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br Funding br Conflict of interest statement br References a
2021-11-19
Funding Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements Introduction Recent papers have shown that Interferon-free hepatitis C virus (HCV) therapies with
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Receptor guanylyl cyclases play essential roles
2021-11-19
Receptor guanylyl cyclases play essential roles in cardiovascular and gastrointestinal (patho-)physiology, reproduction biology, cell proliferation, bone growth and sensory signal transduction and, therefore, are important pharmacological targets. Accordingly, the receptor guanylyl cyclase agonists
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The CNP pGC B cGMP pathway
2021-11-19
The CNP/pGC-B/cGMP pathway has been reported to be potent inhibitor of fibrosis, from an intrinsic compensatory protective response as well as a therapeutic in cardiorenal injury and disease states [6,12,13,22,30]. Indeed, fibrosis is a progressive process leading to increased risk for morbidity and
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Our observations with RBC in human platelets suggested a mor
2021-11-19
Our observations with RBC8 in human platelets suggested a more wide-ranging role for Rals in platelet function compared to our observations in Ral deficient mouse platelets. Using lumi-aggregometry, 10 μM RBC8 significantly reduced platelet aggregation and ATP secretion responses in both WT and DKO
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An interesting question is why RhoF has such
2021-11-19
An interesting question is why RhoF has such the slow rate of GDP dissociation. The amino herpes simplex virus type 1 mutations in a presumable GDP-binding site of RhoF had only moderate effects on the GDP dissociation (Fig. 3C), which suggests a mechanism involving the global amino acid sequence of
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br Introduction The Ras superfamily of small
2021-11-19
Introduction The Ras superfamily of small GTPases is composed of more than 150 protein members involved in a wide variety of biological processes, such as proliferation, differentiation, cytoskeletal organization, and protein trafficking [1]. The Ras superfamily proteins act as molecular switches
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Various inhibitors have been developed to target molecules
2021-11-19
Various inhibitors have been developed to target molecules present in these pathways. They include both man-made monoclonal γ-Linolenic Acid methyl ester as well as small molecule membrane permeable inhibitors that often target kinases or phosphatases [5], [338], [348], [364]. In summary, these pat
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br Results and discussion br Conclusions In summary we gener
2021-11-19
Results and discussion Conclusions In summary, we generated analogues of the hit compounds 1–3, studied their structure–activity relationships, and created a series of highly potent GPR55 agonists. The most potent agonists among the series were 17a-b, 17e, 17g and 17l with EC50 values below 10
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XMD17-109 Notably Cu labeled dimeric exendin subunit which w
2021-11-19
Notably, 64Cu-labeled dimeric exendin-4 subunit, which was designated as 64Cu-Mal2Sar-(exendin-4)2, showed higher tumor uptake than that of the monomeric exendin-4 subunit [245]. Besides the most commonly-used GLP-1R agonists exendin-3 and -4 and their derivatives, exendin (9-39) exhibits strong bin
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Similar to GPR A activation of G protein
2021-11-19
Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic Annexin V-Cy3 Apoptosis Kit Plus synthesis receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et
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The Berlin patient is a unique
2021-11-19
The Berlin patient is a unique case and dependent on the histocompatibility-matched CCR5Δ32/Δ32 homozygous donors. These donors occur at a little higher rate in the European Caucasian population, but they are very rare in Asians and Africans.15, 16, 17 The recently developed genome-editing technolog
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GSK3787 IBs had a clear vesicular ultrastructure suggesting
2021-11-19
IBs had a clear vesicular ultrastructure, suggesting that a large part of the iron-containing mitochondrial remnants might be cleared via normal autophagy processes during final reticulocyte maturation [21]. IB formation was followed by characteristic changes in RBC morphology, with irregularly shap
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Hesperidin is an abundant and inexpensive plant flavonoid
2021-11-19
Hesperidin is an abundant and inexpensive plant flavonoid, largely derived from citrus species including sweet orange and lemon. Hesperetin (Hst) is the aglycone of hesperidin. Hesperidin and hesperetin have been reported to show a battery of pharmacological properties, including anti-hyperlipidemic
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The inhibition of NSAIDs towards
2021-11-19
The inhibition of NSAIDs towards GLOI provides a direction for the development of novel effective GLOI inhibitors. Although the inhibitory activity of indomethacin was determined and the interactions between it Nicotinamide and GLOI were probed by NMR titration experiments, no detailed inhibitory m
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Hippocampal lesioned mice were less able to withhold respond
2021-11-18
Hippocampal-lesioned mice were less able to withhold responding during a DRL-10 requirement (i.e. when the animals had to wait 10s between lever presses), and were thus less efficient than sham operated controls. In contrast, GluR-A−/− mice did not differ from wild-type mice when the DRL requirement
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