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The product chain length determination mechanism of prenyltr
2022-06-07
The product chain-length determination mechanism of -prenyltransferases has not yet been elucidated, although mutational analyses of highly conserved residues and of characteristic amino proton pump inhibitor residues in each subfamily of -prenyltransferases have enabled the understanding of the ba
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Contrary to the transient nature of signal
2022-06-07
Contrary to the transient nature of signal transmission through PLCβ, genome-wide RNAi screens revealed that the signaling events driven by Gαq that result in aberrant cell proliferation depends on highly specific protein-protein interactions, rather than solely on diffusible second messenger system
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The site of paracetamol action remains controversial
2022-06-07
The site of paracetamol action remains controversial. Some publications are in favor of a central action (Barrière et al., 2013, Dogrul et al., 2012, Mallet et al., 2010, Pickering et al., 2006), while others report a peripheral action (Dani et al., 2007, Ferreira et al., 1978). FAAH is a ubiquitous
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Thus far it is reported that
2022-06-07
Thus far, it is reported that the histone methyltransferase activity of SUV39H1 is regulated through some posttranslational modifications. For example, deacetylation of SUV39H1 at Lys-266 by SIRT1 deacetylase increases SUV39H1 activity [31], and methylation of SUV39H1 at Lys-105 and Lys-123 by SET7
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br Introduction The coronary vasculature
2022-06-07
Introduction The coronary vasculature is required for supplying oxygenated blood to the cardiac muscle. Proper coronary blood circulation is essential for embryonic and adult cardiac tissue homeostasis. Defects associated with the coronary function leads to myocardial ischemia, infarction, and he
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phosphodiesterase inhibitors Recent studies have also identi
2022-06-07
Recent studies have also identified additional proteins that could act as scaffolds and promote the interaction of core Hippo pathway components. APC, which is best known as a key component of the β-catenin destruction complex, was observed in mammalian phosphodiesterase inhibitors to have an addit
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br Methods br Results br
2022-06-07
Methods Results Discussion TA-TMA is a severe complication for patients after HSCT. The pathogenesis of TA-TMA is unclear. Complement activation and endothelial cell injury may be involved in the pathogenesis of TA-TMA. Our previous investigations had demonstrated that plasma levels of C5b-
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HBV is an enveloped double stranded DNA virus which is
2022-06-07
HBV is an enveloped, double-stranded DNA virus, which is transcripted into four major transcripts [6]. Among them, the 3.5 kb pregenomic RNA (pgRNA) directs the translation of HBV polymerase, core protein and acts as template for reverse transcription. So viral transcription is a key step of virus l
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The physiological and pharmacological roles of GPR remain la
2022-06-07
The physiological and pharmacological roles of GPR81 remain largely unclear because of several reasons. The low potency of lactate agonizing GPR81 in the millimolar range, together with its fast metabolic turnover, renders as a challenge in in vivo studies using lactate. Furthermore, there are no po
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The GPR receptor is also emerging as an
2022-06-07
The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Also
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Human GPR hGPR was originally isolated in as
2022-06-07
Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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Firstly the impact on activity
2022-06-07
Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)
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With this goal in mind we proceeded
2022-06-07
With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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Thermal analysis of the NQ
2022-06-07
Thermal analysis of the NQ21 peptide was performed with the Solar CM2203 spectrofluorometer. We prepared three 1 μg/mL peptide solutions with different C598-0466 levels (5.0, 7.4, 8.5) in 0.01 M phosphate buffers. Each solution was slowly heated up from 28 °C to 54 °C with a step of 1 °C. Spectra we
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Elevated methylglyoxal levels also contribute to
2022-06-06
Elevated methylglyoxal levels also contribute to carbonyl stress, cytotoxicity, DNA damage, apoptosis and cell death. These mechanisms may be important for normal aging of the nervous system as well as for the development of neurodegenerative diseases such as Alzheimer's and Parkinson's disease wher
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