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Receptor interactions and binding mode
2022-06-07
Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat
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The variants all occurred at
2022-06-07
The 17 variants all occurred at residues conserved among vertebrates (Figure 1B) and in regions depleted in missense variants in gnomAD. Indeed, when we assessed missense tolerance ratios for TRRAP, we observed that most of the 17 variants were in regions intolerant to missense variants (Figure 2B).
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In the current study Olfml knockdown increased
2022-06-07
In the current study, Olfml1 knockdown increased YAP but decreased the respective target genes of canonical Wnt signaling and Hedgehog signaling, Axin2 and Gli1. YAP suppresses canonical Wnt via binding to Dishevelled and/or β-catenin [[39], [40], [41], [42]]. Tariki et al. reported that adenovirus-
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Three main mechanisms have been proposed
2022-06-07
Three main mechanisms have been proposed for the secretion of active forms of hedgehog ligands: first, construction of a multimeric molecule with lipid moieties placed on the inside, making a soluble Hh protein which can diffuse from the membrane; second, function of dispatched proteins through pack
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In the course of studies leading to the discovery
2022-06-07
In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of
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Haploid germ cell specific nuclear protein kinase Haspin pro
2022-06-07
Haploid germ cell-specific nuclear protein kinase (Haspin) proteins are divergent members of the eukaryotic protein kinase family. Haspin (encoded by germ cell-specific gene 2: Gsg2) is found in many eukaryotic lineages (animal, fungi, and plants), and the protein and its mRNA were initially detecte
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The absolute requirement for substrate prephosphorylation ra
2022-06-07
The absolute requirement for substrate prephosphorylation raised the possibility that short phosphorylated peptides might serve as selective substrate competitive inhibitors. A set of phosphorylated peptides patterned after known GSK-3 substrates was generated and shown to inhibit GSK-3 in vitro in
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Glycogen synthase kinase GSK a serine threonine kinase has
2022-06-07
Glycogen synthase kinase-3 (GSK-3), a serine/threonine kinase, has been confirmed to be involved in some biological processes in NaCl or wound-treated plants (Chen et al., 2003, Hai et al., 2001, Jonak et al., 2000). NO has been recently recognized as a vital signaling compound in plants. The NO don
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Introduction Glycogen synthase kinase GSK is an enzyme
2022-06-07
Introduction Glycogen synthase kinase-3 (GSK-3) is an enzyme playing multiple roles in animal tissues and organs, and BAY 57-9352 sale is not an exception. Apart from involvement in regulation of apoptosis and survival GSK-3 influences neuronal morphology, synapse formation, memory reconsolidation
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IC is a rat mAb specifically binding to
2022-06-07
IC2 is a rat mAb specifically binding to insulin granula [127,128]. Although this mAb was discovered 30 years ago, it has only recently been used for β-cell imaging in vivo. Moore et al. used this mAb for β-cell imaging in 2001 [129]. After DTPA conjugation, IC2 was labeled with 111In. Both in vitro
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Previously we reported that the inhibition of
2022-06-07
Previously, we reported that the inhibition of PKC-ζ and PKC-ε activity in hypertrophic adipocytes had deleterious effects on EPA-induced GPR120-mediated VEGF-A production [12]. However, the activation of PKC-θ, -ζ and -λ can also enhance the phosphorylation of IKK and p65, and facilitate the transl
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br Potential endogenous agonists of GPR
2022-06-07
Potential endogenous agonists of GPR35 The first endogenously produced chemical that was shown to be able to activate GPR35 was the tryptophan metabolite kynurenic LY2603618 [8]. When human GPR35 was expressed along with a mixture of promiscuous and chimeric G proteins 9, 10 (Box 1) in CHO cells
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In addition to the increase of extracellular glutamate
2022-06-06
In addition to the increase of extracellular glutamate, ICH can also increase the levels of reactive oxygen species (ROS) and oxidative stress. Although the products of red blood cell lysis and plasma components, as well as the excitotoxic effect of glutamate have been to increase oxidative damage (
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br Acknowledgements br Introduction Aminoacyl tRNA synthetas
2022-06-06
Acknowledgements Introduction Aminoacyl-tRNA synthetases catalyze the formation of an ester bond between an amino beta lactamase and the 3′ end of a tRNA in a two-step reaction. First, the amino acid is activated and an enzyme-bound adenylate intermediate is formed. Then, the amino acid is tra
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SGLT inhibitors have been accepted as
2022-06-06
SGLT-2 inhibitors have been accepted as a new class of antidiabetic agent (Kurosaki and Ogasawara, 2013). They limit renal glucose reabsorption and promote urinary excretion of glucose, thereby reducing plasma glucose levels (de Leeuw and de Boer, 2016, Jojima et al., 2016, Pérez López et al., 2010,
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