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To facilitate the development of novel diagnostic and
2021-12-24
To facilitate the development of novel diagnostic and therapeutic interventions in NASH, a plethora of animal models have been used to identify molecular targets that are involved in the onset and progression of NASH. In view of recent advances in the understanding of the pathogenesis of NASH and pr
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As preclinical toxicity and efficacy both appear to be assoc
2021-12-24
As preclinical toxicity and efficacy both appear to be associated with GlyT1 inhibition, it remains to be determined whether on-target toxicity can be separated from efficacy. The present study evaluated a series of GlyT1 inhibitors for target potency, mode of inhibition, residence time, activity in
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To date glycine receptors have
2021-12-24
To date, glycine receptors have been found in five distinct transmembrane protein subunits (one β subunit and four α subunit (α1–α4)), combining to form two different types of functional receptors [4], [14], either α homomeric, the immature extrasynaptic glycine receptor subtype, or αβ heteromeric,
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This data is in accordance with our recent results on
2021-12-24
This data is in accordance with our recent results on the influence of cholesterol-depleting agent methyl-β-cyclodextrin on platelets (Borisova et al., 2011a). Dissipation of the proton electrochemical gradient of secretory granules by methyl-β-cyclodextrin did not evoke the release of endogenous gl
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ICH induced striatal lesion produced a
2021-12-24
ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino ll 37 synthesis transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain isc
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Previous reports have showed that the expression and localiz
2021-12-24
Previous reports have showed that the expression and localization of GLUT8 in mouse (Gómez et al., 2006; Kim and Moley, 2007), rat (Ibberson et al., 2002) and human (Schürmann et al., 2002). In this study, GLUT8 protein mainly localized in the spermatocytes, elongated and round spermatids in the adu
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br STAR Methods br Acknowledgments We would like to thank
2021-12-24
STAR★Methods Acknowledgments We would like to thank Dr. Xiping Cheng for help with the immunohistochemistry staining, Qi Su for help with gene expression analysis, and Dr. Chaoying Liang at the UTSW Genomics Microarray Core facility for assistance on RNA-seq. W.-H.L. was supported by grant awa
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It is possible that regulation
2021-12-24
It is possible that regulation of adiposity and glucose homeostasis by GIP are in part mediated by altering leptin levels and/or leptin signaling. However, we are unaware of reports that support this mechanism of action of GIP. In addition, leptin levels in GIP receptor knockout mice [12], [52] and
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Ghrelin contains an n octanoylation at its
2021-12-24
Ghrelin contains an n-octanoylation at its Ser3 residue (Kojima et al., 1999). While des-acyl ghrelin is found in high concentrations in the blood, only the lipidated form is active at GHSR (Bednarek et al., 2000). We previously showed that ghrelin interacts with the membrane via its lipid modificat
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The biochemical cell culture activities and properties of bi
2021-12-23
The biochemical, cell culture activities and properties of bicyclic carboxamides are compiled in , with the prototype of the series, 4-fluorobenzyl carboxamide , displaying an antiviral profile comparable to the spirocyclic carboxamide . The introduction of a small hydrophobic methyl () and chloride
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rhein Some biguanides can cross the mitochondrial membrane a
2021-12-23
Some biguanides can cross the mitochondrial membrane and increase L-lactate formation by inhibiting oxidative rhein [34]. On the other hand, it has also been reported that levels of fasting plasma lactate in T2DM patients are similar regardless of whether or not metformin is administered [35] and t
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gap-26 There is abundant literature about different function
2021-12-23
There is abundant literature about different functional aspects of the cannabinoid system (Badal et al., 2017, Balenga et al., 2011, Henderson-Redmond et al., 2016, Nair et al., 2015); however, not a great deal is known about the mechanism by which ethanol impacts its function in connection to the i
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br Activity dependent control of myelination and myelin main
2021-12-23
Activity-dependent control of myelination and myelin maintenance Oligodendrocytes have intrinsic myelinating capacity and can myelinate fixed histone deacetylase in addition to synthetic nanofibers and micropillars [21, 34, 35]. What prevents oligodendrocytes from myelinating dendrites or other c
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ionophore Further explorations at the ortho and
2021-12-23
Further explorations at the ortho- and meta-positions of the phenyl in the tail proceeded on the basis of the preliminary results. First, we investigated the fluorine group at the meta- (13p) and ortho-positions (13q) of the phenyl group, with both compounds being slightly less potent than 13o. Surp
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br Activators Many compounds are
2021-12-23
Activators Many compounds are known to influence the activity of Ca2+-activated K+ channels, and since hIK1 was cloned more insight has been gained on compounds that have the capacity to increase channel activity. Activation by divalent metal cations has been investigated, with Ca2+, Pb2+, Cd2+,
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