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TGR is a class A GPCR
2021-10-01

TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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It is important to control hyperglycaemia because it
2021-10-01

It is important to control hyperglycaemia because it can contribute to serious complications. Hyperglycaemia can be managed by maintaining stable blood glucose levels inside the normal range. This can be achieved by various strategies such as diet, medications and exercise (O’Keefe & Bell, 2007). Se
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Here we studied GLUT targeted nanomedicines as
2021-10-01

Here, we studied GLUT1-targeted nanomedicines as a new strategy directed to overcome vascular barrier, enhancing delivery and efficacy in solid tumors. These nanomedicines were prepared by controlled installation of glucose on polymeric micelles incorporating the antitumor agent cisplatin, which is
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br Results br Discussion Using a novel
2021-10-01

Results Discussion Using a novel viral vector for norepinephrine-targeted gene deletion, we have shown that glucocorticoid receptor Bleomycin Sulfate from locus coeruleus norepinephrine neurons reduces social interaction specifically in female mice. This effect is not attributable to changes
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Fpr which belongs the family of the formyl peptide receptors
2021-10-01

Fpr1, which belongs the family of the formyl peptide receptors with FPRL1 and FPRL2, is the principal receptor for formylated peptides which prototype is the tri-peptide fMLF. Fpr1 is highly expressed on neutrophils and macrophages [6,30], promotes their migration into the mucosa and lumen in respon
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br Acknowledgements and disclosures This work was supported
2021-09-30

Acknowledgements and disclosures This work was supported in part by the National Institutes of Health (R01 HL-131673-01A1) and the Veterans Administration (BX-002539-01), United States. The authors have nothing to disclose concerning any conflict of interest. Introduction Adaptations are ofte
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br Introduction The Ras superfamily of small GTPases is
2021-09-30

Introduction The Ras superfamily of small GTPases is composed of more than 150 protein members involved in a wide variety of biological processes, such as proliferation, differentiation, cytoskeletal organization, and protein trafficking [1]. The Ras superfamily proteins act as molecular switches
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A linker length of and atoms was found to be
2021-09-30

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 d
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The glycine receptor is an
2021-09-30

The glycine receptor is an ionotropic neurotransmitter receptor coupled to a chloride ion channel. Glycine receptors are typically described as inhibitory and distributed in the spinal cord and brainstem, though mRNA transcription labelling studies in rats show expression in the hippocampus, cingula
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Closantel Sodium br Introduction L Glutamate is one of
2021-09-30

Introduction L-Glutamate is one of the most prevalent excitatory signaling molecules in the central nervous system (CNS) (Salazar et al., 2016) and plays a crucial role in a variety of Closantel Sodium functions such as memory and learning (Danbolt, 2001, Nedergaard et al., 2002). At elevated co
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A main finding of this study was that
2021-09-30

A main finding of this study was that the impact of exogenous insulin on hippocampal memory and glucose utilization was GluT4-dependent. Although insulin was administered directly to the hippocampus, it is important to point out that such administration does indeed have physiological relevance; that
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br Prospects The prospects for
2021-09-30

Prospects The prospects for GABAergic Anisomycin mg can be projected from the rate at which new compounds have been introduced (Fig. 1) and the amounts used. More than three billion pounds of NCA-IA insecticides were used in the past seven decades. There was no target site cross-resistance of the
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To investigate the potential molecular mechanism of FXR medi
2021-09-29

To investigate the potential molecular mechanism of FXR-mediated regulation of liver cancer cell proliferation, gene expression profiles were determined using Agilent arrays in SK-Hep-1-FXR and NC after treatment with the FXR agonist GW4064. The results indicate that mTOR and S6k are involved in div
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br Other strategies for ferroptosis In addition to
2021-09-29

Other strategies for ferroptosis In addition to ROS-generating and GPX4 inactivating nanomaterials, small molecules and genetic manipulation targeting key factors in the ferroptosis pathway have also been tested for their anticancer effects [39,47,48]. Among a myriad of proteins involved in ferro
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In an effort to more fully explore the structure
2021-09-29

In an effort to more fully explore the structure–activity relationships of the ALLINIs and potentially attenuate resistance to known mutants, the central scaffold of these compounds was identified as a potential site for structural manipulation. Specifically, we wished to examine whether a scaffold
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