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An intriguing feature of the pre and postsynaptic processes
2019-12-30
An intriguing feature of the pre and postsynaptic processes at the level of the VTA that have been shown to be mediated by CRF2 receptors [9], [34] is that they are exerted only by agonists with high affinity for both CRF2 receptors and CRF-BP. The four endogenous peptides of the CRF system have hig
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Previous studies have demonstrated the role of the
2019-12-30
Previous studies have demonstrated the role of the COMT Val158Met in response to positive and negative emotional stimuli (Bouhuys et al., 1999, Cohn et al., 2009), a fundamental process involved in well-being (Diener et al., 2009a, Diener et al., 1999, Gross and John, 2003). A handful of studies rep
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Sensory gating describes a filter
2019-12-30
‘Sensory gating’ describes a filter mechanism protecting the central nervous system from sensory overload by inhibiting behaviorally irrelevant input (Boutros et al., 2004, 2008). This permits (-)-Huperzine A to a changing contextual environment (Fruhstorfer et al., 1970; Grunwald et al., 2003). Aud
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Two additional hydrogen bonds are formed by the substituted
2019-12-30
Two additional hydrogen-bonds are formed by the -substituted methoxy-group with Ser and Asp. Ser exerts the role of a gate keeper in CK1: Entry of the ATP in the binding-site causes a conformational change into the closed form by Ser, which locks the binding-site and prevents ATP-diffusion out of th
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To investigate the mechanism of action of
2019-12-30
To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due
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br Conclusions In conclusion the
2019-12-30
Conclusions In conclusion, the substrates 18c–18e all produced highly fluorescent colonies with the panel of Gram-negative microorganisms. This has been attributed to the combination of two synergistic effects; the wide distribution of l-alanylaminopeptidase in Gram-negative microorganisms and th
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br Cytochrome P monooxygenases Cytochrome P monooxygenases P
2019-12-30
Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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Plasminogen is composed of five N terminal kringle
2019-12-30
Plasminogen is composed of five N-terminal kringle domains and a C-terminal serine protease domain. The kringle domains have an affinity to lysine and binding of plasminogen with its receptors is dependent on its lysine interacting kringle domains [10], [28]. In the current report, we show that enol
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The potential off target activity of against other ATP depen
2019-12-30
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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br Ubiquitination and deubiquitination pathways Ubiquitinati
2019-12-30
Ubiquitination and deubiquitination pathways Ubiquitination is a part of the post-translational modification (PTM) process. Ubiquitination affects proteins in various ways, but its main functions are to signal protein degradation via the 26S proteasome, modify cellular location of proteins, affec
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Dipeptidyl peptidase inhibitors DPP is or gliptins
2019-12-30
Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit spectinomycin secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good efficacy
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In the case of the reaction of a with
2019-12-30
In the case of the reaction of 1a with Py2SMeCu(II), compound 4a was observed as the major oxidation product suggesting that further oxidation or hydrolysis of 4a was prevented under our conditions. The precise factors that govern the reactivity and stability of nitrosoamidines remain poorly known.
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Interestingly all three lesions that significantly inhibited
2019-12-30
Interestingly, all three lesions that significantly inhibited transcription – CPD, εA and the AP site, – promoted insertion of ixabepilone residues opposite the damaged nucleotide. Thus, bacterial RNAP seems to follow the so-called ‘A-rule’ for incorporation of nucleotides opposite AP-sites and bul
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A939572 br Materials and methods br Statistical analysis
2019-12-30
Materials and methods Statistical analysis All statistical analyses were performed using SPSS software version 20. Protein A939572 data of DNMTs and clinicopathological parameters were collected. Mann-Whitney U Test was used to assess the differential expression of nonparametric data of DNMTs
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Carbazole could be recrystallised from ethyl acetate to prov
2019-12-30
Carbazole could be recrystallised from ethyl acetate to provide bright red crystals suitable for single crystal X-ray diffraction (see ). The first crop showed had crystallised preferentially as the ()-isomer (A). Examining the single crystal X-ray data of it was interesting to find that the N2C15 b
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