• Considering together the conformational docking and SAR resu

  2022-04-19

  

  Considering together the conformational, docking and SAR results of this and of previously published papers, a three points pharmacophore model can be developed considering the indispensable residues of SRSRY derived antagonists, namely Arg89, Arg91 and Tyr92. This model is shown in Fig. 10, and req

• Corresponding to the different insulinotropic

  2022-04-19

  

  Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct Sorbitol on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site for full agonist

• This study introduces a mouse model

  2022-04-19

  

  This study introduces a mouse model carrying the point mutation R258W in Ffar1, which abolishes the stimulation of insulin secretion in response to long chain fatty acids. The minimal genetic alteration mirrors the human situation and has the advantage over conventional knockout/congenic mouse mode

• myc pathway One of the main mechanisms enabling recycling of

  2022-04-19

  

  One of the main mechanisms enabling recycling of intracellular redox-active iron is lysosomal degradation of ferritin in the process of autophagy, often referred to as ‘ferritinophagy’ [128]. Autophagy was suggested to contribute to ferroptotic cell death by promoting the degradation of iron storage

• Paroxysmal or sustained atrial fibrillations

  2022-04-19

  

  Paroxysmal or sustained atrial fibrillations profoundly activate platelets and induce coagulation factors in the heart (Choudhury and Lip, 2003). Accumulating factor Xa and downstream thrombin in the fibrillating left atrium activate PAR1 and/or PAR2 signaling to modulate electrical characteristics

• In summary tail vein injection of mmLDL activated the ERK

  2022-04-19

  

  In summary, tail vein injection of mmLDL activated the ERK1/2 signaling pathway, leading to increased serum concentrations and increased vascular wall expression of ICAM-1 and VCAM-1, and may cause increased expression of vascular smooth muscle ETB receptors and the ETB receptor-mediated contractile

• Although we showed that RBL H Sc

  2022-04-19

  

  Although we showed that RBL-2H3 Sc98 resveratrol took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, including SE

• Several classes of small molecules that

  2022-04-19

  

  Several classes of small molecules that modulate CDK8 activity have been reported in the patent literature (Fig. 1). A quinazoline derivative, Senexin B (SNX2-1–165, 1), showed CDK8 enzyme inhibitory activity with an IC50 value of 24–50 nM in different assay, and displayed potent, selective enzymati

• br Conclusions br Introduction Astrocytes contribute to phys

  2022-04-18

  

  Conclusions Introduction Astrocytes contribute to physiological PX-478 2HCl function on many levels. They help maintain the physiological composition of the extracellular medium by, for instance, buffering potassium and uptake of neurotransmitters. They can also provide neurons with energy su

• The isoenzyme hGSTP is an attractive

  2022-04-18

  

  The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t

• Decreasing GSK activity has therapeutic benefits in animal

  2022-04-18

  

  Decreasing GSK-3β activity has therapeutic benefits in animal model of colitis [45] and traumatic BGP-15 injury [46] and ischemia/reperfusion injury [47,48]. In brain, activation of GSK-3β promotes Aβ toxicity by elevating APP expression and its amyloidogenic cleavage, and by dysregulating Aβ clear

• Finally our data found that the EBV

  2022-04-18

  

  Finally, our data found that the EBV dUTPase protein modulates tryptophan, serotonin, and DA metabolism and use in vitro and in vivo. The EBV dUTPase may alter kynurenine catabolism in microglia in vitro, suggesting that there is an increase synthesis of quinolinic acid. Quinolinic acid, an agonist

• br Materials and methods br Results br Discussion br Disclos

  2022-04-18

  

  Materials and methods Results Discussion Disclosures Author contributions Acknowledgements Introduction Diabetes mellitus is one of the fastest growing chronic diseases worldwide, with an estimated prevalence of 382 million patients, of which about 90% have type 2 diabetes melli

• br Flavonoid function Antioxidants are compounds when presen

  2022-04-18

  

  Flavonoid function Antioxidants are compounds - when present at a lower concentration compared oxidizable substrate - that delay or prevent oxidation of the substrate [14], [106]. Antioxidants act as nucleophiles to reduce an oxidative molecule to prevent its interaction with another molecule [14

• MHC class II antigen (45-57) [Homo sapiens] br Materials and

  2022-04-18

  

  Materials and methods Results Discussion Since 1990s, solving structures for most DNA glycosylases by X-ray crystallography significantly advanced mechanistic understanding of the catalytic activity and substrate specificity of this important class of DNA repair enzymes. However, static str

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