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Our recent discovery M P H R
2020-01-21
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs,
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Among the CYP enzymes CYP D
2020-01-21
Among the CYP450 enzymes, CYP2D has been considered a crucial protein that involves in the metabolism of xenobiotics and drugs (Zanger and Schwab, 2013). Some isoforms of the CYP2D subfamily have been well characterized, such as CYP2D6 due to its clinical importance and CYP2D14 in black cattle (Hama
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In the preclinical evaluation of CRF receptor
2020-01-21
In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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br Alcohol and the amygdala br Alcohol and the CRF
2020-01-21
Alcohol and the amygdala Alcohol and the CRF1 system Given the marked effects of alcohol on inhibitory neurotransmission in the amygdala and the regulation of amygdalar GABAergic activity by CRF and activity at the CRF1 receptor, the CRF system is a logical site for the actions of alcohol in t
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The full length human CPG protein is expressed
2020-01-21
The full-length human CPG2 protein is expressed in CNS tissue with the highest expression in the neocortex, hippocampus and striatum, consistent with mRNA localization patterns of the rat Cpg2 homolog (Cottrell et al., 2004). In the rat, the CPG2 protein localizes primarily to the postsynaptic endoc
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Mass spectrometry has previously been used to examine the pr
2020-01-21
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 Wiskostatin analysis [33], and also by analysis of mass changes to tryptic peptides [34]. The present study, however, ha
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br Results and discussion br Conclusion This study describes
2020-01-21
Results and discussion Conclusion This study describes the development of a highly sensitive on-sorbent derivatisation technique, using the novel high-surface area CMV devices, to sample methamphetamine vapour. Previous methods for air sampling for methamphetamine such as sampling cassettes ha
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TNF a major cytokine that is critical in
2020-01-20
TNF-α, a major cytokine that is critical in acute and chronic inflammation, is responsible from chemotaxis, acute phase reactions and endothelial activation (Mahalingam and Karupiah, 1999). Our study showed that TNF-α is increased significantly in the pyelonephritic rats and montelukast displayed an
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Curcumin is a polyphenol extracted from turmeric which is
2020-01-20
Curcumin is a polyphenol extracted from turmeric, which is commonly used as a spice and food-coloring agent in many cultures [9]. Curcumin possesses anti-inflammatory, antioxidant, and cancer-preventive properties [10], [11], [12]. In addition to these well-known effects, consuming curcumin may bene
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br Conclusions br Acknowledgements br Protein
2020-01-20
Conclusions Acknowledgements Protein tyrosine kinases (PTKs) of Src family are important components in cellular signal transduction pathways that couple diverse extracellular signals to appropriate cellular responses . Their activities are tightly regulated in the cells and aberrant activati
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Pyruvate dehydrogenase multienzyme complex PDHc catalyzes th
2020-01-20
Pyruvate dehydrogenase multienzyme complex (PDHc) catalyzes the oxidative decarboxylation of pyruvate, and subsequently acetylates coenzyme A (CoA) to acetyl-CoA during the tricarboxylic Sildenafil metabolic pathway using thiamine diphosphate (ThDP) and Mg2+ as cofactors. PDHc poses a key role in cy
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br Conflict statement br Introduction
2020-01-20
Conflict statement Introduction Prostate cancer (PCa) is the second most frequently diagnosed cancer and the second leading cause of cancer death in men after lung cancer [1], [2]. The incidence and mortality rate of prostate cancer are significantly higher in developed countries especially th
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Chromocarb sale A series of monocarboxylated chalcones e g c
2020-01-20
A series of monocarboxylated chalcones (e.g. compounds 7 and 8, Fig. 2A) was previously identified as good CysLT1 antagonists [20], and none of them exhibited CysLT2 antagonistic activities (Supplementary Table S1). This study was consistent with reported result that CysLT2 Chromocarb sale was not
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A variety of fused membered
2020-01-20
A variety of fused 6–5-membered ring chemotypes have arisen such as 7-azaindole acetic acids, benzimidazolyl acetic acids, spiro-indolinone acetic acids, and indolizine acetic acids, however, to the best of our knowledge, fused 5,5-membered ring systems have not been reported. Prostaglandin D (PG
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A comparison between tinnitus and controls subjects showed
2020-01-20
A comparison between tinnitus and controls subjects showed increased activity in the left AUD and PHC for the gamma frequency band. The link between gamma band activity in the AUD and tinnitus has been identified using both EEG (van der Loo et al., 2009) and MEG (Weisz et al., 2005, 2007). This is s
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