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Ghrelin contains an n octanoylation at
2021-10-23

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 overall very satisfactory potency profile of compounds
2021-10-23

The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic Tenovin-6 core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly sen
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More specific quantitative assays for
2021-10-22

More specific quantitative assays for DiXaIs are based on the inhibition of chromogenic or clotting activity of Factor Xa. During drug development, Kubitza developed an endogenous Anti-Factor Xa assay [45], which is very sensitive to Rivaroxaban drug concentration. This assay was based on Factor Xa
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The above inferences concluded that histidine
2021-10-22

The above inferences concluded that histidine is enhancing the overall stability and rigidity of the protein which further might be restraining the protein during the transition from inactive to active state and vice-versa present in the SANT domain. Since the SANT domain binds with histone via elec
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Kobe0065 br Experimental br Results br Discussion In
2021-10-22

Experimental Results Discussion In this study, we performed molecular docking analysis and in vitro studies to determine whether genistein binds to HIF-1α in BC Kobe0065 and identify the residues involved in this interaction. We found that some functional groups (residues) mimic the bindin
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Mitochondrial binding by HK prevents mortality by inhibiting
2021-10-22

Mitochondrial binding by HK prevents mortality by inhibiting pro-apoptotic factor (Bcl-2 family)-mediated opening of the mitochondrial permeability transition pore (mPTP) (Arora and Pedersen, 1988, Calmettes et al., 2016, Kodde et al., 2007, Pedersen et al., 2002, Rosano, 2011, Schindler and Foley,
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However HDACi can also increase the acetylation of other
2021-10-22

However, HDACi can also increase the acetylation of other transcription factors that regulate p65 transcriptional activity. The HDACi-induced activation of p65 can be negated by acetylated STAT1, which can specifically bind to p65 and inhibit its transcriptional activity 81, 82, 83. Interestingly, a
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br Conclusion and future perspectives
2021-10-22

Conclusion and future perspectives In the setting of myocardial I/R stress, HDAC activity is induced and contributes to myocardial injury. HDAC inhibition appears to protect the Nitrotetrazolium Blue chloride sale from I/R injury by activating a variety of pro-survival molecular pathways. From a
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Finally a potentially effective therapeutic
2021-10-22

Finally, a potentially effective therapeutic approach is to target the LDH enzymes that mediate bidirectional conversion of pyruvate into lactate. In particular, because LDHA is the predominant isoform expressed in glycolytic tumours, an array of LDHA-targeting compounds have been proposed and valid
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Selection of the month br Fibrosis br Liver protection devic
2021-10-22

Selection of the month Fibrosis Liver protection device Non-alcoholic steatohepatitis Genetic metabolic liver disease Hepatitis C virus (HCV) infection Hepatitis B virus (HBV) infection Cirrhosis Regeneration Introduction Upon catalysis by hepatic and bacterial enzymes, c
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The effect of GCK NES
2021-10-22

The effect of GCK-NES mutations on enzyme kinetics and protein stability might account for the hyperglycaemia that characterizes MODY2 patients, since reduced GCK activity would increase the threshold for glucose stimulated insulin release in beta-cells [31,37,49]. However, a more in depth functiona
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According to the aforementioned preclinical and clinical
2021-10-22

According to the aforementioned preclinical and clinical data, GHS-R1a blockade appears to be a potential pharmacological approach to treat AUD. Given that GHS-R1a has high constitutive (ligand-independent) activity, inverse agonism of the receptor may exert more potent and desirable effects than pu
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The advent of the genomic era has allowed
2021-10-22

The advent of the genomic era has allowed greater detailed investigation of enzymatic properties and has shown that specific enzyme activity is linked to the substrate utilization profiles of the isoenzymes [30], [31]. Not surprisingly, the functional four β-galactosidases from A. niger F0215 shared
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br Materials and methods br Results and
2021-10-21

Materials and methods Results and discussion Conclusions Notes Declaration of interest statement Acknowledgment This work was supported by the National Natural Science Foundation of China (No. 21775132, 21505112), Scientific Research Foundation of Hunan Provincial Education Departm
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According to its major function
2021-10-21

According to its major function as master regulator of BA homeostasis, FXR has been shown to have a specific tissue distribution; it is expressed along the entire gastrointestinal tract with a peak in the liver and ileum, as well as in the kidney, and adrenal glands [30], [66], [135]. Low FXR expres
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