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As comparators compounds and were made using the
2022-01-29
As comparators, compounds and were made using the pyrazolopyridine core with the CF triazole attached. The 2-fluorophenyl group was replaced with the methylpyrimidine in compound . The potency of these compounds were very good and compound looks attractive from a physicochemical perspective as it
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Two distinct mechanisms have been
2022-01-29
Two distinct mechanisms have been described for niacin’s macrophage-based actions [21,22]. First, niacin blocks recruitment of macrophages to atherosclerotic lesions. Second, niacin upregulates macrophage ABCA1 and ABCG1, transporters involved in reverse cholesterol transport. Upregulation of choles
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Based on these findings we set out to identify
2022-01-29
Based on these findings, we set out to identify GPR109A agonists capable of biasing the receptor's signaling towards the functional anti-lipolytic and presumed therapeutic response, and away from the flushing side-effect pathways. Indeed, using recombinantly expressed GPR109A, two classes of compoun
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br Material and methods br Results br Discussion
2022-01-29
Material and methods Results Discussion Organisms have developed a variety of anti-glycation defense mechanisms. In L-Phenylephrine to the aldose-reductase-pathway or 2-oxoaldehyde dehydrogenase-pathway, the glyoxalase system is the only mechanism, which is not restricted to liver [19]. Th
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However it is unclear whether the
2022-01-29
However, it is unclear whether the parent and transition metal substitution in Keggin-type phosphomolybdic Meleagrin will reveal the best effects on α-glucosidase. Therefore, the Keggin-type H3PMo12O40 (abbreviated as PMo12) and three transition metal-substituted POMs (Na4PMo11VO40, Na6PMo11FeO40 an
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br Acknowledgements The authors are grateful
2022-01-29
Acknowledgements The authors are grateful for funding provided by the Health Research Council of New Zealand. Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, fa
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br Conflict of interest statement br Acknowledgements
2022-01-29
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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Taken together previous data suggest that ghrelin signaling
2022-01-29
Taken together, previous data suggest that ghrelin signaling is causally linked to alcohol use and may regulate alcohol seeking and consummatory behaviors [[66], [67], [68]]. As such, the ghrelin system may represent a therapeutic target for AUD. Here, we provide a narrative review of the existing l
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From a cell signaling perspective given the
2022-01-28
From a cell signaling perspective, given the importance of agonist-directed signaling and biased agonism, one goal of this research update was to review the known contributions of G protein-dependent versus β-arrestin-dependent signals toward promotion of beneficial functions that FFA4 facilitates.
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Receptor interactions and binding mode of in
2022-01-28
Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat
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The cases of the Berlin
2022-01-28
The cases of the Berlin and London patients also highlight our limits to defining an HIV cure. No signs of the virus have been found in numerous assays with multiple samples from diverse tissues that Timothy Brown has generously contributed to advance research over the past 12 years. In the case of
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br Hh Proteins at a Glance Hh
2022-01-28
Hh Proteins at a Glance Hh family proteins are evolutionarily conserved morphogens that provide cells with positional information and fate instruction during early embryonic development. After development, Hh ligands contribute to tissue homeostasis and wound healing 1., 2.. Consistent with these
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Furthermore we observed a striking difference between
2022-01-28
Furthermore, we observed a striking difference between BR 11257 and activators from the dicarboxylic signal transducer and activator of transcription 6 fragment receptor type in thermofluor measurements on thermostability. The dicarboxylic acids cinaciguat [30] and BAY 60-2770 (see Fig. 3) induced
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However a direct effect of ROS on GSNOR has
2022-01-28
However, a direct effect of ROS on GSNOR has also been described. Inhibition of GSNOR by ROS has been demonstrated for yeast [44], Arabidopsis[36], and Baccaurea ramiflora (Burmese grape) [45] suggesting that this could be a general mechanism of crosstalk between ROS and ·No signaling. Interestingly
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Importantly lactate and H exert some of
2022-01-28
Importantly, lactate and H+ exert some of their biological effects independently of each other, though sometimes through redundant pathways leading to a same biological effect, as for angiogenesis. In other cases, they can have antagonist effects: lactate was shown to stimulate extracellular matrix
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