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To further investigate if GPR was
2021-10-25

To further investigate if GPR40 was the functional target of these phenylpropiolic SRT2104 analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK293-GPR40 c
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br Materials and methods br Results br Discussion To
2021-10-25

Materials and methods Results Discussion To the best of our knowledge, the current study presented the first evidence that GPR40, also named FFAR1, played an essential role in bone formation and mediated apexbio dilution induced osteogenic effect via Wnt/β-catenin signaling. We found that d
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br Discussion Our results indicate that marked changes
2021-10-25

Discussion Our results indicate that marked changes in the relative distribution of AMPA receptors in microsomal and synaptic fractions occur during the postnatal period, and that these changes are correlated with changes in different populations of AMPA binding sites. At early postnatal ages (PN
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In the present study a significant
2021-10-25

In the present study, a significant increase in liver glut4 mRNA levels as well as an increase in liver glycogen content was observed in the dogfish in response to glucose-loading, although we did not observe any changes in liver glycogen content or glut mRNA levels following insulin administration
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br Acknowledgements This work was supported by a
2021-10-25

Acknowledgements This work was supported by a fellowship to C.H. under the ‘100 Foreign Expert’ scheme of the Shanxi province government(R100456). Conflict of interest: Dr. Holscher is a named inventor on a patent submitted by Lancaster University on the use of dual GLP-1/GIP analogues in neurode
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Herein exploiting several spectroscopic techniques i
2021-10-23

Herein, exploiting several spectroscopic techniques, i.e. CD, UV and NMR, along with gel electrophoresis, size exclusion chromatography and in silico prediction analysis, the conformational behaviour of R1.2 and R1.3 was studied in Na+- and K+-rich solutions, which mimic the extra- and intracellula
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Since we were able to reach low micromolar to
2021-10-23

Since we were able to reach low micromolar to sub-micromolar potency in both compound series (6 and 7), we were also keen on assessing the preliminary ADME profile (particularly with respect to plasma and liver microsomal stability) of the most active compounds from these series. As it is evident fr
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Ion Channel Compound Library The mechanistic basis of a PAE
2021-10-23

The mechanistic basis of a PAE-induced reduction in HDC isoform expression is unclear at present. These reductions may be a consequence of reduced histaminergic innervation of PAE-affected brain regions. Given that these three brain regions are anatomically more distant from the ventral hypothalamus
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Isochlorogenic acid C receptor The zinc dependent HDACs are
2021-10-23

The zinc-dependent HDACs are classified into four groups based on their structure, complex formation, and expression pattern: class I (HDAC1, HDAC2, HDAC3, and HDAC8), class IIa (HDAC4, HDAC5, HDAC7, and HDAC9), class IIb (HDAC6 and HDAC10), and class IV (HDAC11) [16]. We recently reported on a cyto
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Activation of sGC induces the generation of cyclic guanosine
2021-10-23

Activation of sGC induces the generation of cyclic guanosine monophosphate (cGMP), phosphorylation of protein kinase G (PKG) and changes in activity of effector proteins such as phosphodiesterases (PDE), ion channels and ion pumps [43]. This pathway eventually leads to dilation of TNF-alpha, recombi
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CB-5083 GSTP is a class Glutathione S transferase GST
2021-10-23

GSTP1 is a π-class Glutathione S-transferase (GST-π) enzyme involved in tumor suppression by protecting CB-5083 against genomic damage mediated by various oxidants. Although the loss of GSTP1 function by hypermethylation has been reported as a common epigenetic alteration in prostate carcinogenesis
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br Competing interests br Introduction An effective vaccine
2021-10-23

Competing interests Introduction An effective vaccine against the Human immunodeficiency virus (HIV) is still to be created, even though many strategies have already been tried [1]. Antibodies against a vaccine antigen must be either neutralizing or inducing cellular cytotoxicity [1]. It is kn
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Previous studies showed that pregnancy rate improves
2021-10-23

Previous studies showed that pregnancy rate improves when ewes have a BCS that exceeds a minimum threshold [43]. The pregnancy rate is increased in sheep with BCS ≥2.5 [44] and >2 [45]. In this work, pregnancy rate was higher in the GnRH group with low BCS compared to the hCG and Control groups. Des
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Glutamate activates cationic glutamate gated channels i e io
2021-10-23

Glutamate activates cationic glutamate-gated channels (i.e. ionotropic glutamate receptors) that mediate the fast excitatory actions of glutamate. It also activate G protein-coupled receptors, named metabotropic glutamate receptors (mGluRs) (Pin and Bettler, 2016). The eight subtypes of mGluRs are k
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A great number of proteins entering the nucleus possess
2021-10-22

A great number of proteins entering the nucleus possess a characteristic nuclear localization sequence (NLS) in their primary structure. One of such sequences is the KKKGK motif [30]. It is present in all known muscle (but not liver – except human liver) FBPase sequences (human, rabbit, rat and mous
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