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The Ala to Leu substitution would reduce
2022-01-26

The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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It is well established that transcription factors are the ma
2022-01-26

It is well established that transcription factors are the major key players in regulating the transcriptional state of the targeted gene. 15 TFs were found in the present study, which were predicted to have the binding affinity with the EZH2 promoter region. Out of these, GCF, AP-2 and Sp1 were most
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One year after the Brose
2022-01-26

One year after the Brose . paper was published, Littleton . reported the first measurements of evoked synaptic transmission in syt1 nulls, using the neuromuscular junction as a model system. These experiments revealed that syt1 was essential for rapid, robust evoked neurotransmitter release. Similar
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Regulation of gene expression in mammalian cells is governed
2022-01-26

Regulation of gene expression in mammalian cells is governed by the epigenetic machinery, which includes several distinctive yet entangled branches. DNA and histone modifying enzymes, non-coding regulatory RNAs, and ATPase-dependent chromatin remodeling proteins all contribute to the dynamic alterat
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It is important to mention that the IC
2022-01-26

It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co
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Recently an increasing number of
2022-01-26

Recently, an increasing number of studies have highlighted the crucial role of nociceptive factors produced by microglia under neuropathic pain conditions (Mika et al., 2013; Popiolek-Barczyk and Mika, 2016). iNOS is an important pronociceptive factor that is strictly expressed by microglia/macropha
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In addition researchers studying GPR agonists favor the
2022-01-26

In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it hyPerFUsion™ high-fidelity DNA polymerase is unclear why Sanofi-Aventis chose to termina
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br Ghrelin and energy balance To characterize the
2022-01-25

Ghrelin and Memantine hydrochloride mg balance To characterize the physiological role of ghrelin in energy homeostasis, ghsr−/− and ghrelin−/− mice were generated [33], [36], [41], [47]. Although ghrelin regulates the amplitude of episodic GH release, ghsr−/− mice were not dwarfs, and in fact ap
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FXR agonists represent an attractive class of drugs
2022-01-25

FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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Regarding IAV types of hemagglutinin
2022-01-25

Regarding IAV, 18 types of hemagglutinin and 11 types of neuraminidase were described and none of the commercialized antiviral drugs are susceptible to protect against all strains that will emerge from the animal reservoir (Webby and Webster, 2003). The strong dependencies of influenza viruses on we
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In this study we evaluated and compared the kinetics and
2022-01-25

In this study we evaluated and compared the kinetics and duration of the oral and systemic HPV-16 and HPV-18 specific antibody response to three doses of the qHPV vaccine in mid-adult aged HIV+ men from the AIDS Malignancy Cohort (AMC) 052 trial and mid-adult aged HIV− men from the Mid-Adult Male [M
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In conclusion we have demonstrated that the ejection of stru
2022-01-25

In conclusion, we have demonstrated that the ejection of structural zinc ions from G9a and GLP in the presence of selenium-, and sulfur-containing electrophilic small Danazol leads to inhibition of these two biomedically important epigenetic enzymes. Our work demonstrates that clinically used ebsel
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Histone demethylases are involved in the transcriptional out
2022-01-25

Histone demethylases are involved in the transcriptional output of the AR and hypoxia signaling pathways, and thus contribute to prostate cancer development [12]. For example, the histone demethylase KDM3A serves as a transcriptional coactivator of HIF1α and AR in regulation of their target genes [1
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br Conclusions H K demethylases perform an important
2022-01-25

Conclusions H3K27 demethylases perform an important catalytic function in mediating change in gene expression, whether it is during cell differentiation or activation, because they remove repressive marks from histones which opens the chromatin and facilitates transcription. The number of publica
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br Introduction Sister chromatid cohesion is established dur
2022-01-25

Introduction Sister-chromatid cohesion is established during DNA replication by a ring-shaped cohesin complex consisting of the core subunits Smc1, Smc3, Scc1, and SA1 or SA2, which recruit regulatory subunits Pds5 (Pds5A/B in vertebrates), Wapl, and Sororin to regulate the association of cohesin
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