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br Conclusion The role of DNA PK target in DNA
2019-08-23
Conclusion The role of DNA-PK target in DNA DSB repair renders this Kifunensine kinase of great medicinal interest in cancer chemotherapy especially the cancer types of linked to DNA defects. Due to the absence of 3D DNA-PK target structure, different ligand-based methods were applied for design
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br DDR receptor and MMP expression Type II collagen
2019-08-23
DDR2 receptor and MMP-13 expression Type II collagen protein in articular cartilage is highly stable structure as its half-life is 117 years [43]. The chondrocytes have limited ability to synthesis type II collagen protein in the matrix of mature articular cartilage once the collagen gets disrupt
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Because flavonoids are widely considered to contribute to
2019-08-23
Because flavonoids are widely considered to contribute to health benefits in humans, including anti-inflammatory, antibacterial, antiviral, anticancer, antiplatelet properties, and free radical scavenging capacity (Xiao et al., 2011), efforts have frequently been made to increase their bioavailabili
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With a favorable spectrum of
2019-08-23
With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i
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Mass spectrometry has previously been used
2019-08-23
Mass spectrometry has previously been used to examine the presence of Hyp in recombinant collagen, using hydrolysates to identify the individual imino acid, equivalent to an amino Z-LEHD-FMK analysis [33], and also by analysis of mass changes to tryptic peptides [34]. The present study, however, ha
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br Conflict of interest br Acknowledgements This work
2019-08-23
Conflict of interest Acknowledgements This work was partially supported by University of Cagliari. Introduction Organophosphorous pesticides (OPs) are wildly used in the world due to high efficiency, broad spectrum and low residue, which in turn results in environmental pollution and adver
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Sampling sediments is usually performed with
2019-08-23
Sampling sediments is usually performed with grab corers [16], [29]. The digested sludge analyzed by Ternes et al. [16] was taken directly from the digester and the activated sludge was obtained by BAMB-4 of the slurry of STPs [16]. Collected samples are transported under cooled conditions (+4 or −
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MoAbs targeting the tumourigenic pathways such as IGF R
2019-08-23
MoAbs targeting the tumourigenic pathways, such as IGF-1R may theoretically have a dual working mechanism. On the one hand they block pathways having an anti-tumour working mechanism, and on the other hand they may also stimulate an immunological response inducing a reaction of the patients own immu
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Binding affinity was measured by a scintillation proximity b
2019-08-23
Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six
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On the other hand although the cardiovascular effects
2019-08-23
On the other hand, although the cardiovascular effects of Epac have been investigated more intensely in recent years [31], there are hardly any studies that suggest or discard a participation of Epac in endothelium-dependent cAMP-induced relaxation. Only our previous results in rat 5-Formyl-CTP manu
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Further modifications on the position of compound led
2019-08-23
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po
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It has been reported that cAMP also acts via
2019-08-23
It has been reported that cAMP also acts via Epac and Epac to attenuate CREB. However, in human monocytes ONO-AE1-329 (the EP4 receptor agonist used in this study) worked entirely through the cAMP-PKA pathway and not vis Epac [12]. Our data suggests that the cAMP-PKA-CREB pathway predominates for MU
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br EBV BILF A Virus Encoded TM Receptor with Immune
2019-08-22
EBV-BILF1—A Virus-Encoded 7TM Receptor with Immune Evasive Functions The EBV-encoded BILF1 receptor (EBV-BILF1) is thought to be implicated in the immune evasion strategy of EBV.56, 61, 62 This orphan 7TM receptor is expressed at significant levels during the early lytic phase of the virus infect
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The potential off target activity
2019-08-22
The potential off-target activity of against other ATP-dependent enzymes, such as kinases, was also investigated. Encouragingly, there was no significant inhibition of ATP binding to 97 human kinases, when was evaluated at 10μM within a DiscoveRx scanEDGE® kinome screen (, ). All together, these d
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The mesolimbic dopamine system is believed
2019-08-22
The mesolimbic dopamine system is believed to be highly important for evaluating environmental stimuli in order to generate an adaptive behavioral response. Thus, not surprisingly these functions appear to have been highly conserved across the vertebrate subphylum. Even though teleost fish lack midb
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