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ELUXA HM EMSI is an ongoing pivotal Phase II global
2020-06-05
ELUXA 1 (HM-EMSI-202) is an ongoing pivotal Phase II global clinical trial, designed to further investigate the efficacy and safety of Olmutinib in patients T790M-positive NSCLC with acquired resistance after first-line EGFR TKIs. Primary endpoint is ORR according to RECIST 1.1, while secondary endp
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A set of small molecule LigI inhibitors were identified
2020-06-05
A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib
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Therefore in this study we determined whether
2020-06-05
Therefore, in this study we determined whether exogenous LTD, a potent agonist of both CysLT and CysLT receptors , , induces JANEX-1 edema and AQP4 expression in mouse brain; if so, which subtype of the receptors is involved in AQP4 expression in mouse brain and the cultured rat astrocytes. Materi
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br Materials and methods br Results Metabolic stability of
2020-06-05
Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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Next we evaluated the therapeutic potential of compound usin
2020-06-05
Next, we evaluated the therapeutic potential of compound () using the mouse model of collagen-induced arthritis (CIA model), which is the pathological model for RA. Consequently, oral once-daily dosing of 3 mg/kg reduced the overall progression of the clinical score, including inflammation and bone
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In the preclinical evaluation of CRF receptor antagonists
2020-06-05
In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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It was recently reported that a functional single nucleotide
2020-06-05
It was recently reported that a functional single nucleotide polymorphism (rs75932628) within Triggering receptor expressed on myeloid NSC228155 2 (TREM2) is associated with AD (Guerreiro et al., 2013). Homozygous loss of function mutations in TREM2 are also associated with an autosomal recessive f
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In the original ELF study patients
2020-06-05
In the original ELF study [7], patients were considered eligible if they were due to undergo liver biopsy for the investigation of chronic liver disease, defined as abnormal biochemical liver function tests persisting for more than 6 months, ability to provide informed consent and age between 18 and
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br Results and discussion br Conclusion In
2020-06-05
Results and discussion Conclusion In this research, several anti-inflammatory agents with pyrazolo[3,4-d]pyrimidine cores were synthesized. Such choice of large core than regular pyrazole was valid as a proper modification. That most of the prepared compounds showed excellent AI activity. In a
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Whether a school is private or public may also
2020-06-04
Whether a school is private or public may also be an indicator of its quality. In general, private schools have smaller class sizes which may provide a better learning environment. Lindquist and Smith (2013) state that smaller class sizes provide more opportunities for students to interact with prof
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Using characteristic features of ECM proteins and a computat
2020-06-04
Using characteristic features of ECM proteins and a computational pipeline combining interrogation of protein and gene databases, we previously defined the matrisome as the ensemble of ECM and ECM-associated proteins [[16], [17], [18]]. In mammals, the matrisome represents 4% of the genome, or appro
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The major concern of PDE I use in
2020-06-04
The major concern of PDE-5-I use in liver cirrhosis is the potentially harmful effect on systemic blood pressure. Data of clinical studies are conflicting [27], [30], [31], [32], but available patient details suggest that in advanced liver cirrhosis, PDE-5-Is lower systemic blood pressure to a great
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br Author contribution br Acknowledgements We
2020-06-04
Author contribution Acknowledgements We want to thank Dr. Manuel Rodriguez, Dr. Ch. Blattner, Dr. Jorge Moscat, Dr. Erwin Knecht and Dr. Peter Tontonoz for materials. This work has been supported by grants from the Spanish Ministry of Education and ScienceSAF2011-27442 and a grant from General
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A growing number of other post translational modifications a
2020-06-04
A growing number of other post-translational modifications are implicated in regulation of the ubiquitin system, including substrate modification by hydroxylation, glycosylation, acetylation, methylation, modification by poly(ADP-ribose) (PAR), and attachment of ubiquitin-like modifiers. The HIF1-α
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The mesolimbic dopamine system is believed to be highly
2020-06-04
The mesolimbic dopamine system is believed to be highly important for evaluating environmental stimuli in order to generate an adaptive behavioral response. Thus, not surprisingly these functions appear to have been highly conserved across the vertebrate subphylum. Even though teleost fish lack midb
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