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Endothelins ETs are peptides expressed in both the periphera
2021-08-30
Endothelins (ETs) are peptides expressed in both the peripheral and the central nervous systems, which can contribute to sensory changes seen in animal models of inflammatory, cancer and neuropathic pain [10], [11]. All three mammalian isoforms (ET-1, ET-2 and ET-3) activate specific G protein-coupl
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br ILCs anticipate neuronal derived
2021-08-30
ILCs anticipate neuronal-derived factors Recent studies have revealed that ILCs express receptors for neural peptides, thus enabling cross-talk with the peripheral nervous system. ILC3s express RET (Figure 2), which is a receptor for members of the glial cell-derived neurotrophic factor family of
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Gliptins have become a part of
2021-08-30
Gliptins have become a part of various therapeutic regimens to treat type 2 diabetics in recent decades. Gliptins were developed to lower the blood glucose in type 2 diabetes patients and have been shown to be effective [4,5]. More than a dozen gliptins have been developed for the treatment of T2DM,
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ABH expression is elevated in prostate carcinomas
2021-08-30
ABH3 expression is elevated in prostate carcinomas and has been referred to as prostate cancer antigen-1 or PCA-1. ABH3/PCA-1 was proposed as a diagnostic marker for prostate cancers, and suggested as a possible therapeutic target [82]. However, the recent studies of ABH2 and ABH3-null mice indicate
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α-Naphthoflavone Our data indicate that the ability
2021-08-28
Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa
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In the PTEN loss mouse model deletion of ATG gene
2021-08-28
In the PTEN loss mouse model, deletion of ATG7 gene not only caused an autophagy-deficient phenotype, but also postponed the progression of inoculated prostate tumor [22]. On the basis of these experimental facts, these ATG7 and PTEN related genes were then compared with the 3020 BCR-associated gene
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The most important finding in
2021-08-28
The most important finding in the present study is that the EKR1/2-Egr-1 signaling pathway might be involve in the mechanisms underlying CysLT2 receptor-mediated IL-8 production. The signaling profile can be described by the following sequential processes: the agonists (LTC4 and LTD4) activates CysL
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As previously reported azole class
2021-08-28
As previously reported, azole class antifungal drugs inhibit fungal CYP450 14α-demethylase, as this interrupts the conversion of lanosterol to ergosterol, a component of the fungal cell membrane (Hof, 2006). Furthermore, correlation between fluconazole dose, the extent of hepatic hypertrophy, the le
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Free Fatty Acid Quantification Colorimetric/Fluorometric Kit
2021-08-28
Findings from the present study indicate that CRF1 receptors are especially important in fear acquisition. CP154,526 given before acquisition training, at least partly, reinstated the fear-potentiated startle response and blocked the development of contextual conditioned fear in SERT−/− rats. CP154,
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The present study has shown that additional protein
2021-08-28
The present study has shown that additional protein stability can be achieved (Fig. 6). The 0.6 to 1.0 °C increases that were observed were not large compared, for example, to the ∼5 °C increase that has been reported using sequence modifications [22]. This may reflect that the Hyp enters both the X
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br Method Detailed study protocol was reported previously
2021-08-28
Method Detailed study protocol was reported previously. The ULTIMATE- HFrEF trial was approved by the Institutional Review Board of our hospital, and the study drug, udenafil, was approved as Investigational New Drug for treatment in patients with chronic HFrEF by Ministry of Food and Drug Safety
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Although we observed increases in AR
2021-08-28
Although we observed increases in α1-AR mediated cAMP production separately in the nucleus and cytoplasm, compartment specificity was observed for PKA activation. GPCRs and their effector proteins are commonly found in multiprotein signalosomes with A-kinase anchoring proteins (AKAPs) serving as sca
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At one time the biological effects
2021-08-28
At one time, the biological effects of cAMP were thought to be mediated exclusively by Protein Kinase A (PKA). Consistent with this, PKA inhibitors have been shown to reverse the effects of cAMP-elevating agents on VSMC proliferation [5]. However, we recently reported that cAMP-mediated inhibition o
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Conventional assays rely on a comparable transformation
2021-08-28
Conventional assays rely on a comparable transformation of the target analytes and the structurally similar (but not identical) proxy substrates and are commonly used to measure individual enzyme activities in (pre-treated) intact sludge flocs (Burgess and Pletschke, 2008a, Gessesse et al., 2003, Yu
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TBB The development of novel approaches to study GPCR
2021-08-28
The development of novel approaches to study GPCR-mediated transactivation in live TBB is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment of Grb2 to R
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