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A linker length of and
2022-03-01

A linker length of 4 and 5 atoms was found to be optimal ( and ) compared to the only weakly active compounds with longer linkers ( and ) or the inactive compounds with shorter linker chains (–). In a next step incorporation of hetero-atoms in the linker was explored (). An amide linker as in and di
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br Introduction Cell surface receptors are central to the
2022-03-01

Introduction Cell surface receptors are central to the interaction of cells with their surroundings and play an important role in determining functional responses. These receptors are integral membrane proteins responsible for the binding of extracellular signaling molecules and transduction int
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Several groups studied CTD mouse models which
2022-02-28

Several groups studied CTD mouse models, which largely mimicked the symptoms (i.e. impaired cognition and autistic-like behaviour) of the human disease (Kurosawa et al., 2012; Baroncelli et al., 2016; Stockebrand, 2018). The CRT-1 knockout mice showed a drastic deterioration in the GABAergic system,
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br Introduction Prostate cancer is the most commonly diagnos
2022-02-28

Introduction Prostate cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths in men in the United States, accounting for about 30,000 cancer deaths annually [1]. Epidemiological studies that show geographical variations in prostate cancer incidence and mortalit
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br Funding This work was supported
2022-02-28

Funding This work was supported by grants of the National Academy of Sciences of Ukraine within the programs “Molecular and cellular biotechnologies for medicine, industry and agriculture” (#35-2018), “Scientific Space Research for 2018-2022” (#19-2018), “Smart sensory devices of a new generation
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With the exception of R none of the other residues
2022-02-28

With the exception of R5.40310, none of the other residues would appear to be in a position to mediate direct agonist interactions in the active state GLP-1R structures. ECL2 within the GLP-1R is important for affinity and efficacy of both extended and processed GLP-1 peptides [24]. Though distal fr
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br Role of BKCa in Cardiovascular System br Perspective
2022-02-28

Role of BKCa in Cardiovascular System Perspective for BKCa Channels as Potential Target for Cardiovascular Diseases The intermediate conductance Ca-activated K+ channels (IKCa; KCa3.1, also known as SK4, IK, IKCa1, SMIK) were first discovered in erythrocytes by Gardos (1958) and then also fo
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Palosuran receptor br Materials and methods br Results
2022-02-28

Materials and methods Results Discussion Prior studies established that Notch signaling regulates the differentiation of hair cells and supporting cells during inner ear development (reviewed in Kiernan (2013)). Notch signaling is a multistep process that requires the interaction between a
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Interestingly GAL has also been shown to be co expressed
2022-02-28

Interestingly, GAL has also been shown to be co-expressed and/or secreted in luteinizing hormone releasing hormone (LHRH) (Merchenthaler et al., 1991, Marks et al., 1994) and kisspeptin (KISS) neurons (Porteous et al., 2011). Furthermore, GAL was shown to stimulate luteinizing hormone (LH) secretion
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Activation of FXR or TGR has overlapping but also
2022-02-28

Activation of FXR or TGR5 has overlapping but also differing effects on metabolic regulation and inflammation [1]. In this report, we demonstrate that in addition to preventing the progression of obesity, NAFLD, and atherosclerosis, activation of BA receptors can also promote regression of these com
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Macroautophagy hereafter referred to as autophagy
2022-02-28

Macroautophagy (hereafter referred to as autophagy) depends on an intracellular lysosome-dependent degradation system that maintains cellular metabolism and homeostasis [11]. Genes involved in these processes are termed autophagy-related genes (ATGs), which regulate autophagosome formation and compl
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citco receptor We thus asked whether enhanced AEA levels in
2022-02-28

We thus asked whether enhanced AEA levels in the citco receptor reduce the level of age-related inflammatory changes and slow down brain ageing. To answer this question we compared the morphology of microglia and level of pro-inflammatory cytokines in the hippocampus of young and old wild-type and
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br Sources of funding This work was supported by
2022-02-28

Sources of funding This work was supported by grants from the Canadian Institutes of Health Research (CIHR) (No. MOP-111096) and from the Heart and Stroke Foundation of Canada awarded to Dr. Danielle Jacques. Disclosures Acknowledgments Introduction A large number of epidemiological, hu
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Computational approaches such as docking and
2022-02-28

Computational approaches such as docking and classical molecular dynamics (MD) are now commonly used to study the structure and dynamics of proteins as well as associated protein-ligand interactions [12]. A fundamental requirement of MD in order to accurately determine the behavior of a protein over
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Traditional methods for HATs activity assays mainly depend o
2022-02-28

Traditional methods for HATs activity assays mainly depend on radioisotope labelling of histone substrates, which is limited by the complex procedures, hazards and wastes of radioactive materials. Hence, various alternative approaches such as electrochemical analysis, fluorescence and colorimetric a
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