensitization via GluN1 [2], [3], [11].

• br Glucose metabolism and diet Glucokinase is

  2022-01-26

  

  Glucose metabolism and diet Glucokinase is essential for sensing blood glucose levels, thus controls metabolism (Iynedjian, 1993, Iynedjian, 2009, Postic et al., 2001, Agius, 2008). Loss of glucokinase activity in humans and mice leads to diabetes (Printz et al., 1993b, Postic et al., 2001, Agius

• Analogous to all GPCRs the GLP R transduces

  2022-01-26

  

  Analogous to all GPCRs, the GLP-1R transduces signals from the outside of the cell to the inside by allosterically converting a ligand-binding event to activation of intracellular effectors. The GLP-1R couples to several intracellular effectors and this pleiotropic coupling is physiologically releva

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