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A number of models have been proposed in order to
2021-10-25
A number of models have been proposed in order to explain the mechanisms of protein transport through nuclear pore complexes. One theory is that the transport is mediated by specific peptide signals known as NLSs. The classical NLSs are short sequences containing a high proportion of the positively
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Underlying this study is the hypothesized importance of insu
2021-10-25
Underlying this study is the hypothesized importance of insulin and glucose metabolism on bone. In our investigation of GIP and GIPR gene polymorphisms in relation to bone phenotypes in young and old women our findings depict a complex relationship between glucose metabolism genes and bone. In the c
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br Clinical trials testing GLP
2021-10-25
Clinical trials testing GLP-1 mimetics in AD or PD patients GIP analogues show good neuroprotective effects in animal models of AD and PD Glucose-dependent insulinotropic polypeptide (GIP) is a 42-amino bafilomycin a1 incretin growth factor which activates pancreatic islets to enhance insulin
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The GABA A receptors containing the subunit are crucial for
2021-10-25
The GABA-A receptors containing the δ subunit are crucial for the mediation of non-synaptic inhibition in the dentate gyrus; thus, the decreased expression of the δ subunit may suggest a decrease in the inhibitory tone and an increase in the neuronal excitability. Moreover, the GABA-A receptors cont
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Herein we describe the design
2021-10-23
Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during
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Type IIIa b the ligand
2021-10-23
Type IIIa/b – the ligand dependent oncogenic Hh pathway (paracrine or reverse paracrine mode) is mediated by paracrine activation and is usually encountered in embryonic development, but also in installation and progression of cancer [58]. Specifically, Hh ligands secreted by malignant Rhapontigenin
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br Introduction In the treatment of patients with AIDS
2021-10-23
Introduction In the treatment of patients with AIDS and human immunodeficiency virus type 1 (HIV-1), anti-retroviral therapy (ART), which uses anti-HIV drugs such as protease inhibitors, integrase inhibitors and reverse transferase inhibitors, has made a major contribution. There are still some s
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Some studies show that testosterone may
2021-10-23
Some studies show that testosterone may be involved in regulating cell proliferation and its stimulating effect has been proved in castrated rats (Wainwright et al., 2011), but not in mice and meadow voles (Ormerod and Galea, 2003; Benice and Raber, 2010). However, the seasonal difference in cell pr
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br Experimental procedures br Results br
2021-10-23
Experimental procedures Results Discussion Although the presence and localization of the GlyR subunits have been determined in the adult retina, the proportion of each GlyR subunit has not been assessed in the adult or in the developing retina. In the present study, we carried out the absol
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Okadaic acid We confirmed a decrease in extracellular glutam
2021-10-23
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
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In the present study we set out to discover
2021-10-23
In the present study we set out to discover new non-steroidal SEGRA and to analyse their mechanism of function. Towards this goal we initiated a virtual screening (VS) approach, utilizing structure-based pharmacophore modeling, in silico docking and molecular dynamics (MD) simulations. Our pharmacop
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So far the functional significance of GluR A and GluR
2021-10-23
So far, the functional significance of GluR-A and GluR-B in synaptic plasticity has been best studied in the context of long-term potentiation of synaptic transmission in vitro in the hippocampus and the regulation of synaptic strength in paradigms underlying activity-dependent learning in vivo Taka
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Xenobiotic metabolizing enzymes are classified as being phas
2021-10-23
Xenobiotic metabolizing enzymes are classified as being phase I, phase II and transporter enzymes, with phase I enzymes metabolizing lipophyllic xenobiotics to make them more polar so that the phase II enzymes can perform the necessary conjugation reactions that afford elimination. Although the phas
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br Introduction The glucagon receptor GCGR is a
2021-10-23
Introduction The glucagon receptor (GCGR) is a G-protein-coupled receptor expressed mainly in the liver and kidney. Upon glucagon binding, it activates the stimulatory G protein (Gs) and increases cAMP level, subsequently transducing glucagon signaling involved in glucose, amino acids and lipid m
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Methoxyflavone and methoxyflavanone Fig both act as
2021-10-23
6-Methoxyflavone and 6-methoxyflavanone (Fig. 2) both act as flumazenil-insensitive positive allosteric modulators of GABA responses at human recombinant α1β2γ2L and α2β2γ2L GABAA receptors. However, unlike 6-methoxyflavone, 6-methoxyflavanone was relatively inactive at α1β2 GABAA receptors. Both fl
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