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Introduction Formate dehydrogenase enzymes FDHs are a group
2021-05-24
Introduction Formate dehydrogenase enzymes (FDHs) are a group of heterogeneous proteins that catalyse the reversible formate () oxidation to carbon dioxide () (Eq. (1)). These enzymes are classified in two families, one gathering the enzymes that hold no redox-active centres and another that includ
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Piperlongumine synthesis DDR expression is upregulated in th
2021-05-24
DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident Piperlongumine synthesis is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic act
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br Materials and methods br Results br Discussion In
2021-05-24
Materials and methods Results Discussion In this study, we developed a new CysLT1 and CysLT2 receptors-mediated N,N-Dimethylsphingosine guinea pig model for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. Unlike human CysLT2 receptors, which are equally stimulated by both
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Several highly potent CysLT receptor antagonists
2021-05-24
Several highly potent CysLT1 receptor antagonists with large structural Repaglinide have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, and thiazo
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The body wall intestine seminal receptacle and seminal vesic
2021-05-24
The body wall, intestine, seminal receptacle and seminal vesicle in the adult worms were also isolated and homogenized to make microsomal fractions to investigate the relative expression of CYP1A2, CYP2E1 and CYP3A4 in these different organs. In order to get sufficient mass, about 20 individual adul
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Diclofenac ibuprofen and meloxicam are
2021-05-24
Diclofenac, ibuprofen, and meloxicam are considered among the most commonly used NSAIDs in many countries [4]. Cardiovascular events were reported with these NSAIDs in several clinical studies. In this study, we provide novel information that diclofenac and ibuprofen altered gene expression and may
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A phenylacetic acid derivative discovered in a high throughp
2021-05-24
A phenylacetic ryanodine derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM (). Compound also inhibited CRTH2 mediated ce
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The on target in vitro pharmacology of
2021-05-24
The on target in vitro pharmacology of 18 was then further explored, first in respect of murine CRTh2 receptor activity (Table 5), where similar levels of activity were found in both a binding and functional assay compared with the human orthologue, consistent with our earlier observations in the su
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The large body of structural knowledge that is
2021-05-24
The large body of structural knowledge that is currently available for CRM1 has contributed to atomic level and mechanistic understanding of many steps in the CRM1 nuclear export cycle. However, structural analysis could still inform on several outstanding questions and guide future discoveries pert
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This work is inspired by the systematic work
2021-05-24
This work is inspired by the systematic work of Coutinho and co-workers, who obtained several very useful experimental data, which will be also used in our work, and applied the CPA equation of state for the modeling of systems relevant to the production of biodiesel [8], [9], [10], [11], [12], [13]
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The classification of CK substrates based on active enzyme
2021-05-24
The classification of CK2 substrates based on active enzyme subunit composition provides a framework for understanding the regulatory function of CK2β subunit. However, few experiments exist that functionally explore such classification [17], [18], [19], [20], [21], [22], [23]; this reflects practic
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phosphocholine mg The second part of this study evaluated th
2021-05-24
The second part of this study evaluated the role of CK1 in the eFABP4 cellular uptake in endothelial cells. By blocking CK1 expression using a specific siRNA, we corroborated that the presence of CK1 was fundamental for FABP4 cellular uptake and internalization in endothelial cells, thus decreased m
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Introduction Angiotensin II Ang II and Endothelin ET are
2021-05-22
Introduction Angiotensin II (Ang II) and Endothelin 1 (ET-1) are potent vasoconstrictive peptides recognized as key players in many cardiovascular diseases [1]. Cardiac hypertrophy, ischemic arrhythmia, and stroke have been associated to an overstimulation of the angiotensin II type 1 (AT1) recepto
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Interest in the PGE EP pathway is increasing given its
2021-05-22
Interest in the PGE2/EP4 pathway is increasing given its diverse capability of regulating central nervous system activity [13]. EP4 has a protective function by reducing cerebral injury and improving functional outcome after stroke [14], and in suppressing GSK2656157 inflammation [15]. The EP4 rece
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Our results demonstrate that pt PGE in addition to its
2021-05-22
Our results demonstrate that 17-pt-PGE2 - in addition to its described effects on EP1 and EP3 receptors - also acts as an EP4 agonist and thereby enhances vascular barrier function. Materials and methods Results Discussion In this study we demonstrate that the purported EP1/EP3 receptor ag
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