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br The hedgehog signalling pathway The canonical Hh pathway
2021-09-11

The hedgehog signalling pathway The canonical Hh pathway is a conserved, highly complex signalling cascade, with many players and intricate regulation. However, it can be simplified into four fundamental components: i) the ligand Hh, ii) the receptor Patched (Patch [PTCH1]), iii) the signal trans
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Some data also suggested that CCR could
2021-09-11

Some data also suggested that CCR5Δ32 could influence the progression of HCV-related liver diseases (Goulding et al., 2005; Hellier et al., 2003; Wald et al., 2004). However, after stratifying HCV+ individuals according to clinical/histological criteria, no association of CCR5Δ32 with these HCV-rela
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br GC C and cGMP of
2021-09-11

GC-C and cGMP: of mice and men As is usually the case for many genes, most of the studies that relate to GC-C have to date been carried out in mouse models, or in cell lines derived from human colorectal cancer tissue. What appeared to be a lacuna was any report of a human disorder that resulted
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GSTP c C T SNP was genotyped
2021-09-11

GSTP1 c.341C > T SNP was genotyped in 90 patients tumor and 180 normal healthy individuals. The profile of GSTP1 c.341C > T STF-62247 sale and genotypes is shown in Table 2. The profile of the genotypes was in agreement with Hardy-Weinberg equilibrium (χ2 = 2.11). Minor allele frequency (341T) amo
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After establishing improved GSNOR potency some
2021-09-11

After establishing improved GSNOR potency, some of the potent inhibitors were further evaluated for microsomal stability and CYP inhibition studies (). Majority of the tested analogs revealed high metabolic stability in human and rat liver microsomes, and moderate to low stability in mouse liver mic
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We previously evaluated the immuno modulatory efficacy of
2021-09-11

We previously evaluated the immuno-modulatory efficacy of GSNO in different EAE models and reported prophylactic and therapeutic efficacy of GSNO against the clinical disease of EAE [22], [36]. GSNO inhibited the IL-6-induced STAT3 activation (Tyr705 phosphorylation) by S-nitrosylation of the STAT3
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In the brain hydrolysis of AG by MGL
2021-09-11

In the brain, hydrolysis of 2-AG by MGL is the primary source of AA for conversion to PGs by cyclooxygenase (Nomura et al., 2011). PGE2 production is required for IL-1β-evoked synapse loss (Mishra et al., 2012). Here, we tested whether decreased PG levels contributed to the synapse protective effect
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Glucagon was described as an
2021-09-11

Glucagon was described as an insulin secretagogue as early as 1965 (Samols et al., 1965). Our studies extend these findings by demonstrating that this is a direct effect mediated by distinct receptors in the mouse pancreas. Previous experiments on isolated β dapagliflozin synthesis clearly show that
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Introduction G quadruplexes are therapeutically important no
2021-09-10

Introduction G-quadruplexes are therapeutically important non-canonical nucleic (+)- Corydaline mg structures that are formed by a planar assembly of four guanines, termed G-tetrads (Fig. 1), in the guanine rich regions of genome [[1], [2], [3]]. As it is getting increasingly established, several
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The subcellular redistribution of some metabolic enzymes is
2021-09-10

The subcellular redistribution of some metabolic enzymes is dynamic and responsive to metabolic conditions. In the absence of glucose, Glucokinase (GK) is bound to its regulatory protein in the nucleus of the hepatocyte and translocates to the cytoplasm when sugar levels increase [12]. Muscle glycog
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br Hippo pathway signalling The Hippo pathway is an evolutio
2021-09-10

Hippo pathway signalling The Hippo pathway is an evolutionarily conserved signal transduction pathway regulated by cell-cell contact, cell polarity, mechanical cues, ligands of G-protein coupled receptors, and cellular Y-27632 australia status [10]. This pathway is linked to development, cell pr
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br Acknowledgments Work in SI
2021-09-10

Acknowledgments Work in SI’s laboratory is supported by grant IM 20/4-1 from the Deutsche Forschungsgemeinschaft, Bonn (Germany) and grant EKFS 2012_A309 from the Else Kröner Fresenius Stiftung, Bad Homburg (Germany). FW’s group is supported by the Dr Vaillant Foundation and the Dutch Burns Found
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Numerous strategies of cardiomyocyte protection are effectiv
2021-09-10

Numerous strategies of cardiomyocyte protection are effective in preclinical, animal models and in small clinical trials. However, most have disappointed in large clinical trials [4,5]. Failures of cyclosporine and post-conditioning to mitigate reperfusion injury are recent examples [[6], [7], [8]].
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Having identified initial leads and
2021-09-10

Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic Z-IETD-FMK derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl, chlo
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Notably Cu labeled dimeric exendin subunit which was designa
2021-09-10

Notably, 64Cu-labeled dimeric exendin-4 subunit, which was designated as 64Cu-Mal2Sar-(exendin-4)2, showed higher tumor uptake than that of the monomeric exendin-4 subunit [245]. Besides the most commonly-used GLP-1R agonists exendin-3 and -4 and their derivatives, exendin (9-39) exhibits strong bi
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