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br Modulators of the GUCY C cGMP
2022-08-22

Modulators of the GUCY2C/cGMP/PDEs signaling pathways for CRC prevention and therapy (pre-clinical and clinical development) Several modulators of the GUCY2C/cGMP/PDEs signaling pathways, including GUCY2C agonists and PDEs inhibitors, have been developed and explored as chemopreventive agents for
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Previous reports have implicated the guanylin GC C
2022-08-22

Previous reports have implicated the guanylin/GC-C signalling system as being important in osmoregulation in fish, especially in euryhaline species such as the eel which migrate between freshwater (FW) and seawater (SW) environments at different stages of their life cycle (Comrie et al., 2001a, Comr
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INO-1001 br Materials and methods br Results Our data indica
2022-08-22

Materials and methods Results Our data indicated that 1,8-cineol leads to a noticeable but not significant (p = 0.07) 45% decreased phosphorylation of GSK-3α/β at Ser-9/21. Phosphorylation of GSK-3α/β at Tyr-279/216 was not affected (Fig. 1A/B). To ensure, that the decreased phosphorylation of
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R R MNF is a unique bitopic
2022-08-22

(R,R′)-MNF is a unique bitopic agent with selective and potent β2AR agonistic and GPR55 inhibitory properties [10], [11] that are independently associated with the drug's anti-mitotic and anti-tumorigenic actions. In 1321N1, U118MG, and melanoma cell lines, (R,R′)-MNF activation of the β2AR decrease
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br Conclusions br Introduction G protein coupled
2022-08-22

Conclusions Introduction G protein-coupled receptors (GPRs) share common structural motifs, including seven transmembrane helices, and the ability to activate heterotrimeric G proteins such as Gs, Gi, Gq and G12/13. A variety of GPR cellular functions are mediated by second messengers such as
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GK also called hexokinase IV or D is a
2022-08-22

GK, also called hexokinase IV or D, is a glycolytic enzyme that converts G-1 to glucose-6-phosphate. GK has unique characteristics compared with those of the ubiquitously expressed hexokinase isoforms I–III, and is predominantly expressed in the pancreas and liver. In pancreatic β-cells, GK regulat
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br SMO antagonists pitfalls and limitations The first
2022-08-22

SMO antagonists: pitfalls and limitations The first Hh inhibitor discovered was cyclopamine, a naturally occurring alkaloid isolated from Veratrum californicum[21], which inactivates SMO by directly binding to its hepathelical bundle. Nevertheless, cyclopamine has shown several limitations as a d
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br Acknowledgements Funding for this study
2022-08-19

Acknowledgements Funding for this study is gratefully acknowledged from the Department of Employment and Learning (QC) and the Northern Ireland Chest Heart and Stroke Association (2008107). Introduction Preeclampsia is a major human pregnancy-specific disorder that occurs in at least 5–10% o
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Several other assay parameters were also explored First
2022-08-19

Several other assay parameters were also explored. First, the thermal dependence of the assay was investigated by measuring the specific activity at different temperatures (Fig. 7). That data show that enzymatic activity increases with increasing temperature. Interestingly, the observed rate increas
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Aberrant activity of PRC as a result of over
2022-08-19

Aberrant activity of PRC2 as a result of over expressed EZH2, has been frequently seen in a wide range of human cancers including breast and prostate tumors [10]. However, leukemia-associated epigenetic aberrations are not fully understood [7]. Herein, we will overview the current knowledge of epige
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The exact mechanism by which mitochondrial hexokinases such
2022-08-19

The exact mechanism by which mitochondrial hexokinases such as HK1 and HK2 prevent apoptosis is unclear. Mitochondrial hexokinases have been shown to bind with the voltage-dependent anion channel 1 (VDAC1), giving them direct access to ATP for use as an energy source [36]. Akt has been shown to prom
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The primary physiological role of the HO system is the
2022-08-19

The primary physiological role of the HO system is the protection of SID 26681509 from oxidative stress. These cytoprotective effects are attributable both to the degradation of the pro-oxidant heme and to the positive contribution of the metabolites produced during this degradation, namely CO, BV,
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CW069 Starting from the hypothesis that the linker portion
2022-08-19

Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [
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Piperlongumine br Acknowledgements This work was
2022-08-19

Acknowledgements This work was financially supported by the National Natural Science Foundation of China (Grant No. 81803033) and the “Double First-Class” University project (CPU2018GF02). Introduction Atrial fibrillation (AF) is the most common progressive cardiac rhythm disorder. Studies ha
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HBV VL quantitation has been shown
2022-08-19

HBV VL quantitation has been shown to be affected by genotype/subtype, and varying degrees of positive and negative bias has been seen in previous comparison studies when analyzing across HBV genotypes. In studies comparing RealTime and Cobas for example, negative bias of ∼0.25 log10 was seen for ge
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