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The existence of EAAT subtypes
2021-11-22
The existence of 5 EAAT subtypes raises obvious questions as to the cellular and anatomical distribution of the various transporters (for review, see Gegelashvili & Schousboe, 1998, Danbolt, 2001). While difference in techniques (i.e., protein vs. mRNA), reagents, and preparations (i.e., in vivo vs.
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In the present study we characterized the expression of
2021-11-22
In the present study, we characterized the expression of glucose transporters in the developing and adult mouse lens and showed that GLUT1 is the primary transporter expressed in the lens epithelium. We found that mice with a homozygous deletion of Slc2a1 from the lens epithelium developed cataracts
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CP-690550 Citrate A number of GCK activators for treating T
2021-11-22
A number of GCK activators for treating T2D have been developed and tested but not progressed successfully from clinical trials into therapy [45]. Our observations suggest that increased risk of hypoglycemia might be possible, particularly if drugs penetrate into brain. A further possibility is that
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LbGlcK crystallized as a ligandless dimer in the asymmetric
2021-11-22
LbGlcK crystallized as a ligandless dimer in the asymmetric unit of space group P21 (Fig. 1a) with two identical subunits stabilized by a large contact surface area of 2295 Å2 (13% of the total surface area) as determined by the Protein Interfaces, Surfaces, and Assemblies (PISA) server [18]. Each m
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br Conclusions We have shown that despite the development of
2021-11-22
Conclusions We have shown that despite the development of severe insulin intolerance and marked alterations in whole body substrate oxidation that Gcgr−/− mice are protected against olanzapine-induced hyperglycemia. Our data provides evidence that this protective effect is likely due in large par
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To identify inhibitors of the Hh GLI signaling pathway from
2021-11-22
To identify inhibitors of the Hh/GLI signaling pathway from natural resources, we have recently reported the successful construction of a cell-based screening assay system for the Hh/GLI signaling pathway (Fig. 1). This is an assay using a GLI-dependent luciferase reporter in human keratinocyte cell
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br Neural circuits that control hunger br
2021-11-22
Neural circuits that control hunger Ghrelin & cognitive control of feeding Ghrelin is a 28 amino 2768 orexigenic peptide that stimulates food intake in rodents and patients (Andrews, 2011, Cummings, 2006, Horvath et al., 2001, Müller et al., 2015, Nakazato et al., 2001, Tschöp et al., 2000, Wr
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br Genetic manipulation variation of the ghrelin system and
2021-11-22
Genetic manipulation/variation of the ghrelin system and alcohol-related outcomes Genetic manipulation of the ghrelin system (either the peptide or the receptor gene) via knockout rodent models has provided further insight into the role of this system in alcohol seeking and consummatory behaviors
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Optimization of the tetrahydroindazole series led to the
2021-11-22
Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ()
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Irpex lacteus was well known as an edible
2021-11-22
Irpex lacteus was well known as an edible and medicinal mushroom. It had been reported that I. lacteus could produce a thermostable α-galactosidase [17]. The reported α-galactosidase from I. lacteus, however, seemed to be unsuitable for the practical application due to its poor hydrolysis ability to
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Recently considerable effort has been invested in developing
2021-11-20
Recently, considerable effort has been invested in developing FDPS inhibitors based on alternative scaffolds (including nonbisphosphonates) that allow other tissue types and parasite-derived forms of FDPS , to be targeted. There are several limits in analyzing inhibitors of FDPS activity: the most
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It has been reported that
2021-11-20
It has been reported that CD133+ glioma stem Eribulin receptor are resistant to temozolomide (TMZ) therapy [155]. Dose dependent TMZ treatment of CD133+ cells enhanced activities of the Notch and SHh pathways [156]. Moreover, 500 μmol/L TMZ induced a significant upregulation of Gli1, HES1 and HES5
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The occurrence of naturally HCV NS resistance associated sub
2021-11-20
The occurrence of naturally HCV NS3 resistance-associated substitutions (RAS) affects virological outcome of DAA-based combination therapies [14], [15], [16], [17], [18], [19]. For the majority of NS3 protease inhibitors the frequency of natural occurrence of single RASs in HCV genotype 1-infected p
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br The mode of binding of ligands to GPR As
2021-11-20
The mode of binding of ligands to GPR35 As noted above, although kynurenic N-Benzylacetamidine hydrobromide is an agonist at GPR35, this is true for neither kynurenine [8] nor kynurenic acid ethyl ester [13]. This implicates a key role for the carboxylate group in binding and/or activation of GPR
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While the S site has been implicated
2021-11-20
While the S2 site has been implicated in binding, it Protease Inhibitor Cocktail (EDTA-Free, 200X in DMSO) is unclear whether the S2 site plays a role in the substrate transport process. Crystal structures have revealed that different drugs and detergents can bind to the S2 site of SERT [8] and LeuT
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