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To study the effect of DDR inhibition by imatinib nilotinib
2021-01-08

To study the effect of DDR inhibition by imatinib, nilotinib and dasatinib in a cellular environment we generated DDR1 and DDR2 expressing HEK293 cell lines by stable transfection. Of the five DDR1 splice variants we focused on the 1b variant whose over-expression has been associated with pulmonary
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The DDRs have also been shown to be regulators of
2021-01-08

The DDRs have also been shown to be regulators of certain immunological functions. DDR1 is expressed in stimulated peripheral blood mononuclear (E)-2-Decenoic acid receptor (Kamohara et al., 2001) and on activated T cells (Chetoui et al., 2011, Hachehouche et al., 2010, Kamohara et al., 2001). DDR1
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Itch also known as astrophin
2021-01-08

Itch, also known as astrophin-1 interacting protein-4 (AIP4), is a HECT domain-E3 ligase. It was discovered in 1998 in mouse coat color genetic studies which displayed the disruption caused by the Itch gene inducing a lethal autoimmune inflammatory condition. The substrates of Itch are transmembrane
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The three dimensional crystal structure of Ca loaded CaM rev
2021-01-08

The three-dimensional crystal structure of Ca2+ loaded CaM reveals a dumbbell-shaped molecule with two roughly globular lobes, the N- and C-terminal lobes linked by a long solvent-exposed helix, which has been shown by NMR to be non-helical in its central part and flexible in solution [13]. Each glo
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Atipamezole hydrochloride Fig S an
2021-01-08

Atipamezole hydrochloride (Fig. S1), an α2-adrenoceptor antagonist, is commonly used by veterinarians to recover animals from sedation-anesthesia induced by α2-adrenoceptor agonists. Recent studies in animals suggest that atipamezole might have beneficial effects in Sunitinib damage repair, it also
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Almost of drugs in the market
2021-01-08

Almost 75% of drugs in the market undergo deactivation though oxidation, reduction or hydrolysis by cytochrome P450 (CYP) enzymes, and then, either directly or by facilitated excretion from the body (Guengerich, 2008). The CYP3A subfamily is of particular interest because of its broad substrate spec
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Previous studies demonstrated that cPLA translocates to the
2021-01-07

Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at
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Collectively the results presented here provide new insights
2021-01-07

Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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One of the critical functions
2021-01-07

One of the critical functions of the product of the AR gene is to activate the expression of target genes. This transactivation activity resides in the N-terminal domain of the protein encoded in exon 1, which contains polymorphic repeats. These trinucleotide repeats, (CAG) and (GGC), encode polyglu
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Like compound substitution on compound contains amino and ca
2021-01-07

Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226.
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Several single nucleotide polymorphisms SNPs in humans affec
2021-01-07

Several single nucleotide polymorphisms (SNPs) in humans affect CYP3A expression and activity (Lamba et al., 2002). The CYP3A4 SNP rs2740574 (also referred to as CYP3A4*1B, by The Human Cytochrome P450 (CYP) Allele Nomenclature Database, http://www.cypalleles.ki.se/) is a change in the promoter regi
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Nearly years ago the first two enzymes which catalyze the
2021-01-06

Nearly 60years ago, the first two Icotinib receptor which catalyze the phosphorylation of proteins were discovered [1]. Protein phosphorylation was originally identified as a regulatory mechanism for the control of glycogen metabolism. Today it is clear that protein phosphorylation regulates most a
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Although it remains an unsettled issue evidence favors
2021-01-06

Although it remains an unsettled issue, evidence favors that the endothelin ETA Carprofen synthesis may play a more important pathological role. While both endothelin ETA and ETB receptors are found in most tissues, endothelin ETA receptor is the predominant receptor responsible for the vasoconstri
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Another clinical study indicated the daily consumption
2021-01-06

Another clinical study indicated the daily consumption of green tea with low concentrations of theanine and catechin would improve cognitive function (Ide et al., 2014). Further, in a double blind randomized clinical study involving 102 patients, the Hypericum extract was examined in terms of effica
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Docking experiments showed that Me MeGlcA
2021-01-06

Docking experiments showed that Me-MeGlcA3Xyl4 and MeGlc3Xyl4 were bound to EcXyn30A and the R293A variant in the same way as MeGlcA3Xyl4, having MeGlcA or its modified forms accommodated in the -2b subsite. All ligands were coordinated by the same Cynomolgus ANGPTL7 / Angiopoietin-like 7 Protein (H
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