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A straightforward synthetic pathway was adopted to synthesiz
2023-11-01
A straightforward synthetic pathway was adopted to synthesize the target compounds as outlined in . The starting chloromethylquinazolinones (–) were synthesized from anthranilic Alda 1 in two steps following reported procedures., , , The first step involves chloroacetylation of anthranilic acid us
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OCT also is known as
2023-11-01
OCT4 (also is known as POU5F1) plays an important role in embryonic stem cell self-renewal, development and reprogram somatic cell into pluripotent stem cell [[5], [6], [7]]. Recently, many studies also find OCT4 promotes the progression of many tumors. For example, Wnt/β-catenin promotes the expans
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br ABCA and cancer drug
2023-11-01
ABCA2 and cancer drug response Overall, the expression of ABC transporters has been linked with multidrug resistance phenotypes through the efflux of drugs via ATP-dependent transport. For example, 13 distinct transporters (ABCA2, ABCB1, ABCB4, ABCB11, ABCC1–6 ABCC10, ABCC11 and ABCG2) have been
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Mass spectrometry MS analysis and
2023-11-01
Mass spectrometry (MS) analysis and selective enrichment methods of phosphorylated proteins are powerful tools that can help address these challenges. Recent advances in MS have made it possible to analyze signaling pathways by facilitating high-throughput identification of phosphorylation sites wit
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Further investigations were concerned to
2023-11-01
Further investigations were concerned to study the mechanisms by which GABA modulates adenosine-mediated effects in hippocampal tissue. From these results it can be concluded that endogenous GABA exerts an inhibitory effect through GABAA receptors via a predominant adenosine-mediated action and this
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ML133 HCl mg Regarding A Rs and A ARs basal
2023-11-01
Regarding A1Rs and A2ARs, basal conditions generate a low tone of endogenous adenosine and cause A1R activation, in contrast to situations of increased adenosine where A2AR activation becomes dominant. When adenosine concentrations rise, e.g. during hypoxia, also time appears likely important in reg
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Given the powerful and ubiquitous nature of adenosine action
2023-11-01
Given the powerful and ubiquitous nature of adenosine action within the CNS, basal levels of extracellular adenosine are carefully regulated and are estimated to be in the region of 30–300 nM (Fredholm et al., 2001). The two main pathways for the control of extracellular adenosine involve phosphoryl
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Plant material and growth conditions Arabidopsis
2023-11-01
Plant material and growth conditions. Arabidopsis thaliana ecotype Columbia was grown on a mixture of soil, vermiculite, and perlite (4:2:1) with a 16h light/8h dark Celecoxib in a temperature-controlled growth room (22°C), unless indicated otherwise. Molecular cloning and plant transformation. The
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Small kinase inhibitors have been developed to block AXL by
2023-11-01
Small kinase inhibitors have been developed to block AXL by interacting with the kinase cytoplasmic ATP binding site. Up to date, no AXL selective kinase inhibitors are marketed. As depicted in , some marketed kinase inhibitors such as Bosutinib and Cabozantinib or kinase inhibitors in clinical pha
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Aurora A or B selective and
2023-11-01
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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The overall mechanism of the Cdc complex
2023-11-01
The overall mechanism of the Cdc48 complex resembles that of the 19S regulatory subunit of the proteasome, which also uses receptor proteins to bind polyubiquitin chains attached to a substrate and employs a translocation mechanism (for review, see Kish-Trier and Hill, 2013). As with Cdc48, full sub
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br Conflicts of interest br Introduction Phosphatidic acid p
2023-11-01
Conflicts of interest Introduction Phosphatidic dopamine receptors phosphatase (PAP) enzymes are responsible for catalyzing the reaction that dephosphorylates phosphatidic acid (PA), which in turn produces diacylglycerol (DAG) and a phosphate group during phospholipid regulation (Fig. 1A) [1]
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br Author contributions br Acknowledgments TJC KW
2023-11-01
Author contributions Acknowledgments TJC, KW, and VG are supported by awards made to MJN: a Consolidator Grant from the European Research Council under Grant no. 311336; a University Research Fellowship from the Royal Society, and a Career Development Award from the Human Frontiers Science Pro
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Several MAP kinases are involved in the signal
2023-11-01
Several MAP kinases are involved in the signal transduction pathways that lead to the upregulations of inflammatory mediators. Moreover, transcriptional activations of STATs are regulated by MAP kinases, as evidenced by reports that p38 MAPK is necessary for the S727 phosphorylation of STATs (Kovari
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Applications for protein switches are numerous
2023-11-01
Applications for protein switches are numerous. In diagnostics, protein switches can detect analytes as components of inexpensive homogeneous assays that do not require specialized equipment or time-consuming incubation and washing steps characteristic of immunoassays [8]. Protein switches have also
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