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br All platelet agonists acting through specific receptors
2022-04-18
All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) or
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CB-5083 In order to determine whether NF B could interact
2022-04-18
In order to determine whether NF-κB could interact with GSTP1-1 promoter, we performed EMSA. One NF-κB like (−98κB) binding site was previously described in the GSTP1-1 promoter as a regulator element. However, few data about this site have been published and its role in the GSTP1-1 gene regulation
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After the synthesis of methylsulfonyl or tetrazole
2022-04-18
After the synthesis of methylsulfonyl or tetrazole surrogate derivatives, compounds synthesized by introducing hydrogen, fluoro, and methyl groups into the head group of GPR119 agonists were synthesized. Compounds – were synthesized by reacting hydroxybenzaldehyde with fluorine, hydrogen, or a methy
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A high throughput screening campaign
2022-04-18
A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also co
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Pimozide mg TDG furthermore is inhibited in its excision of
2022-04-18
TDG, furthermore, is inhibited in its excision of U on the NCP relative to duplex, though not to the same extent as SMUG1. There is no significant difference between TDGFL and TDG82−308, consistent with a previous report that the N- and C-termini missing from TDG82−308 do not affect the excision of
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The neuronal glycine receptor HSOR allopregnanolone pathway
2022-04-18
The neuronal glycine receptor/3α-HSOR/allopregnanolone pathway may also be extended to the central nervous effects of gelsemine and koumine in brain. 3α-HSOR is expressed in certain brain regions in rats and humans, such as the limbic system including hypothalamus, hippocampus and amygdala, in addit
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br NMDA receptor LBDs The study of GluA was
2022-04-18
NMDA receptor LBDs The study of GluA2 was later expanded to include NMDA receptors [22]. NMDA receptors are obligate heterotetramers that are composed of two glutamate-binding subunits and two glycine-, or d-serine-, binding subunits. In this study, crystal structures of the NMDA receptor glycin
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br STAR Methods br Acknowledgments
2022-04-18
STAR★Methods Acknowledgments We would like to thank Dr. Xiping Cheng for help with the immunohistochemistry staining, Qi Su for help with gene expression analysis, and Dr. Chaoying Liang at the UTSW Genomics Microarray Core facility for assistance on RNA-seq. W.-H.L. was supported by grant awa
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br GLP R expression in the vascular endothelium Immunohistoc
2022-04-18
GLP-1R expression in the vascular endothelium Immunohistochemistry studies utilizing GLP-1R antibodies that have now been demonstrated to be non-specific [46], initially identified GLP-1R protein expression in both mouse mesenteric artery SMCs and heart coronary SMCs [7]. However, evidence for VS
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br Introduction When human red blood cells hRBC are suspende
2022-04-18
Introduction When human red blood IWR-1-endo receptor (hRBC) are suspended in depolarising Ringers, they respond by opening a non-selective voltage-dependent cation pathway, the NSVDC channel, which is permeable to mono- and divalent cations [1], [2], [3]. In patch clamp experiments on excised hR
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The molecular nature of these putative Ca channels
2022-04-18
The molecular nature of these putative Ca2+ Protease Inhibitor Cocktail (100X in DMSO, EDTA plus) australia is at present unknown. Apart from the NSVDC channel, which is permeable to Ca2+ [27], [15] functional Ca2+ channels have been identified in patch clamp experiments [28]. These channels, which
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One effective approach to fine tuning the lipophilicity prof
2022-04-18
One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Levodopa scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well as Amgen
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Our previous study had shown that
2022-04-18
Our previous study had shown that silencing FFAR1 expression weakened the action of PIO in increasing insulin secretion in lipotoxic β Tenovin-3 [6]. Resent research found that PIO promoted insulin secretion by upregulating FFAR1 [17]. Therefore, we presumed that FFAR1 may be involved in the anti-l
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Regorafenib EZH affects cancer by regulating the expression
2022-04-18
EZH2 affects cancer by regulating the expression of target genes [22]. EZH2, together with SUZ12 and EED, forms the polycomb repressive complex 2 (PRC2), which catalyzes trimethylation of histone H3 lysine 27 (H3K27me3) [23,24]. PRC2 may recruit other polycomb complexes, DNA methyltransferases, and
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In addition to the regulation of SV
2022-04-16
In addition to the regulation of SV exo- and PLX3397 by Ca2+ influx retrieval of SV membranes depends on the exocytic insertion of SV components into the presynaptic membrane: If exocytic SV fusion in neurons is abrogated by genetic inactivation of the core release machinery (e.g. knockout of Munc1
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