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A number of synthetic GPR agonists have been reported
2022-06-08
A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,
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In contrast to UDG SMUG exhibits dramatically lower product
2022-06-08
In contrast to UDG, SMUG1 exhibits dramatically lower product yield in its excision of U, and this is not dependent on sequence context. Though we cannot rule out that a small amount of the product is derived from a duplex contaminant, our extensive purification techniques limit the amount of contam
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The need for an inflammatory risk profile was
2022-06-08
The need for an ‘inflammatory risk profile’ was recently discussed by several investigators. The present study is all the more significant in that it shows that a phenomenon that is influenced by various atherosclerotic risk factors and acute phase proteins is, indeed, associated with a less favorab
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br Materials and methods br Results br Discussion In
2022-06-08
Materials and methods Results Discussion In nerve terminals, Na+-dependent glutamate transporters of the plasma membrane are responsible for the maintenance of low (non-toxic) extracellular glutamate concentrations and accomplish uptake of glutamate into the PI3K Akt mTOR Compound Library s
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br Methods GLUT DS was diagnosed
2022-06-08
Methods GLUT1DS was diagnosed either when analysis of the SLC2A1 gene showed a pathogenic mutation and/or when cerebrospinal fluid (CSF) analysis met the criteria for GLUT1DS: a CSF Lamivudine synthesis below the 10th percentile, a cerebrospinal fluid (CSF) to blood ratio below the 25th percenti
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br Introduction Maintaining blood glucose within an appropri
2022-06-08
Introduction Maintaining blood glucose within an appropriate range is crucial for survival. In diabetes, those who suffer episodes of severe hypoglycemia have an increased risk of death [1], [2]. The Prochlorperazine is especially dependent on an adequate, continuous supply of circulating glucos
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br Do the actions of GLP R
2022-06-08
Do the actions of GLP-1R agonists on the vascular endothelium account for GLP-1R agonist-mediated cardioprotection? The previous section highlighted the recent clinical evidence from cardiovascular outcomes studies supporting the notion that GLP-1R agonists confer cardioprotective actions in pati
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br Conflict of interest statement br
2022-06-08
Conflict of interest statement Acknowledgements This work was supported by the National Health and Medical Research Council of Australia (NHMRC) (project grants [1061044], [1065410] and [1126857], and NHMRC program grant [1055134]); P.M.S. and A.C. are NHMRC Principal and Senior Principal Rese
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Ghrelin is a brain gut peptide hormone secreted
2022-06-08
Ghrelin is a brain-gut peptide hormone secreted from the stomach to stimulate food intake by acting on its receptor, growth hormone secretagogue receptor (GHSR). GHSR is expressed throughout the brain and in NPY/AgRP neurons in the ARC (Cowley et al., 2003, Willesen et al., 1999). Ghrelin-expressing
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FPR activation stimulates multiple signal
2022-06-07
FPR1 activation stimulates multiple signal transduction pathways responsible for various neutrophil functions, such as adhesion, chemotaxis, phagocytosis, mechlorethamine of secretory granules, and superoxide anion radical (O2) production, which contribute to the physiological inflammatory response
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Thrilled by these promising results our quest for discoverin
2022-06-07
Thrilled by these promising results, our quest for discovering new PPAR-γ/FFAR1 co-agonists was directed towards exploring the other two new scaffolds. So, in this proposed manuscript, we will describe our efforts regarding the synthesis, biological evaluation and molecular docking studies of the be
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In order to understand the determinants of high affinity
2022-06-07
In order to understand the determinants of high affinity of with amide side chain, an X-ray crystal structure of human liver FBPase in complex with was determined (). The position of phosphonate group and tricyclic scaffold of is similar to those of with no side chain, which suggests the formati
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We characterized the enzyme corresponding
2022-06-07
We characterized the enzyme corresponding to N1. FPP was the most effective substrate as allylic diphosphate, and the activities with GPP and DMAPP were 50% and 11% that with FPP, respectively. The analysis of the prenols resulting from the treatment of prenyl diphosphates with HPF phosphatase () r
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Over of all melanomas have activating
2022-06-07
Over 50% of all melanomas have activating BRAF mutations [29] and inhibition of the Ras/Raf/MEK/ERK signaling pathways is one of the most promising treatments for malignant melanoma [30]. However, studies using BRAF inhibitors have identified various feedback mechanisms to activate BRAF pathway in m
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The ETA receptor has a higher
2022-06-07
The ETA receptor has a higher affinity for endothelin-1 than the two other agonists, with an affinity order of endothelin-1>endothelin-2>endothelin-3, while the ETB receptor exhibits similar affinities for all three isopeptides (Arai et al., 1990b, Sakurai et al., 1990). Earlier studies of the selec
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