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Following the discovery of diketo compounds
2022-02-16
Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent Valinomycin based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bi
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br To explore further the functional impact of the similarit
2022-02-16
To explore further the functional impact of the similarity of the UTY and KDM6A proteins, the FANTOM5 human dataset was analysed to determine whether or not the genes were expressed at the same time in the same tissues (which would suggest that they are controlled by the same regulators) or with o
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Acknowledgements br Introduction Histamine mediates various
2022-02-16
Acknowledgements Introduction Histamine mediates various physiological functions and pathological actions through its interactions with histamine receptors that belong to the superfamily of seven transmembrane G-protein-coupled receptors (GPCRs) (Haas et al., 2008). Four histamine receptor subty
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Conflicting data concerning the involvement of H R on
2022-02-16
Conflicting data concerning the involvement of H2R on glycaemia has also arisen. Its antagonism was reported to decrease [35], not affect [36], [37] and increase [38], [39] 2536 levels. In comparison, the clinical experience with antipsychotic drugs generated clearer evidence for the involvement of
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Acknowledgement This work was supported by grants from the
2022-02-16
Acknowledgement This work was supported by grants from the National Natural Science Foundation of China (No.81802749), Shenzhen Healthcare Research Project (No.SZBC2017029), the Science and Technology Foundation of Shenzhen (JCYJ20170412155231633, JSGG20170414104216477), National Key Research and D
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One of the key epithelium
2022-02-16
One of the key epithelium-derived factors required to maintain immune tolerance in the intestine is Indian Hedgehog (Ihh). Ihh is secreted exclusively by intestinal epithelial cells, and signals in a paracrine manner to the inhibitory receptor Patched1 (Ptch1) on Chlorothiazide in the mesenchyme. Bi
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P corneus is a freshwater hermaphroditic gastropod that is d
2022-02-16
P. corneus is a freshwater hermaphroditic gastropod that is distributed all over the world (Jopp, 2006). In previous works of our laboratory, we have characterized the activities of B-esterases and we have also reported that the exposure for 48h to chlorpyrifos inhibits ChE and CES of whole gamma-Se
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Interestingly myorelaxation and the stimulation of cGMP
2022-02-16
Interestingly, myorelaxation and the stimulation of cGMP production are properties also reported for sGC stimulators, such as YC-1 and BAY 41–2272 (i.e., indazole compounds that were discovered in the 1990s) [35]. They relax aortic ring contractions induced by phenylephrine, and their effects are si
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Preliminary analyses of these identified two bands
2022-02-15
Preliminary analyses of these identified two bands for MALDI-TOF/TOF have shown the presence of approximately 20 proteins, most of which have not yet been characterized. However, several proteins, such as cytochrome c oxidase [53], peroxiredoin II E [54] and alcohol dehydrogenase [55], have been ide
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Here we show that lactate
2022-02-15
Here we show that lactate activates the Gi-coupled receptor GPR81, which is exclusively expressed on adipocytes, and that lactate released from adipocytes in response to glucose and insulin mediates insulin-induced antilipolysis by activation of GPR81. Results Discussion Nutrients and their m
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The action of niacin in upregulating cAMP is most likely
2022-02-15
The action of niacin in upregulating cAMP is most likely determined by the milieu of adenylyl cyclase isoforms expressed in macrophages that are responsive to GPR109A activation. Several adenylyl cyclase isoforms, namely AC2, AC4 and AC7, are responsive to the stimulatory action of Gβγ G-protein sub
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In the course of our ongoing attempts to photolabel
2022-02-15
In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric cystamine australia type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise
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br Acknowledgments This research was supported by the Nation
2022-02-15
Acknowledgments This research was supported by the National Institutes of Health Grants GM58442 and GM084152, as well as the National Institutes of Health Predoctoral Training Grant 5T32GM008700-13. We thank Eric Oldfield (University of Illinois, Urbana-Champaign) for providing the FDPS inhibitor
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The coenzyme S adenosylmethionine SAM binding pocket
2022-02-15
The coenzyme S-adenosylmethionine (SAM)-binding pocket of Set7 is connected to the histone-tail binding groove by a conserved lysine-channel, similarly observed in vSET (Figures 2D and S3). The Set7 SAM-binding pocket is negatively charged as observed in other known HMTase structures. However, the b
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Consideration must be given to
2022-02-15
Consideration must be given to both the tissues themselves and to infiltrating immune cells. As highlighted by Maxwell and Eckardt [88], clinical trials of compounds targeting these pathways will require large numbers of participants and prolonged follow-up to identify rare and late complications or
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