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For the NSCLC patients with
2023-05-30

For the NSCLC patients with EGFR-activating mutations, EGFR-TKIs (gefitinib and erlotinib) are effective clinical therapies [21], [22]. However, approximately 10% of patients harboring EGFR-sensitizing mutations exhibit intrinsic resistance, and up to 40% do not attain a major response to treatment
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Having taken a step back from affinity to
2023-05-30

Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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br Materials and methods br Results and
2023-05-30

Materials and methods Results and discussion In our previous studies (Matarneh et al., 2017), mitochondria were mechanically disrupted and separated into supernatant and pellet fractions by centrifugation. The causative agent for enhnced glycolytic flux was shown to be a protein that resides i
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In liver the essential organ of lipoprotein synthesis ACL pl
2023-05-30

In liver, the essential organ of lipoprotein synthesis, ACL plays a fundamental role in lipogenesis and steroidogenesis by supplying cytosolic Selumetinib to both pathways. By using a tricarboxylic acid cycle intermediate (citrate) to produce acetyl CoA, ACL can be seen as an important bridge betwee
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From an historical perspective ligands for GPCRs adrenaline
2023-05-30

From an historical perspective, ligands for GPCRs (adrenaline, serotonin, WIN 18446 or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands were
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br Conclusions The present protocol for localizing or spotti
2023-05-29

Conclusions The present protocol for localizing or “spotting” the site of action of an antioxidant in a micro-heterogeneous medium is based on the differences in its reactivity vis-à-vis the series of amphiphobic TEMPO derivatives 1a–f. Plots of the relative antioxidant effectiveness of a given A
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Similar studies in Swedish Mutation of APP AD
2023-05-29

Similar studies in Swedish Mutation of APP AD transgenic mice revealed reduced dynamin 1, AP180, and synaptophysin expression in the hippocampus, particularly prominent in the CA1 and CA4 subfields [19]. These findings imply that Aβ can act not only as a modulator of exocytosis but is a potent regul
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It was reported that oral administration of
2023-05-29

It was reported that oral administration of CSZ to C57BL/6J mice significantly improved spatial learning and memory, and prevented Aβ-induced immunoresponse in Aβ25-35-injected mice. However, post-treatment with CSZ after Aβ25-35 administration, when Aβ was already accumulated, did not prevent Aβ-in
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Raltitrexed AAT enzyme activity was readily detected in
2023-05-29

AAT enzyme activity was readily detected in crude cell-free extracts obtained from berry tissues of all accessions but displayed different substrate selectivities (Fig. 2). Cell-free extracts derived from ‘Muscat Hamburg’ berries showed the highest AAT activity with all alcoholic substrates tested,
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The current guidelines are designed
2023-05-29

The current guidelines are designed to optimize the detection of IHC+FISH+ cases, most of which (but not all encountered in our study) being classically good responders to crizotinib therapy (resistance mechanisms to crizotinib therapy were not investigated in our study). In addition to the current
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br Conclusion br Conflict of interest br
2023-05-29

Conclusion Conflict of interest Acknowledgments We thank Nancy Kerkvliet for helpful advice. The research in the lab of CE and THS is supported by the Deutsche Forschungsgemeinschaft (grants ES103/7-1 and 9-1, HA7346/2-1). We apologize to all authors whose work could not be cited due to lim
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br Conclusions and clinical relevance Astrogliosis and an in
2023-05-29

Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic Chromocarb is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R agonists or ADK inh
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Moreover our present work suggests that AXL
2023-05-29

Moreover, our present work suggests that AXL could be a modulator of sunitinib response, at least for cell lines that present high endogenous levels of this RTK activation, since we observed an increased responsiveness to sunitinib in omecamtiv synthesis activated with AXL receptor ligand. A role fo
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Additionally in a previous transgenic model with
2023-05-29

Additionally, in a previous transgenic model with autotaxin under the control of the MMTV-LTR promoter, aberrant expression of human autotaxin caused late-onset, metastatic breast cancer [5]. The AT-ATX transgenic model is analogous to the previous one because ∼30% of all spontaneous tumors appeared
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In response to DSB the lesion recognition factor Mre Rad
2023-05-29

In response to DSB, the lesion recognition factor Mre11-Rad50-Nbs1 (MRN) complex helps the recruitment of ATM to the damage site and its activation by phosphorylation [29]. However, whether UV-damage recognition factors directly influence ATR and ATM recruitment and their phosphorylation is not clea
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