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Considering the conformational preferences of the SRSRY
2022-05-12
Considering the conformational preferences of the SRSRY sequence in the x-ray structures of soluble uPAR (SuPAR) [18], [19], [20], [50], [51], it is included in a quite flexible linker delimited by Cys76 and Cys95 residues. The SRSRY sequence adopts either α-turned or β-extended conformation. In any
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Several transgenic and knockout congenic mouse
2022-05-12
Several transgenic and knockout/congenic mouse models have been generated in order to assess the role of FFAR1 for proper insulin secretion and maintenance of glucose homeostasis. The results obtained with three different receptor knockout mouse models were not consistent. The protection against hig
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Two recently developed highly specific EZH
2022-05-12
Two recently developed, highly specific EZH2 enzymatic inhibitors, GSK126 and EPZ-6438, are currently in clinical trials for treating lymphomas (Kim and Roberts, 2016). Although these EZH2 inhibitors have shown antitumor effects in lymphoma cells with enzyme-activating mutations of EZH2 (Knutson et
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Recent studies are beginning to explore this complex interpl
2022-05-12
Recent studies are beginning to explore this complex interplay of pathways. For example, intracellular trafficking of poly(lactic-co-glycolic acid)(PLGA) based nanoparticles was studied in detail using 30 different Rab proteins as markers for intracellular transport vesicles (involved in exocytosis,
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All of the designed compounds was synth http www apexbt
2022-05-12
All of the designed compounds – was synthesized from -cyclopropane aldehyde , which was prepared following a procedure we reported previously. Treatment of with 4-chlorobenzene-1,2-diamine in pyridine constructed benzimidazole structure of , which was subjected to deprotection and subsequent oxidat
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In various models histamine has been shown
2022-05-12
In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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br Prostaglandins meet Hippo The prostaglandins
2022-05-12
Prostaglandins meet Hippo The prostaglandins lie at the crossroads between inflammation, regeneration and tumorigenesis (Figure 3). Prostaglandins are synthesized from archidonic hmg-coa reductase inhibitor by Cox1 and Cox2 enzymes [40, 41] and in the gut, prostaglandin E2 (PGE2) protects agains
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Almost all of the series and compounds
2022-05-12
Almost all of the series and compounds exhibited higher activities compared with the compounds in the other series. In these series, the tetrazole group was directly linked to a nitrogen atom of the amide group at the C-28 position, and the C-3 hydroxy group was either unmodified, oxidized, esteri
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Finally worth of mention are
2022-05-12
Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a (-)-p-Bromotetramisole Oxalate library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development o
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In diseased blood vessels increased production of
2022-05-12
In diseased blood vessels, increased production of reactive oxygen species (ROS), such as peroxynitrite, superoxide, and hydrogen peroxide, have been found [[53], [54], [55]]. Peroxynitrite was suggested to alter the redox state of sGC [53] while hydrogen peroxide interfered with the action of NO bu
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It has been indicated that chemicals
2022-05-12
It has been indicated that chemicals-induced mammalian cell death is mediated by GSK-3 activation (by downregulated of GSK-3 phosphorylation) leading to apoptosis (Huang et al., 2014, Li et al., 2014, Tanabe et al., 2011, Yun et al., 2009). In contrast, accumulating evidences have reported that the
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br Acknowledgments This work was supported by the Slovak
2022-05-11
Acknowledgments This work was supported by the Slovak grant agency VEGA, Grant 2/0084/13. We would like to thank Dr. J. Bauer for careful reading of the manuscript. Introduction Glycine is an important neurotransmitter which regulates both microtubule inhibitory neurotransmission and excitat
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cox-2 br Reactive Dicarbonyls and Mitochondrial
2022-05-11
Reactive Dicarbonyls and Mitochondrial Dysfunction Although mitochondrial dysfunction has been suggested to be one of the main pathogenic mechanisms in diabetic neuropathy, little is known about the nature and extent of mitochondrial damage resulting from chronic hyperglycemia. Mitochondria funct
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The unique ability of R PabI to
2022-05-11
The unique ability of R.PabI to specifically excise wst-1 assay receptor from a palindromic sequence is based on a novel structural architecture that is distinct not only from other DNA glycosylases but also from other proteins [88]. In the absence of DNA, R.PabI forms a dimer with a central, highl
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During pain signal transmission glutamate is released
2022-05-11
During pain signal transmission, glutamate is released into the synaptic cleft, which, in turn, causes activation of N-methyl-d-aspartate (NMDA) receptors and hence neurotransmission across the synapse occurs. The synaptic concentration and resultant activity of glutamate are controlled by excitator
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