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ganciclovir receptor br BA induced activation of TGR TGR is
2022-05-23
BA-induced activation of TGR5 TGR5 is a membrane-bound G protein-coupled receptor for BAs and its activation is dependent on cAMP formation and further stimulation of protein kinase A [53], [31]. The receptor is expressed in the enterochromaffin cells, smooth muscles, immune cells and more import
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br Conclusion In summary a
2022-05-23
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic chloride channels motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing
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The precise mechanism by which erastin
2022-05-23
The precise mechanism by which erastin inhibits SLC7A11-mediated cystine import it still unknown. The initially proposed mechanism, by which erastin binds a related transport protein, SLC7A5, and inhibits SLC7A11 in trans [25], was revised soon after, and it was suggested that erastin inhibits SLC7A
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Recently results obtained by our group
2022-05-23
Recently, results obtained by our group have demonstrated that hEECs are able to secrete NPY into the extracellular medium and that this peptide can induce an increase in the [Ca]i of these cells (Jacques et al., 2003b). In light of these results and those obtained in this study, we can speculate t
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DIS used standard methods for locating and contacting person
2022-05-23
DIS used standard methods for locating and contacting persons for interview, including the use of phone calls, letters, in person contact, and contact through social media. During this time period, contacts of persons with diagnosed HIV (first-generation contacts) were tested for HIV and, regardless
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Regulation of gene expression in mammalian cells is
2022-05-23
Regulation of gene expression in mammalian cells is governed by the epigenetic machinery, which includes several distinctive yet entangled branches. DNA and histone modifying enzymes, non-coding regulatory RNAs, and ATPase-dependent chromatin remodeling proteins all contribute to the dynamic alterat
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Histamine H and H receptors are considered as low affinity
2022-05-23
Histamine H1 and H2 receptors are considered as low affinity receptors (pKi of 4.2 and 4.3 respectively), whereas histamine H3 and H4 receptors as a high affinity receptors (pKi of 8 and 8.2 respectively) (Schreeb et al., 2013). Therefore it might well be that other histamine receptors might be invo
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These inhibitors possess a cap group build from cyclization
2022-05-23
These inhibitors possess a cap group build from cyclization of several amino-acid or non-amino-acid residues, four or more, with one residue bearing an alkyl arm terminated by ZBGs of various types: thiols, ketones or epoxides. In the case of romidepsin 30 (Fig. 7), the thiol group is initially in a
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Several classes of small molecules that
2022-05-23
Several classes of small molecules that modulate CDK8 activity have been reported in the patent literature (Fig. 1). A quinazoline derivative, Senexin B (SNX2-1–165, 1), showed CDK8 enzyme inhibitory activity with an IC50 value of 24–50 nM in different assay, and displayed potent, selective enzymati
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PU-WS13 The fibulins are a newly abundantly in
2022-05-21
The fibulins are a newly abundantly in the basement membrane of blood vessels. Among them, fibulin-1 is essential for elastin polymerization. Tropoelastin cannot be assembled into mature elastin fibrils without the functional fibulin-1. In adult blood vessels, pronounced fibulin 1 deposition can be
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PBI is an agonist of GPR and acts as an
2022-05-21
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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br Differences among flavivirus vaccines and
2022-05-21
Differences among flavivirus vaccines and implications for CD4 T cell immunity There are currently three classes of flavivirus vaccines in use – live-attenuated virus (for immunoprophylaxis against YF and JE), whole inactivated virus vaccines (JE, TBE) and chimeric vaccines (JE, DEN). The chimeri
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Harmine Thermal analysis of the NQ peptide
2022-05-21
Thermal analysis of the NQ21 peptide was performed with the Solar CM2203 spectrofluorometer. We prepared three 1 μg/mL peptide solutions with different Harmine levels (5.0, 7.4, 8.5) in 0.01 M phosphate buffers. Each solution was slowly heated up from 28 °C to 54 °C with a step of 1 °C. Spectra wer
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Functional studies based on patch clamp electrophysiology
2022-05-21
Functional studies based on patch-clamp electrophysiology provide additional information on the active state of GlyR α1. Current-voltage measurements from single 493 in outside-out patches at symmetric 145-mM chloride concentration yielded a unitary conductance of 86 pS for the main open state and
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br Regulation of Glu transporters
2022-05-21
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino sodium salt calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcri
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