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br Involvement of gap junctions and Panx in
2021-09-13
Involvement of gap junctions and Panx1 in spinal cord processing of pain information Several studies indicated that GJs in the CNS contribute to pain. A common finding in such studies is that intrathecal administration of GJ blocker attenuates pain behavior. For example, intrathecal CBX attenuate
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Doxycycline HCl The co crystal structure of GPR
2021-09-13
The co-crystal structure of GPR40 complexed with TAK-875 provided precise structural information for the rational design of novel GPR40 agonists. The key interactions between the carboxylate with the residues Arg183, Arg258, Tyr91 and Tyr240 of GPR40 were observed. And Trp174ECL2 was oriented nearly
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This study introduces a mouse model carrying
2021-09-13
This study introduces a mouse model carrying the point mutation R258W in Ffar1, which abolishes the stimulation of insulin secretion in response to long chain fatty acids. The minimal genetic alteration mirrors the human situation and has the advantage over conventional knockout/congenic mouse model
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In conclusion our results showed that
2021-09-13
In conclusion, our results showed that FFAR1 can mediate the effect of PIO in attenuating β-cell lipoapoptosis through anti-oxidative stress, which may be related to the activation of the PLCγ-ERK1/2-PPARγ pathway. Our study helps not only to distinguish the role played by FFAR1 in lipotoxicity, but
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We compared the mixotrophic growth of
2021-09-13
We compared the mixotrophic growth of mutant DRHB1486 and the wild-type at different light intensities. The mutant grew at a similar rate as the wild-type at a low light intensity but much more slowly at a high light intensity (Fig. 3). Because the slr2094 mutant was unable to grow under photoautotr
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The molecular target of N BPs is farnesyl diphosphate syntha
2021-09-13
The molecular target of N-BPs is farnesyl diphosphate synthase (FPPS), a crucial enzyme at the branch point of cholesterol and isoprenoid synthesis in the mevalonate pathway [5]. Because they bind calcium ions, N-BPs accumulate quickly in the skeleton and are internalised by osteoclasts, leading to
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ATN Ac PHSCN NH is a small
2021-09-13
ATN-161 (Ac-PHSCN-NH2) is a small peptide antagonist of integrin α5β1, a recently developed anticancer drug that interacts with the N-terminus of the β1 region of integrin α5β1 to lock integrin α5β1 in its non-activated conformation (Wang et al., 2016). The drug has been tested in Phase 2 clinical t
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Contrary to the transient nature
2021-09-13
Contrary to the transient nature of signal transmission through PLCβ, genome-wide RNAi screens revealed that the signaling events driven by Gαq that result in aberrant cell proliferation depends on highly specific protein-protein interactions, rather than solely on diffusible second messenger system
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Compounds that induce exocytosis in cultured cells
2021-09-13
Compounds that induce exocytosis in cultured INNO-406 include Ca2+-dependent [14] or Ca2+-independent [15] mechanisms. Ca2+-dependent exocytosis releases soluble enzyme content from lysosomes [16] operating by increasing the cytosolic concentration of Ca2+[13] by recruiting extracellular Ca2+[14], l
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br HO regulation and physiology The catabolism of cellular
2021-09-11
HO-1: regulation and physiology The catabolism of cellular heme in humans and other species is mediated by the heme oxygenase (HO) family of enzymes (E.C. 1:14:99:3; heme-hydrogen donor:oxygen oxidoreductase). The HOs localize primarily to the endoplasmic reticulum (ER) where they serve, in conce
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Although resembling a differential symbiotic relationship
2021-09-11
Although resembling a differential symbiotic relationship, interplay between prostate tumour CAFs promotes PKM2/HIF-1-driven transcriptional regulation in prostate cancer cells that exploit lactate produced by CAFs and undergo epithelial-to-mesenchymal transition (EMT) [21]. Although recent observat
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In addition to the increase of extracellular glutamate
2021-09-11
In addition to the increase of extracellular glutamate, ICH can also increase the levels of reactive oxygen species (ROS) and oxidative stress. Although the products of red blood cell lysis and plasma components, as well as the excitotoxic effect of glutamate have been to increase oxidative damage (
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vegf inhibitor br Methods br Results br Discussion In the
2021-09-11
Methods Results Discussion In the general population BNP has been established as a marker for vegf inhibitor failure diagnosis. Moreover, there is growing evidence that elevated levels of natriuretic-peptides may improve CV risk prediction in the general population above traditional risk f
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For the SAR study human haspin kinase inhibitory activity of
2021-09-11
For the SAR study, human haspin kinase inhibitory activity of the various compounds was evaluated using the same assay utilized for the HTS, except in the presence of varying test compound concentrations. DYRK2 kinase inhibitory activity was measured by P-incorporation into Woodtide peptide substrat
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Glycogen synthase kinase GSK is an evolutionarily conserved
2021-09-11
Glycogen synthase kinase-3β (GSK-3β) is an evolutionarily conserved serine/threonine kinase that plays multifaceted role in diverse cellular and neurophysiological processes [8]. GSK-3β is regulated by inhibitory serine and stimulatory tyrosine phosphorylation on Ser9 and Tyr216 respectively [9]. Dy
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