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To maintain low Glu concentrations in
2021-12-23
To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino inno-206 is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocytes, and in
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As a part of our continuing efforts towards discovery
2021-12-23
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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br Results and Discussion br STAR
2021-12-23
Results and Discussion STAR★Methods Author Contributions Conflicts of Interest J.P.F. is a consultant for AstraZeneca, BMS, Johnson and Johnson, Novo Nordisk, and Sanofi, a member of the advisory panel for AstraZeneca and Sanofi, a member of the speaker’s bureau for Sanofi and Novo Nordi
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Trifluoromethyl ketones and fluorophosphates were the first
2021-12-22
Trifluoromethyl ketones and fluorophosphates were the first generation FAAH inhibitors identified. They showed good in vitro FAAH inhibition potency, but most of them exhibited poor selectivity for FAAH over other serine hydrolases (such as the triacylglycerol hydrolase and the membrane-associated h
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DZNep is a PRC inhibitor that
2021-12-22
DZNep is a PRC2 inhibitor that inhibits S-adenosylhomocysteine hydrolase, resulting in cellular accumulation of S-adenosylhomocysteine. S-adenosylhomocysteine is a competitive inhibitor of methyl donor for methyltransferases [38]. DZNep targets EZH2 by reduction in the level of the enzyme H3K27me3 a
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In Arabidopsis GCN containing protein complexes
2021-12-22
In Arabidopsis, GCN5-containing protein complexes are found to be involved in cell differentiation, leaf and floral organogenesis [[8], [9], [10]]. AtHAC1 has involvement with root elongation, flowering, fertility and de novo shoot regeneration [11,12]. AtHAM1 and AtHAM2 control flowering time by ep
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br Conclusion H R H
2021-12-22
Conclusion H1R, H2R, and H3R mRNAs were expressed in rat OE. Moreover, these three histamine receptors were present in the cytoplasm of ORNs in OE. This is the first report of the expression and localization of histamine receptors in mammalian OE. These findings indicate that histamine may play a
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In our substudy patients carrying the Ile Val or
2021-12-22
In our substudy, patients carrying the Ile/Val or Val/Val genotypes had significantly worse DFS compared to patients carrying the Ile/Ile genotype, after adjustment for potential confounders. Two previous studies examining the association between HER2 Ile655Val polymorphism and trastuzumab response
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br Materials and methods br Author contributions br
2021-12-22
Materials and methods Author contributions Acknowledgments We thank members of the Skaar laboratory for critical evaluation of the manuscript. This work was supported by grants from the National Institutes of Health, R01AI069233 (EPS), and T32GM008554-21 (LJL). Introduction Pseudomonas
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Although it is currently unknown
2021-12-22
Although it is currently unknown why the longer splice variant found in the human has not been found in any other species, similar results have been reported for other receptors, including the more helpful hints receptor splice variant ERbeta2 identified in human and primate, but not other species
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GPR A a G protein
2021-12-22
GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic potassium channel blocker [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads
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br Acknowledgements We thank the support
2021-12-22
Acknowledgements We thank the support of the National Natural Science Foundation of China (NSFC) project 81501342 and support from the Disciplinary Group of Oncology and Immunology program of Xinxiang Medical University. Introduction First described as a new clinical entity in 1981, the Acqui
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br Reactive Dicarbonyls and Mitochondrial
2021-12-22
Reactive Dicarbonyls and Mitochondrial Dysfunction Although mitochondrial dysfunction has been suggested to be one of the main pathogenic mechanisms in diabetic neuropathy, little is known about the nature and extent of mitochondrial damage resulting from chronic hyperglycemia. Mitochondria funct
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The aims of the present study
2021-12-22
The aims of the present study were to further investigate the localisation of glycine and GABAA receptors on individual neurons and how closely these two receptor types were associated with each other by carrying out double immunofluorescent labelling and imaged using confocal laser scanning microsc
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In conclusion we have designed and
2021-12-22
In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date, c
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