• Historically covalent drugs have had great

  2019-08-13

  

  Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form

• br Funding This work was

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  Funding This work was supported by the National Natural Science Foundation of China (grant number 81671411); Beijing Natural Science Foundation (grant number 7162062); Beijing Nova Program Interdisciplinary Cooperation Projects (grant number Z161100004916045); Beijing Municipality Health Technolo

• br Funding This work was supported by

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  Funding This work was supported by a research grant of the Deutsche Forschungsgemeinschaft (SCHN477-9-2 to R.S.S), the Manfred-Stolte-Stiftung (to R.S.S.) and by a research grant from the German Cancer Aid (Deutsche Krebshilfe, No. 106696/TP 5 to T.F.). Introduction Death-associated protein k

• Functional studies suggested the presence

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  Functional studies suggested the presence of a cysLT1 receptor. We observed an LTD4-induced cytosolic calcium response, albeit one that was very weak by most standards. The magnitude of the average response was partially explained by the low percentage of A-54556A formula showing a very transient r

• Rambabu et al reported A series of novel

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  Rambabu et al. reported A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives synthesized from readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and further reacted with different substituted am

• br Experimental section br Author contributions br Acknowled

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  Experimental section Author contributions Acknowledgements Introduction Many The impact of in cells are sequential enzymatic reactions where the product of one enzyme serves as the substrate of a second enzyme (1, 2). Experimental evidence suggests that some of these consecutive enzyme-

• Previous studies demonstrated that cPLA translocates to

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  Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at

• Ageing is associated with increased reactive oxygen

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  Ageing is associated with increased reactive oxygen species (ROS) production, oxidative stress and oxidative damage [43,44]. Overproduction of ROS can impair endothelial function by suppressing NO synthesis and scavenging NO thereby decreasing its overall bioavailability. Moreover, sustained oxidati

• Like all other cellular processes ubiquitination is

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  Like all other cellular processes, ubiquitination is also tightly regulated; more so, as myriads of pathways are controlled via this conjugation and dysregulation of ubiquitination has been implicated in various diseases including cancer [16], [17]. Quite a few of such regulatory mechanisms that con

• pgc-1α inhibitor This study had some limitations First a sma

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  This study had some limitations. First, a small number of HP patients were enrolled because of the extreme rarity of this disease, which may have caused some selection bias. Yokoseki et al., found no increase in Th2 cytokines, such as IL-4, in IHP patients (Yokoseki et al., 2014). The sensitivity of

• Several lines of evidence suggest

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  Several lines of evidence suggest that the anxiety provoking behavioral effects of CRF involve CRF1 receptors. CRF1 knockout mice show increased anxiolytic-like activity in the elevated plus maze and a tendency to enter the illuminated region of a light–dark box [49], [52]. In addition, studies usin

• br Conclusions Taken together a distinct

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  Conclusions Taken together, a distinct contrast is observed between ERK1/2 phosphorylation in hypothalamic and extra-hypothalamic Berberine hydrochloride regions. The hypothalamus is the only brain region where ERK1/2 phosphorylation was increased 15minutes after the OF stressor. In SD rats CRFR

• Cepharanthine calculator br Methods br Results IAA abrogated

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  Methods Results IAA-94 abrogated the protective effects of IPC as it increased myocardial infarction (MI) due to IR injury in vitro (Diaz et al., 1999), and also prevented cyclosporine A mediated cardioprotection (Diaz et al., 2013). Moreover, IAA-94-sensitive currents were observed in cardiac

• The strong adsorption of amines to the stationary

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  The strong adsorption of amines to the stationary phase of gas chromatography (GC) columns causes issues such as tailing, ghosting and low reproducibility [12], [13]. A common practice to overcome this problem is the chemical derivatisation of amines prior to GC analysis [14]. Comprehensive reviews

• guanabenz calculator br Materials and methods br Results br

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  Materials and methods Results Discussion Our previous study showed that ERRγ negatively regulates osteoblast differentiation via inhibiting Runx2 transactivity (Jeong et al., 2009). In the present study, we found that ERRγ also induced miR-433 in osteogenic mesenchymal cell lineage C3H10T1/

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