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EP is the major receptor to mediate PGE
2020-06-10
EP4 is the major receptor to mediate PGE2-induced inflammatory pain. EP4 is upregulated by Isoxsuprine hydrochloride in DRG neurons [16]. Intrathecal injection of the EP4 agonist produced pain responses [25]. Either systemic or local injection of EP4 antagonists relieves inflammatory pain [3], [16],
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br Results br Discussion The ubiquitin system has in recent
2020-06-10
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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MicroRNA miRNA is a class
2020-06-10
MicroRNA (miRNA) is a class of highly conserved, non-coding small molecules containing 19–25 nucleotides. miRNAs are involved in the regulation of genes associated with cancer development and progression and therefore can act as oncogenes, by contributing to tumor formation,17, 18 or as tumor suppre
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As before all calculations are based on thermodynamically
2020-06-10
As before [3], [4], all calculations are based on thermodynamically first- and second-order hydropathic (amino acid) scales [6], [7], linearly scaled to a common center and a common range for each of the 20 amino acids. These are then converted to a triangular matrix , where is the length of a s
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Egr together with catecholamine biosynthetic enzymes
2020-06-10
Egr1, together with catecholamine biosynthetic enzymes, such as tyrosine hydroxylase (TH), dopamine β-hydroxylase (DBH), and phenylethanolamine N-methyltransferase (PNMT), is induced in adrenal medulla by different types of stress (Liu et al., 2005, Morita et al., 1996, Nankova et al., 1993, Papanik
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This study evaluated the role of SERT in classica http
2020-06-10
This study evaluated the role of SERT in classical fear conditioning using a SERT knockout rat model. We found a clear disruption of cue-conditioned fear in SERT−/− rats, as measured with the fear-potentiated startle. This disruption was due to a deficit in fear acquisition and was accompanied by de
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Moreover in this study weak expression
2020-06-09
Moreover, in this study, weak expression of MT1 and MT2 was also detected in the oviduct muscular layers. Although there are no reports regarding the role of MT1 and MT2 in oviduct muscular layers, previous studies have demonstrated that melatonin plays an important role in the uterine contractility
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Geneticin As before all calculations are based on thermodyna
2020-06-09
As before [3], [4], all calculations are based on thermodynamically first- and second-order hydropathic (amino acid) scales [6], [7], linearly scaled to a common center and a common range for each of the 20 amino acids. These are then converted to a triangular matrix , where is the length of a s
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br Are incretins the only mediators of the
2020-06-09
Are incretins the only mediators of the anti-hyperglycaemic effects of DPP-4 inhibitors? Even though both GLP-1 and GIP were identified as substrates for DPP-4 early on [17], [19], [20], [22], and DPP-4 inhibition in vivo raises levels of the intact endogenous forms of both of them [43], [44], fr
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br Materials and methods br Results Artemis
2020-06-09
Materials and methods Results Artemis has been reported to possess 5′–3′ exonuclease activity in vitro on ssDNA, as well as DNA-PK-dependent endonuclease activity on single-strand overhang and hairpin DNA structures [11]. However, enzymes within the metallo-β-lactamase family typically contain
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Since the initial identification of DNA ligase inhibitors by
2020-06-09
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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Regarding eicosanoid production iPLA VIA appears
2020-06-09
Regarding eicosanoid production, iPLA2-VIA appears, in general terms, not to play a major role in mediating this response in innate immunity and inflammation, as evidenced by the large number of studies highlighting the lack of effect of selective inhibition of the enzyme in stimulus-induced AA rele
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The discoidin domain receptors DDR and DDR are receptor tyro
2020-06-09
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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We can think of two ways in which
2020-06-09
We can think of two ways in which collagen binding could activate DDR (Figure 8). A single collagen triple helix could interact with both DS domains in the DDR dimer (“composite binding site”) and thereby activate the receptor, similar to the situation exemplified by the growth hormone-growth hormon
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br Rationale and hypothesis To discover an allosteric inhibi
2020-06-09
Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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