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GPR shares a amino acid sequence identity in humans
2022-04-14
GPR81 shares a 52% amino AS1842856 sequence identity in humans to GPR109A [1], [2], [3]. In addition, GPR81 is localized more specifically to the adipose tissue [3]. In 2008, lactate was discovered to be the endogenous ligand for GPR81 [9], [10]. Plasma lactate levels reach concentrations capable o
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Overall this study provides compelling evidence that overexp
2022-04-14
Overall, this study provides compelling evidence that overexpression of catalase coupled with an enriched diet of OM3 fatty acids are metabolically beneficial. This combination was shown to increase adipose tissue expression of the GPR120/FFAR4, which by interacting with the Nrf2 pathway, resulted i
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The compounds described in this paper were prepared
2022-04-14
The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m
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A-317491 Because of its excellent GPR potency
2022-04-14
Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, A-317491 was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive panel o
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Disrupting the dialog between microbiota and the host especi
2022-04-14
Disrupting the dialog between microbiota and the host, especially at the level of mucosal immunology, is expected to have profound effects on disease development. By using the AOM+DSS model of colitis-associated CRC, Singh et al. (2014) showed that development of inflammation and CRC are exacerbated
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CD binding to gp causes
2022-04-14
CD4 binding to gp120 causes a large scale conformational change of gp120 which involves the gp120 core structure and the transitions of inner-domain layers (layer 1, 2 and 3), but also involves the movement of the major loops (V1, V2 and V3) [16], [17], [18], [19]. For instance, the V2-loop joins th
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br Brief overview of the glutamate
2022-04-14
Brief overview of the glutamate system and rationale for targeting the glycine site of NMDARs In the central nervous system (CNS), glutamate is the major excitatory neurotransmitter and works in concert with gamma-aminobutyric Gedunin (GABA), the primary inhibitory neurotransmitter. Together, GA
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To get a broader view of
2022-04-14
To get a broader view of the interplay between glycolysis and Hippo signaling, we tested the involvement of YAP1 in the regulation of C-MYC and GLUT1 expression. We were able to detect a YAP1-TEAD1 interaction in the nuclear fraction of Jurkat Nogo-66 (1-40) sale and confirm the inhibition of this i
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Here we studied the effects of BZ flurazepam FZ at
2022-04-14
Here we studied the effects of BZ flurazepam (FZ) at high doses in acute and chronic settings of tolerance and dependence in GluR-A−/− mice (Zamanillo et al., 1999). We used measurements in which the phenomenon of “learning while intoxicated” should play only a minor role in order to find out the si
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Such responses have led to the
2022-04-14
Such responses have led to the idea that elasmobranchs may be glucose intolerant. However, certain species, such as the North Pacific spiny dogfish (Squalus suckleyi; note that the species used in this study was previously referred to as Squalus acanthias but a study by Ebert et al. (2010) provided
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In this study we investigated the
2022-04-14
In this study, we investigated the contribution of GCK, G6PC, and PCK expression to glycemia in diabetes. We examined liver tissue from 40 obese subjects: 12 had normal glucose tolerance (NGT) and 28 had type 2 diabetes. Materials and methods Results Discussion This study aimed to investig
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The bioconversion of inositol from glucose
2022-04-14
The bioconversion of inositol from glucose was anticipated nearly a century ago and later confirmed by isotope tracing methods [[22], [23]]. This biosynthesis of inositol involves three sequentially acting enzymes: Firstly, ATP-dependent glucokinase converts glucose to glucose-6-phosphate (G-6P) [[2
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br Materials and methods br
2022-04-14
Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini
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br Materials and methods br Results Bgal from Alteromonas sp
2022-04-13
Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino used by residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other additional ami
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Inflammasomes are multimeric protein complexes involved in t
2022-04-13
Inflammasomes are multimeric protein complexes involved in the host defense protecting activity against invading pathogens and in physiological aberrations such as cancer and auto-inflammatory, metabolic, and neurodegenerative diseases. Inflammasomes induce the inflammatory process by triggering the
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