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Historically pharmacological investigations have been carrie
2021-09-06

Historically, pharmacological investigations have been carried out by first identifying a biological response to a ligand, and then subsequently using that ligand to identify the receptor(s) responsible for the response (Wilson et al., 1998). However, this approach needed revision with the discovery
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The diversity of biological properties
2021-09-06

The LY2109761 of biological properties and interactions of GSK-3 have been reviewed recently (, , , , ). The interactions of GSK-3 in the signaling pathways induced by nutraceuticals is covered in the review by ) in this special issue of . GSK-3 is a frequent target of many nutraceuticals such as c
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Also the decrease in adipocyte cAMP levels seen
2021-09-06

Also, the decrease in adipocyte cAMP levels seen after an acute glucose challenge in wild-type mice was strongly reduced in mice lacking GPR81, indicating that the activation of PDE3B alone was not sufficient to mediate the effect of insulin on cAMP levels and lipolytic activity. The fact that insul
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In addition during the preparation of this manuscript Oka et
2021-09-06

In addition, during the preparation of this manuscript, Oka et al. [7] demonstrated that LPA acts as receptor ligand for GPR35 and that LPA is more potent than KYNA in eliciting a calcium mobilization (EC50: 30nM vs. 39μM for LPA and KYNA, respectively). Other endogenous GPR35 ligands, therefore, mi
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We suggest that the FRET enhancement observed when the modif
2021-09-06

We suggest that the FRET enhancement observed when the modified mD1 protein containing Acd at position 28 was excited at 260nm (), may differ from the diminution in fluorescence observed following excitation at 280nm due to the excitation of different transitions in Trp (i.e., the L and L transition
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Transient forebrain ischemia in rodents induces a
2021-09-03

Transient forebrain ischemia in rodents induces a reduction in expression of mRNA encoding the AMPA receptor subunit GluR265, 66, 67, 68, 69 (Fig. 3). gluR2 mRNA expression is markedly reduced in the CA1 region (the quinpirole synthesis region most vulnerable to ischemia-induced damage), but not in
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In order to test whether the enhanced hyperpolarization in t
2021-09-03

In order to test whether the enhanced hyperpolarization in the presence of increasing amounts of extracellular Ca2+ could be due to an ionophore effect of NS309, red cell uptake of 45Ca and partition of 45Ca into a water/n-octanol phase +/−100 μM NS309 were determined. However, no indication of iono
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The objective of this study is to design and
2021-09-03

The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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Next we aimed to investigate if the cardiac apoptosis induce
2021-09-03

Next, we aimed to investigate if the cardiac apoptosis induced by CO-HFD, LA, T1DM or hyperglycemia involves up-regulation and activation of Fas/FasL-mediated cell death and if such effects are mediated by ROS and/or Ca+2/calcineurin/NFAT signaling axis. Similar to previous reports, [8], [9], [10],
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Liposomes that are less than nm in diameter are
2021-09-03

Liposomes that are less than 200nm in diameter are necessary to optimize uptake of liposomes by dgat inhibitor (Oesterling et al., 2014). The liposomes constructed in these experiments were found to be sufficiently small in diameter for use in in vivo and in vitro experiments. Even smaller diameter
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In addition JMJ proteins respond to biotic stress
2021-09-03

In addition, JMJ proteins respond to biotic stress and abiotic stress in plants. Rice genes OsJMJ704 and OsJMJ705, which have demethylase activities of H3K27me2/3 and H3K4me2/3, respectively, regulate defense-related genes and affect the defense ability of rice against bacterial pathogen Xoo (Li et
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Evidence indicates that astrocytes play a role in the modula
2021-09-03

Evidence indicates that astrocytes play a role in the modulation of NMDAR activity in the CA1 (Henneberger et al., 2010; Papouin et al., 2017a, Papouin et al., 2017b; Robin et al., 2018). Therefore, we sought to examine whether astrocytes are involved in the H1 receptor antagonist/inverse agonist-in
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BMS265246 The study by Pigna and collaborators
2021-09-03

The study by Pigna and collaborators provides an elegant demonstration why class IIa HDAC inhibition may not be suitable to protect the neuromuscular function in ALS, consistent with a recent study that showed only a transient protection of motor performance after treatment of the same ALS model wit
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In first wave first generation
2021-09-03

In 2013, first-wave, first-generation drugs telaprevir and boceprevir was the first protease inhibitors (PIs) incorporated in Brazilian Clinical Guidelines for the treatment of patients infected with HCV Paclitaxel 1. Based on this 2013 Clinical Guideline, telaprevir could be used for both naïve and
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Since TgGC resisted several knockout attempts
2021-09-03

Since TgGC resisted several knockout attempts with CRISPR-Cas9, we utilized traditional epitope tagging and an auxin-inducible degron (AID) system (Brown et al., 2017, Brown et al., 2018, Long et al., 2017) to detect and regulate TgGC expression. TgGC localizes to the apical cap region of the plasma
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