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br Materials and methods br
2021-10-20
Materials and methods Results Discussion Myocardium reperfusion injury contributes almost half of myocardial infarct size in myocardial infarction patients, and infarct size is closely correlated with the probability of developing Yeast Extract failure [1]. Despite this knowledge, myocardia
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While phosphorylation site motifs are
2021-10-20
While btk inhibitor site motifs are typically described in terms of residues that promote phosphorylation, negatively selected residues can also be an important component of substrate recognition. Such ‘forbidden’ resides can act as a filter to prevent phosphorylation of a site by the ‘wrong’ kinas
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sgk inhibitor Activity of compound in rat brain tissue highl
2021-10-20
Activity of compound 10 in rat sgk inhibitor tissue highlights the potential to use this new class of allosteric sGC inhibitors to study the role of the NO—sGC—cGMP signalling pathway in the brain. Reducing amounts of cGMP in cells would have implications in downstream signalling proteins, such as
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We tested this hypothesis with
2021-10-20
We tested this hypothesis with two experiments. In the first experiment OVX monkeys implanted with an E2 Fmoc-L-Arg(Aloc)2-OH receptor (this results in LH levels similar to the level during the follicular phase) were treated with daily injections of letrozole for 1 week and then EB was injected sys
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To directly address whether pharmacological attenuation of p
2021-10-19
To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N
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On the contrary the benzhydrol series showed modest activity
2021-10-19
On the contrary, the benzhydrol series showed modest activity with EC of two digit micromole. The bulkiness of the CGP 57380 sale tail may be the reason for the low activity. Interestingly, introduction of H-bonding groups, such as OMe in and CF in , slightly improved the activity compared to the
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The first suggestion that the
2021-10-19
The first suggestion that the Hh pathway might be involved in the pathogenesis of chronic liver disease was reported at the beginning of this millennium by Shackel et al. who noted that Patch and Gli were upregulated in their microarray analysis of liver tissues from patients with primary biliary ch
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KT182 br Introduction Topological hedgehogs keep generating
2021-10-19
Introduction Topological hedgehogs keep generating interest in point-set topology as they are a rich source of counterexamples and applications (for a comprehensive survey on topological hedgehogs we refer to [1]; see also [9]). They may be described as a set of spines identified at a single poin
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br Materials and methods br Results
2021-10-19
Materials and methods Results Discussion Recently, we characterized the interaction of the PH domains of various Lbc family RhoGEFs with the activated small GTPase, RhoA, and demonstrated that this could serve as a positive feedback mechanism for robust activation of RhoA (Medina et al., 20
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Lactate as administered in these
2021-10-19
Lactate as administered in these models is metabolized rapidly and it appears that transient engagement of GPR81 with lactate serum concentrations in the range of moderate exercise physiology, as measured here at 3–4 mmol/L, are sufficient to suppress tissue macrophage NF-κB activation in our models
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CD binding to gp causes a
2021-10-19
CD4 binding to gp120 causes a large scale conformational change of gp120 which involves the gp120 core structure and the transitions of inner-domain layers (layer 1, 2 and 3), but also involves the movement of the major loops (V1, V2 and V3) [16], [17], [18], [19]. For instance, the V2-loop joins th
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br Acknowledgements br Introduction Obesity
2021-10-19
Acknowledgements Introduction Obesity is a growing pandemic, which becomes a global public health problem. The evidence has been readily available and mounting, demonstrating that obesity increases incidences of chronic comorbidities, such as non-alcoholic fatty liver diseases, diabetes, cardi
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The role of GJs in
2021-10-18
The role of GJs in liver fibrogenesis was studied recently. Studies showed a significant decrease in liver fibrosis in Cx32 knockout mice compared to wild-type mice. Although the mechanism underlying this protective effect of Cx32 deletion is not clear, reduced oxidative stress was suggested as a po
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br Materials and methods br Results br Discussion
2021-10-18
Materials and methods Results Discussion The roles of EZH2 during oocyte maturation, early embryogenesis, and somatic cell nucleus transfer (SCNT) have been studied extensively in mouse [12,30]. How it functions during porcine preimplantation development, especially the maternal effect, how
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For further understanding of the interaction
2021-10-18
For further understanding of the interaction between these inhibitors and proteins (BRafV600E and HDAC1) for guiding the SAR, compound 10e, the most potent compound of this series, was chosen as a representative for docking into the BRafV600E (PDB code: 1UWJ) and HDAC1 (PDB code: 1C3R), revealing ex
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