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In the Medicines for Malaria Venture
2021-10-09

In 2011 the Medicines for Malaria Venture (MMV) distributed the Open-Access Malaria Box to accelerate antimalarial drug discovery (Spangenberg et al., 2013). The Malaria Box consists of 400 structurally diverse compounds, curated from >20,000 hits generated from large-scale screens, that inhibit the
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Drosophila is a well established model to investigate
2021-10-09

Drosophila is a well-established model to investigate the molecular and cellular defects underlying human neurodevelopmental disorders (Oortveld et al., 2013, van der Voet et al., 2014). Here, we establish Drosophila as a model for understanding the mechanisms linking mutations in KDM5 family protei
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br Conflict of interest statement
2021-10-09

Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements We thank Urann Chan for assistance with the figures. This work was supported in part by National Institutes of
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According to the literature HER mutations are present in
2021-10-09

According to the literature, HER2 mutations are present in 2–4% of lung adenocarcinoma (ADC) patients. Most HER2 mutations are in-frame insertional mutations occurring at exon 20 in the protein kinase domain [[2], [3], [4], [5]]. Although several small molecules and HER2 WZ3146 synthesis have been
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Assays can perform differently by genotype and
2021-10-09

Assays can perform differently by GSK 2193874 and under-quantification of HCV GTs has been seen with HCV assays [8], [9], [10], [11]. Under-quantification of GT4 has been reported in some early studies of the VERIS Assay [7], [12] where a bias greater than −0.5 log10IU/mL was seen. In two more rece
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br STAR Methods br Acknowledgments
2021-10-09

STAR★Methods Acknowledgments Anthony Koleske is thanked for helpful discussions and for providing p190RhoGAP-A cDNA. Anatoly Kiyatkin and Mark Lemmon are thanked for use of the BioTek Synergy 2 plate reader for the MANT assays. Leena Kuruvilla is thanked for assistance with the thermal shift a
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br Conflict of interest statement br Acknowledgments The
2021-10-09

Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). Introduction G protein-coupled receptor 55 (GPR55) has emerg
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thymidylate synthase Acute in vivo experiments were
2021-10-09

Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding thymidylate synthase control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/k
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IBs had a clear vesicular ultrastructure suggesting that a
2021-10-09

IBs had a clear vesicular ultrastructure, suggesting that a large part of the iron-containing mitochondrial remnants might be cleared via normal autophagy processes during final reticulocyte maturation [21]. IB formation was followed by characteristic changes in RBC morphology, with irregularly shap
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Next we focused on B part the phthalazine ring While
2021-10-09

Next, we focused on B-part, the phthalazine ring. While both nitrogen atoms of the phthalazine ring were found to be important (data not shown), replacing the benzene ring of the phthalazine part was attempted, and shows the results of the substituted pyridazine rings with bearing 2-methoxy benzene
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br Conflict of interest br
2021-10-08

Conflict of interest Introduction Since its discovery in 1958 [1]the Ca2+-dependent K+ efflux in human red blood 2 nbdg mg (RBC) (further referred to as the Gárdos effect) has been extensively studied (see 2, 3for review) and has been helpful in understanding the role of the Ca2+-activated K+
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LLY507 receptor Following an endoproteolytic cleavage of C
2021-10-08

Following an endoproteolytic cleavage of C99, γ-secretase trims the remaining fragment Aβ49 or Aβ48 in successive, mostly three-residue steps. Aβ49 typically gives rise to Aβ46, Aβ43, and Aβ40; whereas Aβ48 usually yields Aβ45 and Aβ42 [59]. The physical basis for this characteristic cleavage patter
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br Development of calibrators and controls for DiXaIs br Met
2021-10-08

Development of calibrators and controls for DiXaIs Method validation and comparison with reference technique (LC:MS) At this stage, anti-Factor Xa bioassays can be established for reliably measuring DiXaI concentrations in plasma, with the available appropriate drug specific calibrators and co
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Histone modification is one of the major epigenetic
2021-10-08

Histone modification is one of the major epigenetic mechanisms.8, 10 Specific histone modifications confer active or repressive transcriptional states. For instance, the trimethylation of Histone3-Lysine27 (H3K27me3) is a marker of tightly packaged heterochromatin and is associated with gene repress
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Introduction Histone is the core
2021-10-08

Introduction Histone is the core component of chromatin and histone modification is one of the key mechanisms of epigenetic regulation (Bannister and Kouzarides, 2011). Amino Caspase Inhibitor Set I synthesis residues on histone tails can be modified under different mechanisms including acetylatio
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