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PD0325901 As described above we designed and synthesized a n
2021-01-22
As described above, we designed and synthesized a new 1,4-di-substituted isoquinoline lead compound, and was identified as a ligand with moderate potency for the CRTH2 receptor. We initially we examined the effects of the steric factor of R group on the CRTH2 binding potency (). When the methyl gro
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Stressful life events are modulators
2021-01-22
Stressful life events are modulators of mood and can trigger a variety of destructive behavior, including drug abuse and relapse in addicts (Association, 2013; Chen et al., 2012; Sinha, 2009). Likewise, drug-associated stimuli evoke a negative affective state in abstinent drug users. Compelling evid
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In the present study we
2021-01-22
In the present study, we have examined, an alternative approach for introduction of Hyp into bacterial, non-animal collagens. Previously, Gruskin and colleagues [27] had shown that Hyp could be introduced into recombinant mammalian collagen sequences in E. coli through a mechanism of co-translationa
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The first part of the study
2021-01-22
The first part of the study evaluated the accuracy of recomLine IgG and IgG Avidity to date CMV infection: In our study, 83.1% of samples tested matched onset dates compared to 71.9% with VIDAS avidity. Moreover, the number of inconclusive results (intermediate avidity for VIDAS, positive IgG withou
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Another enzyme class that has
2021-01-22
Another enzyme class that has emerged as a potential alternative to P450s are the so-called ‘unspecific peroxygenases’ (UPOs). They also contain a heme but are extracellularly expressed fungal enzymes that are often more stable than P450 monooxygenases. Importantly, UPOs use H2O2 instead of O2 as th
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br Conclusion The past few years have witnessed
2021-01-22
Conclusion The past few years have witnessed substantial progress in understanding the structural mechanisms of substrate recognition and the reactions catalyzed by the O-GlcNAc-cycling enzymes, but more work remains. In particular, future research will be needed to establish how OGT and OGA inte
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Gupta et al have shown that a genetic variant
2021-01-22
Gupta et al have shown that a genetic variant associated with the 5 vascular diseases (coronary artery disease, migraine, carotid artery dissection, fibro-muscular dysplasia, and hypertension) is a distal regulator of the ET-1 gene [30]. They found that a single nucleotide polymorphism (SNP) located
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Materials and methods br Results Assay of botulinum toxin
2021-01-22
Materials and methods Results Assay of botulinum toxin activity is critical for the risk-assessment, diagnosis, and treatment of botulism cases. The frequently encountered active forms of the toxin are; L chain (inside intoxicated neuronal cells), BoNT (in the blood stream of a botulism patient,
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Emphysema is an important component of COPD which is respons
2021-01-22
Emphysema is an important component of COPD, which is responsible for airflow limitation. In the present study, a significant airspace enlargement was observed 21 days after elastase administration. Interestingly, daily administration of olaparib provided greater protection against emphysema as comp
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It is interesting to note that
2021-01-22
It is interesting to note that Eibinger and colleagues [23] recently reported chemotactic movement to 25-OHC in THP1 cells as well as in primary human monocytes. RNA interference suggested that in part this migration was mediated by EBI2. Competing financial interest statement Acknowledgments
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The aniline R group was extensively explored and
2021-01-21
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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As previously reported azole class antifungal drugs
2021-01-21
As previously reported, azole class antifungal drugs inhibit fungal CYP450 14α-demethylase, as this interrupts the conversion of lanosterol to ergosterol, a component of the fungal cell membrane (Hof, 2006). Furthermore, correlation between fluconazole dose, the extent of hepatic hypertrophy, the le
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The sex dimorphic expression of
2021-01-21
The sex-dimorphic MDV 3100 of mouse CYP3A is partially due to sex-dimorphic plasma GH profile which is a decisive factor in the regulation of sexspecific CYP isoforms [14]. Nevertheless, in our study we did not observe any changes in plasma GH levels in either mouse sex with a selective ablation of
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There has recently been some
2021-01-21
There has recently been some interest in Uba6, which is most similar to slime mold, with BLAST identities of 59% and positives 73% in the 400–600 ADD range. The 400–600 ADD correlation of the two profiles is a striking 87%, so functional differences probably arise outside the ADD binding domain. Hu
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From a mechanistic standpoint the BCL RD domain
2021-01-21
From a mechanistic standpoint, the BCL6 RD2 domain represses the GPR183 and S1PR1 loci by recruiting HDAC2, but not MTA3-NuRD, to suppress the enhancer activation mark H3K27ac at their distal regulatory elements. However, these data do not exclude the possibility that other as yet unknown corepresso
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