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In the phase I AURA trial patients with EGFR activating
2019-10-12
In the phase I AURA trial, patients with EGFR activating mutations and centrally confirmed tumor and/or plasma genotyping (BEAMing) T790M result were enrolled. Among 216 patients with both plasma and tissue genotyping results, the concordance rate was 82% for Lck Inhibitor 19 deletions, 86% for L85
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In the present study DRD decreased in the VTA of
2019-10-12
In the present study, DRD3 decreased in the VTA of OA when compared with the control group. It is reported that DRD3 in the VTA control the firing rate of dopaminergic neurons and inhibition of these receptors enhance firing in the VTA-projecting neurons [18]. A study also indicated that morphine tr
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Nitric oxide NO is synthesized by conversion of the
2019-10-12
Nitric oxide (NO) is synthesized by conversion of the l-arginine to NO and l-citrulline through reaction which is catalyzed by nitric oxide synthetase (NOS) (Knowles and Moncada, 1994). NO as an important molecule not only play a role as second messenger but also binds to cytochrome c oxidase and de
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Sodium Nitroprusside br STAR Methods br Acknowledgments We
2019-10-11
STAR★Methods Acknowledgments We thank members of R.L. lab and F. Schweisguth for critical reading of the manuscript. We are also grateful to F. Janody, M. Miura, C. Bökel, H.D. Ryoo, G. Jiménez, the Bloomington Drosophila Stock Center, the Drosophila Genetic Resource Center, the Vienna Drosoph
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Our previous high throughput screening HTS campaign using au
2019-10-11
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based Xylometazoline HCl assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [
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Etomoxir br Mechanisms of acquired resistance to st
2019-10-11
Mechanisms of acquired resistance to 1st and 2nd generation EGFR inhibitors After treatment with first or second generation EGFR TKIs, virtually all patients after approximately 12 months develop acquired resistance (AR). Different mechanisms of AR to EGFR TKIs have been reported to date and may
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In summary we hypothesize that targeting the A R D
2019-10-11
In summary, we hypothesize that targeting the A1R–D1R heterotetramer with heteromer-selective drugs might improve safety and efficacy of the pharmacological therapy for RLS and other motor diseases, resulting in fewer side effects than classical drugs developed for targeting monomeric A1R or D1R.
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br Phenotypic responses alkylation induced cell death and
2019-10-11
Phenotypic responses: alkylation-induced cell death and mutagenesis E. coli alkB mutants were isolated in a screen for strains specifically sensitive to the cytotoxicity of MMS but not UV-irradiation. This was the first indication that the AlkB protein is a primary cellular defence against alkyla
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br Introduction Malaria remains a
2019-10-11
Introduction Malaria remains a serious parasitic disease in tropical areas due to its high morbidity and mortality rates. It is estimated that 212 million cases occurred globally in 2015, leading to 429, 000 deaths, most of which were in children aged under 5 years in Africa [1,2]. The protozoans
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Recently Schenck et al identified an
2019-10-11
Recently, Schenck et al. [25] identified an active site asparagine 222 (N222) residue in the Glycine max TyrAp/PDH (GmPDH1) that is responsible for its prephenate substrate specificity. Mutating the single N222 into an acidic residue (i.e. aspartate, D) in the legume TyrAp/PDH shifted from prephenat
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One of the most frequent gene alterations in
2019-10-11
One of the most frequent gene alterations in MM is methylation of the p15 and p16 genes in the 5′ upstream region. P15 and p16 proteins are CCK-8 regulators involved in the inhibition of transition from G1 to S phase. Frequencies of p15 or p16 gene methylation up to 32% and 53%, respectively, have
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br Results br Discussion The importance of
2019-10-10
Results Discussion The importance of mitochondria for the initiation and progression of tumorigenesis is now emerging. It is evident that, despite the well-known Warburg effect, tumors have active mitochondrial bioenergetic metabolism (Marin-Valencia et al., 2012, Hensley et al., 2016). Disrup
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DDR is characterized by an N terminal discoidin domain and
2019-10-10
DDR2 is characterized by an N-terminal discoidin domain and a C-terminal kinase domain [7]. Characteristics of DDR1, which is a homologue of DDR2, have been extensively investigated in terms of expression level in cancer tissues and biological functions in normal and cancer cell conditions, but char
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To overcome problems with the biochemical reconstitution of
2019-10-10
To overcome problems with the biochemical reconstitution of these heterodimeric cytokines fusion strategies linking both subunits together have been proposed inspired by the “hyper-IL-6” [28]. Much like fusing a protein to a solubility enhancing protein such as MBP or SUMO, fusing two subunits of a
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A series of monocarboxylated chalcones e g compounds
2019-10-10
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 Alosetron was not sensit
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