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br Aberrantly enhanced adenosine signaling in retina of oxyg
2024-12-21
Aberrantly enhanced adenosine signaling in retina of oxygen-induced retinopathy Current therapeutic development of ROP focuses on directly targeting VEGF and HIF-1α signaling pathway (Cavallaro et al., 2014, Penn et al., 2008, Mintz-Hittner et al., 2011, Hartnett and Penn, 2012). However, cellula
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As an alternative to chronic receptor blockade we have been
2024-12-21
As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify vomitoxin adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK facilitates
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br Aurora A Aurora B and
2024-12-21
Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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It was reported that overexpression of the rat ACL gene
2024-12-21
It was reported that overexpression of the rat ACL gene in tobacco increased the total ACL activity by 4 fold, which increased the production of fatty acids by 16% [8]. Recently, a 1.7-fold increase of fatty acids and 1.9-fold increase of triacylglycerol (TAG) was observed in Aspergillus oryzae with
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Crystal structures were obtained of sulfonamide and
2024-12-20
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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HBTU Thus a majority of known
2024-12-20
Thus, a majority of known chemical and physico-chemical methods of metallic ions assay has a number of disadvantages, such as a low sensitivity and selectivity, high costs and complexity of the equipment. Therefore, the development of simple cost-effective sensitive methods of quantitative analysis
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The relationship between the apelinergic and
2024-12-20
The relationship between the apelinergic and opioid systems has been previously reported (Lv et al., 2011, Yang et al., 2010). Lv and colleagues showed that naloxone has a suppressive effect on apelin-induced depression-like behavior in mice (Lv et al., 2012a). Furthermore, heterodimerization of GPC
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Most human diseases e g cancer diabetes and neurodegenerativ
2024-12-20
Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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br Experimental and computation Standard samples
2024-12-20
Experimental and computation Standard samples of artemisinin (1) and artemether (2) were purchased from China National Institutes for Food and Drug Control. Their ECD spectra, at a concentration of 1.0–5.0mg/mL in ethanol, were recorded in a quartz cuvette of 1mm optical path length using a Jasco
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Accumulating evidence suggest that patients
2024-12-20
Accumulating evidence suggest that patients with advanced -positive NSCLC are at increased risk of VTE or coagulation disorders during the course of their disease, indicating that cancer genotype might play a role in the occurrence of cancer-related thromboembolism . Here we report the case of a pat
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br Conclusions br Conflict of
2024-12-20
Conclusions Conflict of interest Introduction Plants often encounter a series of abiotic stresses during the growth process, including high salinity, extreme temperatures and drought (Knight and Knight, 2001). Plants can adapt through ionic and osmotic homeostasis or osmotic adjustment, con
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In the isolated right atrium
2024-12-20
In the isolated right atrium, activation of muscarinic receptors and adenosine receptors may block the generation of action potentials in the sinoatrial node, inducing cardiac arrest (Fig. 1, Fig. 2, Fig. 3, Fig. 4, Fig. 5) (Camara et al., 2015, Campbell et al., 1989). Physiologically, this conditio
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The first rationally designed dual mPGES
2024-12-19
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic DNA synthesis inhibitor - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have
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br Experimental procedure br Introduction Migraine is
2024-12-19
Experimental procedure Introduction Migraine is a debilitating neurovascular disorder characterized by recurring unilateral pulsating headaches of moderate to severe intensity, associated with nausea, photophobia and/or phonophobia, lasting from 4 to 72 h (Headache Classification Committee of
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Drug resistance development often involves structurally un r
2024-12-19
Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 Protease inhibitor cocktail with enhanced stability and effectiveness are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of E