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Screening a selection of analogues from
2025-02-20

Screening a selection of analogues from this library against the panel of 26 kinases (16, 22, and 24 were screened at 30 μM due to poor solubility; 17 tested at 100 μM) generally demonstrated an increase in activity compared to 5z 3 (Fig. 3, Fig. 6). The benzamide analogue 16 demonstrated >50% inhi
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Matthew et al synthesized and
2025-02-20

Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that 2 deoxy d ribose 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pH
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pregnane x receptor In this study we first determined whethe
2025-02-19

In this study, we first determined whether AIF in bovine LT muscle is expressed and the mitochondria released AIF-mediated apoptosis during postmortem aging. For apoptotic issues, the mitochondrial outer membrane is permeabilized, and AIF translocates to the cytosol and to the nucleus, where it indu
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br Experimental procedures br Results br Discussion Major
2025-02-19

Experimental procedures Results Discussion Major depressive disorder is among the leading causes of disability worldwide (Vos et al., 2015). One of the major causal or exacerbating factors of depression is long term stress or psychological trauma (Liu and Alloy, 2010). Dysregulation of the
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br Metabolic effects of apelin in obesity and type
2025-02-19

Metabolic effects of apelin in obesity and type 2 diabetes Mice fed a high fat diet (HFD) for several weeks become obese, hyperglycemic, hyperinsulinemic and insulin resistant. Acute apelin treatment by intravenous injection or by infusion during a hyperinsulinemic–euglycemic clamp in obese and i
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br Acknowledgments br Protein microarrays were developed to
2025-02-19

Acknowledgments Protein microarrays were developed to provide miniaturized high-throughput tools to study protein function, gonadotropin releasing hormone agonist and post-translational modifications. Just a few years ago, the seminal work performed in Stuart Schreiber's laboratory at Harvard
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br Antifungal resistance what is in a
2025-02-19

Antifungal resistance, what is in a name? Antifungal resistance is an emerging and hot topic in the field of medical mycology. Microbiological resistance is identified by determining minimal inhibitory concentrations (MICs) in vitro for a given antifungal and interpreting this value according to
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br Role of AMPK in inflammation signaling
2025-02-19

Role of AMPK in inflammation signaling Pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), activate Ikβ kinase (IKKβ), which phosphorylates IκBα, triggering the degradation of proteasomal IκB. This liberates active nuclear factor kB (NF-kB) to translocate i
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dopamine receptor antagonist br Experimental section br Abbr
2025-02-19

Experimental section Abbreviations PSA, puromycin–sensitive aminopeptidase; APN, aminopeptidase N; AML, acute myeloid Leukemia; ALL, acute lymphoblastic leukemia; AADR, amino dopamine receptor antagonist deprivation response; PAN, puromycin aminonucleoside; DCC, dicyclohexyl carbodiimide; NHS,
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br Results br Discussion By
2025-02-19

Results Discussion By using an unbiased proteomic screen for xCT binding partners, followed by functional validation, we have made the surprising discovery that mTORC2 regulates amino calcitonin gene related peptide metabolism in tumor cells by phosphorylating serine 26 of the cystine-glutama
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The dependence of blood cell
2025-02-19

The dependence of blood cell production on a limited number of HSC and HPC (hereafter collectively referred to as HSPC) means that protection from potential toxins is essential for maintenance of the hematologic system (see Fig. 1). For example, the generation of blood cells within the intramedullar
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anti-inflammatory agent Medium spiny neurons MSNs in the str
2025-02-19

Medium spiny neurons (MSNs) in the striatum start from a deeply hyperpolarized resting membrane potential, slowly depolarize and show a delayed start of firing during a current injection (Kawaguchi, 1993, Nisenbaum and Wilson, 1995, Planert et al., 2013). The firing pattern during the current injec
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br Materials and methods br
2025-02-19

Materials and methods Results Discussion In this study, we observed that PACAP2 immunoreactivity is mainly distributed in the telencephalon, hippocampus, and cerebellum of the zebrafish brain. This distribution pattern is similar to that reported in a previous study in which PACAP immunorea
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To investigate further the clinical and
2025-02-19

To investigate further the clinical and mutational spectrum associated with -related dyskinesia, we here performed a screen in a large series of patients affected with an unexplained hyperkinetic movement disorder, resulting in the identification of 2 pediatric patients presenting with a novel pheno
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br Colabeling evidence for ACh and GABA
2025-02-18

Colabeling evidence for ACh and GABA cotransmission Though functional demonstrations of ACh/GABA cotransmission remain largely limited to the retina and our recent analyses of cortex (Lee et al., 2010, Saunders et al., 2015a, Saunders et al., 2015b), evidence suggestive of ACh/GABA cotransmission
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