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The inhibitory activities of the
2021-11-26

The inhibitory activities of the compounds with the modification of the amino group against human liver FBPase are summarized in . Replacement of the amino group of with hydrophobic substituent such as a methyl group () led to a substantial loss of activity (IC=995nM). Similarly, replacement with h
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EZH can also interact with Ten Eleven Translocation
2021-11-26

EZH2 can also interact with Ten-Eleven Translocation gene family members (TET1, TET2, and TET3), which convert 5-methylcytosine (5 mC) to 5-hydroxymethylcytosine (5hmC), to cause changes in patterns of histone methylation and DNA methylation [52]. Huang et al. found that the expression levels of all
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The importance of the histone chaperone function of
2021-11-26

The importance of the histone chaperone function of Hat1p was highlighted by the recent demonstration that the catalytic activity of Hat1p is not sufficient for its function in vivo. Fusion of a nuclear export signal (NES) to yeast Hat1p effectively excluded the enzyme from the nucleus, with a conco
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Another property shared between Hat p and Rtt
2021-11-26

Another property shared between Hat1p and Rtt109p is a transient or substoichiometric interaction with Asf1p. Asf1p is necessary for the acetylation of histone H3 lysine 56 by Rtt109p. However, they do not appear to form a stable complex [22], [24], [27], [84], [90]. Surprisingly, the original type
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Based on the aforementioned findings
2021-11-26

Based on the aforementioned findings, variations of the imidazole heterocycle present in the endogenous ligand histamine (1) led to 2-(thiazol-2-yl)ethanamine (2-TEA, 2) and later to 2-(3-bromophenyl)histamine or 2-(3-(trifluoromethyl)phenyl)histamine (3) (Fig. 3). Interestingly, 2-TEA demonstrated
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Sequences of HKI and HKII from
2021-11-26

Sequences of HKI and HKII from humans were compared to those of the Atlantic salmon to better understand the observation of HKI movement to the mitochondrial fraction in this study, as HKI in mammals is commonly assumed to be mostly passively regulated by product inhibition, with little evidence of
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568 br Modulators of the GUCY C cGMP PDEs signaling
2021-11-26

Modulators of the GUCY2C/cGMP/PDEs signaling pathways for CRC prevention and therapy (pre-clinical and clinical development) Several modulators of the GUCY2C/cGMP/PDEs signaling pathways, including GUCY2C agonists and PDEs inhibitors, have been developed and explored as chemopreventive agents for
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Biotin-tyramide The GSTP promoter region in
2021-11-26

The GSTP1 promoter region in PCA cells without or with reduced GSTP1 mRNA expression had a different histone modification pattern than BPH-1 cells with GSTP1 mRNA expression: the repressive histone modifications H3K9me3/H3K27me2 were distinctly increased and H3K27me3/H3K9me2 were slightly decreased
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The GPR gene was included in our survey because
2021-11-26

The GPR35 gene was included in our survey because of its location immediately 3′ to CAPN10 and because it showed evidence of association with type 2 diabetes. Also, its expression in tissues including pancreatic islets and skeletal muscle is consistent with a possible role in type 2 diabetes. Our re
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Modulation of the cannabinoid system has been
2021-11-26

Modulation of the cannabinoid system has been reported to exert anti-parkinsonian properties through different mechanisms. On one hand, cannabinoids have neuroprotective properties in different rodent models of PD, both through a CB1/CB2 receptor-independent mechanism (Lastres-Becker et al., 2005) a
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GPR A a G protein coupled receptor located mainly
2021-11-26

GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic Norfloxacin hydrochloride [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads
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In our study we evaluated adenovirus
2021-11-25

In our study we evaluated adenovirus type 5 (Ad5) as a vehicle for delivering Cre recombinase in conditional transgenic mouse based on the Cre-loxP system, in order to achieve GlyT1 gene modulation in a specific thalamic region in the adult animal. GlyT1 is a sodium- and chloride-coupled glycine tra
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br Materials and methods br Results br Discussion Ajuba
2021-11-25

Materials and methods Results Discussion Ajuba was originally identified as an adaptor protein which communicates cell adhesive events with nuclear responses to remodel the epithelium (Langer et al., 2008; Marie et al., 2003). Recently, increasing evidence has shown that Ajuba functions as
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unlikely Moreover the ubiquitous expression of the OTR and G
2021-11-25

Moreover, the ubiquitous unlikely of the OTR and GHSR was also observed in hippocampal and hypothalamic primary culture, indicating that this expression pattern is likely due to basal activity of these receptors. GPCR trafficking under control conditions has been linked to biased signalling associa
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Most of the above mechanisms
2021-11-25

Most of the above mechanisms are implicated in attenuation of myocardial I/R injury. However, the role of GalR2 receptor activation in cardioprotection remains unclear because of the lack of receptor subtype selectivity of peptides G2 and G3. It has been shown that Ala5-galanin (2–11) (G4) has a hig
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