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Compound was prepared from chloroindole
2020-11-14

Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole TIC10 derivative (). Derivatives and were prepa
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br STAR Methods br Author Contributions br
2020-11-14

STAR★Methods Author Contributions Acknowledgments The authors thank Monika Kuhn for excellent technical assistance and Dr. Antje Schäfer for valuable scientific input. H.S. was supported by the DFG (FZ 82; Graduate School of Life Sciences and SCHI 425-6/1), and A.V.S. by Northwestern Univer
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The discoidin domain receptors DDR and DDR are receptor
2020-11-13

The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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br Discussion The N terminal domain
2020-11-13

Discussion The N-terminal domain of DDRs has long been recognized as a member of the DS superfamily (Johnson et al., 1993, Karn et al., 1993), and its role in collagen binding is understood in atomic detail (Carafoli et al., 2009, Ichikawa et al., 2007). Our crystal structure shows that the secon
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Expression of EBI and its
2020-11-13

Expression of EBI2 and its function for migration in vitro in T cells was recently reported (Chalmin et al., 2015, Hannedouche et al., 2011, Liu et al., 2011, Pereira et al., 2009). Pereira et al. (2009) used an EBI2 reporter mouse and found that most CD4+ T cells, but only approximately half of the
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Lymphocyte mobility and homing is modulated by the chemoattr
2020-11-13

Lymphocyte mobility and homing is modulated by the chemoattractant receptor subfamily of G protein-coupled receptors (GPCRs) (Campbell et al., 2003, Rot and von Andrian, 2004). B cell migration and position are controlled to a large extent by the lymphoid chemokines CXCL13, CXCL12, CCL19, and CCL21
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Egr together with catecholamine biosynthetic enzymes such as
2020-11-13

Egr1, together with catecholamine biosynthetic enzymes, such as tyrosine hydroxylase (TH), dopamine β-hydroxylase (DBH), and phenylethanolamine N-methyltransferase (PNMT), is induced in adrenal medulla by different types of stress (Liu et al., 2005, Morita et al., 1996, Nankova et al., 1993, Papanik
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Azithromycin Dihydrate br Materials and methods br
2020-11-13

Materials and methods Results Artemis has been reported to possess 5′–3′ exonuclease activity in vitro on ssDNA, as well as DNA-PK-dependent endonuclease activity on single-strand overhang and hairpin DNA structures [11]. However, enzymes within the metallo-β-lactamase family typically contain
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Another important issue in biosensors is to design
2020-11-13

Another important issue in biosensors is to design a simple and potable detection strategy to meet the requirement of the point-of-care (POC) test applications. According to the recent research, by using invertase umbelliferone for hydrolyzing sucrose into glucose, the range of personal glucometer
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DNMT is the dominating enzyme responsible for maintenance of
2020-11-13

DNMT1is the dominating enzyme responsible for maintenance of the DNA methylation pattern and the primary enzyme responsible for copying methylation patterns following DNA replication (Moore et al., 2013). DNMT1 maintains the mitotic inheritance of the original methylation pattern in a cell lineage d
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Melanocyte stimulating hormone release inhibiting factor sal
2020-11-13

Although there was little to no expression change observed by TELI of the recA and ruvA genes upon CAA exposure, other specific repair pathways were induced by both CAA and SO and include the SOS-inducible gene sulA, the DNA repair gene ykfG, the mismatch repair gene mutS, the recombination and repa
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Indeed the alkyl group is not seen
2020-11-13

Indeed, the -alkyl group is not seen in the original crystallographic electron density omit map prior to positioning either inhibitor in DHODH, nor can it be found in the final maps. Rather, the electron density maps are consistent with hydrolysis of the amide to the acid. Once the scaffold was clea
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Targeting both PARP and DHODH for anti cancer therapy
2020-11-13

Targeting both PARP-1 and DHODH for anti-cancer therapy would certainly be beneficial as these enzymes share a common role in the DNA replication and repair mechanisms which are involved in the hyper-proliferation of cancer cells. Since benzimidazole-containing compounds have been reported to show g
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Some studies have been conducted
2020-11-13

Some studies have been conducted on the activities of CYP450 [[28], [29], [30], [31]]. For example, Chen et al. reported that low-dose aspirin induced the in vivo activity of CYP2C19 in healthy subjects [30], Krasniqi et al. reported that CYP2C8*3 and CYP2C9*2*3 variants correlated with ibuprofen-in
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AMD is equally active against a broad
2020-11-13

AMD3100 is equally active against a broad range of HIV-1 and HIV-2 strains, but not against simian immunodeficiency virus (SIV) strains in human PBMC (De Clercq et al., 1994). At this moment it is not clear what coreceptor SIV is using in human PBMC, but it does not seem to be CXCR-4 (Feng et al., 1
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