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Since innate immune responses represent
2025-02-18
Since innate immune responses represent the first defense against incoming infectious microorganisms, they are particularly engaged during the early stages of viral infections. Many innate defense mechanisms rely on the engagement of pattern recognition receptors (PRRs) which are conserved, germ lin
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Because of the formation of
2025-02-18
Because of the formation of phosphoenzyme intermediates, the enzymatic Micro BCA protein estimation of P-ATPases can be divided into steps that include a kinase activity, by which an aspartate residue on the enzyme is phosphorylated, and a phosphatase activity, by which the phosphoenzyme is dephosp
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Although the LB domains of
2025-02-18
Although the LB2 domains of mGlu receptors have not been shown to form an extensive interface during activation, they do draw closer to each other, as demonstrated in crystal structures (Kunishima et al., 2000, Muto et al., 2007, Tsuchiya et al., 2002) and by FRET analysis (Doumazane et al., 2013, V
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Crystal structures were obtained of sulfonamide and amide
2025-02-18
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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In addition to connecting high ARG levels with DNMT A
2025-02-18
In addition to connecting high ARG1 levels with DNMT3A/TET2 mutations in MDS/CMML patient biopsies, we also wanted to address the cell type demonstrating elevated ARG1. Following our mouse work, we hypothesized that overexpression of this protein would be found in myelomonocytic dnmt including macr
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As with most G protein coupled receptors GPCRs sustained
2025-02-18
As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et a
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In order to further explore whether the
2025-02-18
In order to further explore whether the cytoprotective effect of isogarcinol against oxidative stress in H2O2-induced HepG2 Milameline cognitive research is a consequence of the breakdown of the endogenous antioxidant defence mechanism, we measured the LDH release, MDA levels, GSH levels and SOD ac
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Plant defensins are cysteine rich cationic peptides of kDa
2025-02-18
Plant defensins are cysteine-rich cationic peptides of 5–8 kDa whose mature domain comprises 45 to 54 amino Disuflo Cy5 azide residues, with an isoelectric point around 9. The global fold of plant defensins consists of a cysteine-stabilized motif (CSα/β) made up of an α-helix and a triple-stranded
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As patients with type diabetes are known to be hyperinsuline
2025-02-18
As patients with type 2 diabetes are known to be hyperinsulinemic per se, this relationship between insulin/IGF1 receptor and AR may point towards a causal role of insulin in AR upregulation. Indeed, this is supported by several previous observations. Beyond the already mentioned AR activation by i
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The androgen receptor gene AR is located on the
2025-02-18
The androgen receptor gene (AR) is located on the X-chromosome and consists of eight exons in humans (Brown et al., 1989; Kuiper et al., 1989). The similar gene structure in mice, monotremes and marsupials indicates AR is highly conserved in mammals (Choong et al., 1998; Faber et al., 1991; He et al
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Alectinib is a second generation ALK
2025-02-17
Alectinib is a second generation ALK antagonist that is built upon a 9-ethyl-6, 6-dimethyl-11-oxo benzo[b]carbazole scaffold (Fig. 5C) [58]. This drug is effective against the ALK L1196M gatekeeper mutation along with C1156Y and F1174L mutations [7]. The 11-oxo group of the drug forms a HNE inhibito
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First investigation of numerous membered ether linked
2025-02-17
First, investigation of numerous 12-14-membered ether-linked macrocycles revealed that smaller motifs were most lipophilic efficient. Compound (3) (12-membered macrocycle) exhibited good cellular potencies (ALK IC50 = 1.0 nM; ALK-L1196 M IC50 = 20 nM) and the highest LipE (4.4) with picomolar bindin
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Increasing evidence indicates that ILCs participate in
2025-02-17
Increasing evidence indicates that ILCs participate in a dialog with CD4+ T Go 6983 [107–110]. This dialog is mediated, in part, through the expression of type II major histocompatibility complex (MHCII) molecules on ILC3s [107]. Depending on the expression of co-stimulatory molecules, MHCII:TCR in
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Last decade has provided a number of
2025-02-17
Last decade has provided a number of studies indicating that AhR signaling could play a role both in the development and in progression of multiple cancer types, with potential implications for cancer therapy (for review see (Kolluri et al., 2017; Murray et al., 2014)). Activation of AhR is consider
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Here we have used transcriptome analysis of primary
2025-02-17
Here, we have used transcriptome analysis of primary neonatal rat cardiomyocytes treated with either the ETR agonist endothelin-1 or the α1-AR agonist phenylephrine to assess differences in their respective signalling networks, and further probed these differences using a panel of fluorescent resona
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