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Several highly potent CysLT receptor antagonists with
2021-03-31
Several highly potent CysLT1 receptor antagonists with large structural Dantrolene, sodium salt have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles
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In humans CYP A major isoforms of CYP
2021-03-31
In humans, CYP3A4/5, major isoforms of CYP3As in the liver, have variants that reduce the enzyme activities [33], [34]. In addition, Werk et al. recently reported the first case of a complete failure of CYP3A enzyme activity due to homozygous loss-of-function mutation of CYP3A4 combined with nonfunc
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Our results show that COX and COX inhibition improve cogniti
2021-03-31
Our results show that COX-1 and COX-2 inhibition improve cognitive performance and decrease the neuronal insult during HH. However, when a neuroinflammatory response was observed, COX-1 inhibition was more effective than COX-2 inhibition at reducing microglial activation and augmenting pro-inflammat
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Instead of introducing extra hardware or
2021-03-31
Instead of introducing extra hardware or hardware modification, software-based CFC techniques just insert extra checking instructions into the source code of the target program at compile time so as to have the target program do checking jobs itself. Preeminent software-based CFC techniques proposed
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Due to the results of the
2021-03-31
Due to the results of the experiment we decided to deploy our cloud service infrastructure with two platform-independent servers instead of one or three. This decision was based on two factors: (a) the use of more than one server is useful to avoid a bottleneck in the system, and (b) using more than
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A comparison between tinnitus and controls
2021-03-31
A comparison between tinnitus and controls subjects showed increased activity in the left AUD and PHC for the gamma frequency band. The link between gamma band activity in the AUD and tinnitus has been identified using both EEG (van der Loo et al., 2009) and MEG (Weisz et al., 2005, 2007). This is s
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The two SNPs rs rs presented
2021-03-31
The two SNPs rs4818-rs4680 presented above are part of the haploblock (rs6269, rs4633, rs4818, rs4680) presenting the 3 major haplotypes which influence the enzymatic activity of COMT. This activity is inversely related to the sensitivity of pain in a chronic pain syndrome; so the haplotype (GCGG) h
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MK 571 Introduction Prolyl hydroxylation is a widely observe
2021-03-31
Introduction Prolyl hydroxylation is a widely observed post translational modification in collagen, an abundant animal protein. The high content (~13% per chain of the triple helical structure) of 4-hydroxyproline (Hyp,O) in collagen, togather with the natural abundance of collagen has led to the e
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br Acknowledgements br Introduction In Arabidopsis thaliana
2021-03-31
Acknowledgements Introduction In Arabidopsis thaliana (L.) Heynh, there are at least four copies of the caseine kinase-like gene Ck1, which is involved in peptide phosphorylation in mammals [1]. These genes are distributed on POM 1 1, 2, 4, and 5. A similar number of copies for Ck1 have been
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br Agonist binding ETA activation is promoted by binding
2021-03-31
Agonist binding ETA activation is promoted by binding of the endogenous peptidergic agonists to their orthosteric binding site on the receptor. ET1 and ET2 (Trp6-Leu7-ET1) bind with equal high affinity to ETA, whereas the third endogenous isopeptide ET3 (Thr2-Phe4-Thr5-Tyr6-Lys7-Tyr14-ET1) binds
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br Discussion EFTs are sarcomas with almost
2021-03-31
Discussion EFTs are sarcomas with almost undifferentiated histologic features, consequently their differentiation from other small, blue, round cell tumors may be difficult. Substantial intracellular puromycin selection concentration on PAS stain is a useful diagnostic feature. The addition of CD
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br Roles of ERR in Physiology and Disease br
2021-03-31
Roles of ERRγ in Physiology and Disease Concluding Remarks and Future Perspectives Over the last decade, the generation of tissue-specific ERRγ transgenic or knockout mice and the use of synthetic ligands have rapidly advanced our understanding of the roles of ERRγ in cellular functions, altho
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br Introduction Vein graft implantation
2021-03-31
Introduction Vein graft implantation into the arterial environment for surgical bypass is the gold standard to treat severe cardiovascular occlusive disease. After placement of a vein into the higher pressure, flow, and oxygen tension of the arterial circulation, the vein adapts to the arterial e
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EC barrier dysfunction triggered by inflammatory mediators i
2021-03-31
EC barrier dysfunction triggered by inflammatory mediators involves more than one mechanism, explaining the partial attenuation of EC barrier compromise obtained with PKA and Epac activators. PKA-dependent phosphorylation of vasodilator-stimulated phosphoprotein (VASP) has been shown to make a posit
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To study systemic potential of the selected
2021-03-31
To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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