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We have previously disclosed the discovery
2020-04-21

We have previously disclosed the discovery of a 7-azaindole-3-acetic atm inhibitor CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that wor
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br Methods br Results br
2020-04-20

Methods Results Discussion Preclinical data indicate that nepicastat modulates sympathetic drive to the CGP 54626 hydrochloride with a mild pressor effect in various animal models of hypertension (Stanney et al., 1998). However in this clinical study, the doses of nepicastat employed did n
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br Conclusions br Acknowledgements br Protein
2020-04-20

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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For human health risk assessment of chemicals a default unce
2020-04-20

For human health risk assessment of chemicals, a default uncertainty factor (UF) of 3.16 is used to capture inter individual variation in toxicokinetics (Dorne and Renwick, 2005). However, the scientific background for this default UF remains unsatisfactory., Several studies have reported that a fac
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In sum although it is reasonable to assume that
2020-04-20

In sum, although it is reasonable to assume that the activities of an enzyme on alternative (metabolically available) substrates may often depend on neutral drift, the point is difficult to prove because various types of selective pressures can be at play, and these will be different in different o
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Introduction Protein ubiquitination is a posttranslational m
2020-04-20

Introduction Protein ubiquitination is a posttranslational modification that plays a major role in almost all cellular processes in eukaryotes (Hochstrasser, 2009; Komander & Rape, 2012). It involves the covalent attachment of ubiquitin (Ub) via its C-terminal glycine carboxylate to a primary amin
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Meanwhile high levels of extraversion have been
2020-04-18

Meanwhile, high levels of extraversion have been associated with weaker conditioning and faster Terazosin learning (Eysenck, 1970). Similar to neuroticism/anxiety, the role of extraversion for fear conditioning and extinction has found only limited empirical support (Rauch et al., 2005) with severa
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Altogether the results of this study demonstrate that periph
2020-04-18

Altogether, the results of this study demonstrate that peripheral blockade of both ETA and ETB receptors reduces tumor-induced facial heat hyperalgesia and increased spontaneous grooming, without modifying ongoing nociception. It is possible to suggest that bosentan is acting upon both receptors pre
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While PRRSV has been recently
2020-04-17

While PRRSV has been recently shown to induce SGs, the exact nature of SG formation and its underlying mechanism of regulating antiviral immune response during PRRSV infection remain unclear (Zhou et al., 2017). Formation of PRRSV-induced SGs was observed in MARC145 Disodium (R)-2-Hydroxyglutarate a
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br Authors contribution br Disclosure statement br
2020-04-17

Authors contribution Disclosure statement Acknowledgements This study has received funding from the Italian Ministry of University and Research (PRIN 2015, grant number 2015373Z39_008) and from the Innovative Medicines Initiative 2 Joint Undertaking under grant agreement No 115797 (INNODIA)
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HC-030031 Introduction Trichloroacetic acid TCA might
2020-04-17

Introduction Trichloroacetic HC-030031 (TCA) might enhance the activation of T cells and disrupt various activities of peripheral T cells [1], which is related to human immune function and reduces human immunity. Trichloroethylene (TCE) has been widely used in many manufacturing industries [2], an
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The possibility that a carboxyl group attached to the or
2020-04-17

The possibility that a carboxyl group attached to the or position of an -arylaminomethylenemalonate ester would lead to increased selectivity for DHODH has been tested and found not to be the case. Indeed, reduced selectivity compared with the corresponding ester is observed and is attributed to a ‘
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We report here that DAPK signaling pathways play significant
2020-04-17

We report here that DAPK signaling pathways play significant roles in OGD-induced neuronal death. Exposure of the all trans retinal to OGD led to DAPK activation, which then promoted cell death through BimEL overexpression. Furthermore, DAPK-induced BimEL overexpression was mediated by inactivating
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Our results implicate a critical role for CXCR in
2020-04-17

Our results implicate a critical role for CXCR-1 in promoting the migration of colonic tumor cells. Expression of this receptor, but not CXCR-2, increased significantly because of the EMT (Fig. 3). Moreover, although Clone A BCH express comparable levels of both IL-8 receptors, only CXCR-1 inhibit
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br Results br Discussion Unraveling
2020-04-17

Results Discussion Unraveling the molecular details of nucleoporin-karyopherin interactions, which have to be strong enough to promote transport but sufficiently weak to avoid stalling of transport complexes within the pore, is key to our understanding of the mechanisms of nucleocytoplasmic tr
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