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Through the analysis of various synthetic GPR
2022-07-21

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic GANT61 australia motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discove
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Axons are the largest component of WM by
2022-07-21

Axons are the largest component of WM by volume and are a significant repository of intracellular glutamate that can be releases under ischemic conditions [1,3,4,29,117]. We have recently shown that the principle route by which mature myelinated Doripenem Hydrate mg release glutamate during acute is
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Bacterial GluRS comes in two flavors discriminatory GluRS D
2022-07-21

Bacterial GluRS comes in two flavors, discriminatory GluRS (D-GluRS) and non-discriminatory GluRS (ND-GluRS). While D-GluRS exclusively catalyses the transfer of Glu to tRNAGlu, the ND-GluRS can also glutamylate tRNAGln forming Glu-tRNAGln. The misacylated product is then transformed to Gln-tRNAGln
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In agreement with the results obtained from GluR A
2022-07-21

In agreement with the results obtained from GluR-A−/− mice, mice in which the NR1 subunit of the NMDA receptor has been selectively deleted from the CA3 subfield of the hippocampus displayed normal acquisition of the standard reference memory version of the watermaze task (Nakazawa et al., 2002), bu
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It is increasingly argued that the immunosuppressive effects
2022-07-21

It is increasingly argued that the immunosuppressive effects of GCs are conferred indirectly by GR through the activation of genes encoding proteins that inhibit Vicriviroc Malate synthesis of proinflammatory genes 86, 87, 88. Genomic studies offer another mechanism compatible with the idea that GC
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Interruption of glucagon signaling pathway
2022-07-21

Interruption of glucagon signaling pathway targeting glucagon receptor (GCGR) by gene knockout, antisense oligonucleotides or specific antagonists induces α-cell hyperplasia and alleviates hyperglycemia and other metabolic symptoms in diabetic animals and patients [[7], [8], [9]]. Here we used a ful
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lpl receptor We have previously shown in the same time
2022-07-21

We have previously shown in the same time frame reported here (10 min) that AG was not degraded into DAG [29] and that the half-life of AG in human serum is ∼10 min [49]. However, we cannot rule out in this study that there is not breakdown to DAG that could contribute to the levels of 125I-ghrelin
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Herein we describe the development
2022-07-21

Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME
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Luciferase Reporter Assay Kit receptor Recently accumulated
2022-07-21

Recently, accumulated evidence has revealed a close link of FXR to gluconeogenesis. For example, activation of FXR by its agonist GW4064 improved hyperglycemia in db/db mice by repressing gluconeogenesis [15], and FXR agonist CDCA decreased transactivation activity of key gluconeogenic genes by indu
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br Introduction GPR also known as
2022-07-21

Introduction GPR40 (also known as free fatty 1-Azakenpaullone receptor 1), a member of the G-protein coupled receptor (GPCR) family, is expressed in pancreatic beta cells, intestine and the central nervous system (Bekinschtein et al., 2008; Itoh et al., 2003). It is activated by medium- and long-
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EW-7197 Introduction of a chloropyridine group onto the fluo
2022-07-21

Introduction of a chloropyridine group onto the fluoro derivative (→) leads to a similarly potent compound that exhibits a lower /, and as was observed with (), was rapidly cleared. However, the high clearance of () did not prevent the increase in the concentrations of FAAs even as its plasma levels
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Based on the inhibitory potency of C for HDAC we
2022-07-20

Based on the inhibitory potency of C646 for HDAC6, we monitored α-tubulin acetylation; an HDAC6 substrate. C646 treatment provided pronounced inhibition of α-tubulin acetylation after both 6 and 20h of incubation, which argues against HDAC6 inhibition by C646 in RAW264.7 cells. The observed effect o
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GSK dimethylpiperidin yl butoxy phenyl piperidine carbonyl n
2022-07-20

GSK-835726 (3-[4-[4-[4-[4-(3,3-dimethylpiperidin-1-yl)butoxy]phenyl]piperidine-1-carbonyl]naphthalen-1-yl]propanoic acid) is a dual H1/H3 receptor antagonist with the potential to be used in allergic rhinitis. Likewise GSK-1004723, the drug-likeness criteria have not been passed by this drug candida
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The second class of proteins
2022-07-19

The second class of proteins necessary for maintaining A-1155463 dynamics is chromatin modifiers, which are considered ‘writers’ and ‘erasers’ and are responsible for modifications of histone N-terminal tails. These post-translational modifications can have direct or indirect effects on chromatin s
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In the H NMR spectrum two pairs of
2022-07-19

In the 1H NMR spectrum two pairs of doublet resonances arising from the protons in the aromatic moiety of the two diastereoisomers can be readily observed around 7.5–7.6 ppm. These resonances can be used to detect and quantify the two diastereoisomers. From the results presented in Fig. 1A it can be
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