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For most enolases fluoride acts as an inhibitor
2021-03-29
For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby
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The glycolytic pathway is a catabolic route that ends
2021-03-29
The glycolytic pathway is a catabolic route that ends with the synthesis of pyruvate (Pyr). In Arabidopsis embryos, the conversion of phosphoenolpyruvate (PEP) to Pyr, catalyzed by pyruvate kinase (PK), is mainly located in the plastids [10], [11]. The preceding reaction is catalyzed by enolase (ENO
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While these previous correlative studies have measured tDDR
2021-03-29
While these previous correlative studies have measured tDDR1 protein by IHC, these studies have not considered that pDDR1 could also be an important marker of cancer prognosis. A phosphoproteomic survey of lung cancer tissues did identify pDDR1 as one of the most commonly phosphorylated receptor kin
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The synthesis of compounds a and b are outlined in
2021-03-27
The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of XAP044 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and 7b were obta
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Herein the interactions of etamicastat nepicastat and zamica
2021-03-27
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the CFDA-SE australia exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP
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The human serotonin hydroxytryptamine HT receptor family
2021-03-27
The human serotonin (5-hydroxytryptamine; 5-HT) receptor family consists of 14 receptor subtypes to date, which are primarily G protein-coupled receptors (GPCRs) with 5-HT3 being the sole ligand-gated ion channel (Alexander et al., 2017). These receptors are widely distributed in the central and per
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G DH has gained interest because of
2021-03-27
G3DH has gained interest because of its broad substrate specificity and site-selective oxidation properties [9,10]. The conversion product, 3-ketoglycoside, possesses potential as a starting material for the chemical industry such as in polymer and surfactants because the keto group becomes a specif
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br Conflicts of interest br Acknowledgments Work in the labo
2021-03-27
Conflicts of interest Acknowledgments Work in the laboratory of SPS is funded by Council of Scientific and Industrial Research (CSIR) Network Project BSC-0111 (INDEPTH) and BSC-0112 (NanoSHE). We are thankful to Director, CSIR-IITR for his constant encouragement and support. We also acknowledg
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Bmp products such as Fig are persistent pollutants
2021-03-27
Bmp7 products, such as 7–9 (Fig. 2), are persistent pollutants that accumulate in the marine environment and can potentially be transferred to the human population via our trophic connections to the oceans (Wan et al., 2009). In addition to potentially addressing the mechanistic curiosities describe
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The detection of galactomannan GM
2021-03-27
The detection of galactomannan (GM), a polysaccharide that is released during Aspergillus growth, is a useful and reliable non-invasive diagnostic test for screening and management of aspergillosis and is often more sensitive than culture (Schelenz et al., 2015, Fisher et al., 2013). The level of ga
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Our conclusion is in disagreement with that of
2021-03-27
Our conclusion is in disagreement with that of a recent paper by Park et al. [10], which suggests that nitric oxide (NO) inhibition of VHL recruitment occurs by nitrosylation of the 520 cysteine in HIF-1α, and that SNAP does not directly inhibit hydroxylation of HIF peptide by HPH-2. Although this d
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P H is a nonheme iron
2021-03-27
P4H is a nonheme iron(II) dioxygenase that uses O2 and α-ketoglutarate as co-substrates (Fig. 1A). The three-dimensional structure of mammalian P4H is unknown. We reasoned that an electrophilic analog of α-ketoglutarate could serve as an irreversible inhibitor of the enzyme and, hence, a useful prob
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In this report we established
2021-03-27
In this report, we established mouse models suitable for human retinal cell transplantation by introducing phosphodiesterase 6B (Pde6b) mutant allele from retinal degeneration (rd) mouse models into NOG background. Pde6b (rd1) and Pde6b (rd10) mice are well-studied and frequently used animal models
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UVRAG is a mammalian ortholog of yeast Vps and a
2021-03-27
UVRAG is a mammalian ortholog of yeast Vps38 and a promoter of autophagy [51,60,61]. It forms distinct complexes with BECN1 (mammalian ortholog of yeast Vps30/Atg6) and the class III phosphatidylinositol 3-kinase (whose catalytic subunit [PIK3C3] is the mammalian ortholog of yeast Vps34) and contrib
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Given that dimethylamine substitution was tolerated as in SR
2021-03-27
Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated SB 431542 amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR20039). The sl
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