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The differential tissue and ligand
2021-10-28
The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va
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In the course of our synthetic studies
2021-10-28
In the course of our synthetic studies, we also discovered an unprecedented application of Burgess reagent. Instead of generating an olefin by an intramolecular syn-elimination, the product resulting from the treatment of spirocyclic alcohols 11 and 12 with Burgess reagent led to the expansion of th
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Cx is the major molecule involved in the dynamic life
2021-10-28
Cx43 is the major molecule involved in the dynamic life cycle of GJIC (Cusato et al., 2006). Initially generated Cx43 exist in the cytoplasm and correctly transfer it to the plasma membrane during its life cycle (Ji et al., 2018). To understand the toxic effects of MC-LR on GJIC, Cx43 localization w
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br Conclusion br Methods br Introduction
2021-10-28
Conclusion Methods Introduction To predict such topologies, several algorithms have been developed. Quadparser (QP), developed by the Balasubramanian group have taken an approach where sequences matching G≥nN≤mG≥nN≤mG≥nN≤mG≥n model in which the lengths of G-tracts are at least n and lengths
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The regulatory effects of NADPH oxidase on ferroptosis might
2021-10-28
The regulatory effects of NADPH oxidase on ferroptosis might also relate to neuroinflammation. Although ferroptosis can trigger inflammatory responses in the brain, neuroinflammation, in turn, can also modify ferroptosis. It has been reported that inflammatory conditions such as those found in neuro
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In the Joint United Nations Program on HIV AIDS UNAIDS
2021-10-28
In 2015, the Joint United Nations Program on HIV/AIDS (UNAIDS) proposed that by 2020, 90% of people living with HIV should be aware of their HIV status, as the first part of 90-90-90 strategy to end AIDS epidemic. Early detection of HIV allows initiating care for proper treatment, which impacts in m
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gamma-Glu-Cys Here we dissect X chromosome dosage compensati
2021-10-28
Here, we dissect X chromosome dosage compensation (DC) in C. elegans to determine the effect of chromatin modifications on higher-order chromosome structure during long-range gene regulation. DC is exemplary because it controls hundreds of genes simultaneously, it distinguishes X chromosomes from au
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Initially the synthesized compounds from were evaluated
2021-10-27
Initially, the synthesized compounds from were evaluated for human GSNOR potency before generating additional SAR in order to understand scaffold feasibility and required functionality as illustrated in . Commercially available 4′-hydroxy-[1,1′-biphenyl]-4-carboxylic rat 4 having similar terminal
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The stress of accelerated lactate production in cancer cells
2021-10-27
The stress of accelerated lactate production in cancer AZ 10606120 dihydrochloride is moderated by the overexpression of lactate transporters – symporters for lactate anions and protons called monocarboxylate transporters (MCTs) – that are capable of bidirectional transport depending on the environ
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An alternative approach to improving
2021-10-27
An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl
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Materials and methods Standard curve for http
2021-10-27
Materials and methods Standard curve for methylglyoxal. Different concentrations (10, 25, 50, and 100μM) of pure MG (Sigma) were derivatized with 1,2-diaminobenzene and the absorbance of the resulting derivative was read by Cary 50 Bio UV-Visible spectrophotometer (Varian). One milliliter of total
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br Regulation of Glu transporters The pivotal role
2021-10-27
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino 3-CPMT calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcription
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br Declaration of interest br Acknowledgments This
2021-10-27
Declaration of interest Acknowledgments This work was financially supported by the National Natural Science Foundation of China (No. 31471615), the Introduction of Talent Research Start-up Fund of Anhui Polytechnic University (No. 2017YQQ017) and the Pre-research Project of National Natural S
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Type diabetes mellitus is characterised
2021-10-27
Type 2 diabetes mellitus is characterised by two major features: peripheral insulin resistance and impaired insulin secretion from pancreatic beta (-)-Bicuculline methiodide [1]. The condition occurs when the pancreatic beta cells are unable to compensate for increased insulin demand due to insulin
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br Experimental br Acknowledgments This project
2021-10-27
Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t
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