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In conclusion our data demonstrated that montelukast and pra
2019-09-20
In conclusion, our data demonstrated that montelukast and pranlukast non-competitively blocked P2Y signaling in several cell systems, but in a relatively nonsubtype-specific manner. The functional antagonism was especially evident at heterologously expressed P2Y1 and P2Y6 receptors, at which IC50 va
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br Materials and methods br Results
2019-09-20
Materials and methods Results Discussion NB has been shown to induce cancers in many tissues including the kidney, liver, and thyroid, following chronic inhalation in animals (Hsu et al., 2007). The available data indicate that a lager majority of studies on NB evaluate the effects of toxic
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Almost of drugs in the market
2019-09-20
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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br Crystal structure of c FMS
2019-09-20
Crystal structure of c-FMS and binding pattern of CSF-1 and IL-34 c-FMS is a 972 amino acids polypeptides containing transmembrane glycoprotein [19]. It contains all the necessary domains required for tyrosine kinase activity, i.e. 512 amino bromocriptine mesylate N-terminal extracellular segmen
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br Introduction Hematopoietic stem cells
2019-09-20
Introduction Hematopoietic stem Rp-8-Br-PET-cGMPS and and leukemic stem cells (HSCs and LSCs, respectively) both have a capacity of self-renewal. Whereas HSCs give rise to all blood lineages during lifetime hematopoiesis, LSCs are responsible for the initiation and propagation of leukemia, as we
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Related with the studies by Zizza et al described above
2019-09-20
Related with the studies by Zizza et al. described above [66], work by Ward et al. [68] suggested that the C2 domain of cPLA2α, which binds to zwitterionic membranes with high affinity in a Ca2+-dependent manner, has a high membrane remodeling activity, producing dramatic changes in membrane curvatu
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L-Glutathione Reduced br Acknowledgments We thank Jon Clardy
2019-09-19
Acknowledgments We thank Jon Clardy, Juan Manuel Domínguez, José Francisco García Bustos, and the GlaxoSmithKline (GSK) Plasmodium falciparum dihydroorotate dehydrogenase project team for their contributions, helpful advice, and discussions. Introduction Dihydroorotate dehydrogenase (DHODH) i
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The focus of this review
2019-09-19
The focus of this review is on the diacylglycerol acyltransferase (DGAT, EC 2.3.1.20) enzymes, DGAT1 and DGAT2, that catalyze the esterification of a fatty acyl moiety to a DAG molecule to produce TAG. These enzymes commit DAG to being stored as TAG rather than being diverted for the synthesis of ph
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Experiments on the rat model of E coli pyelonephritis perfor
2019-09-19
Experiments on the rat model of E. coli pyelonephritis, performed to investigate the relationship between the acute inflammatory processes and the permanent kidney damage (Brooks et al., 1974), have demonstrated a positive correlation between the degree of free radical-mediated renal injury and the
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Introduction Cytochrome P CYP A is
2019-09-19
Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The pretomanid level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and toxicity. A
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EphB promotes tumor growth by stimulating angiogenesis throu
2019-09-19
EphB4 promotes tumor growth by stimulating angiogenesis through EphrinB2 [18]. However, the distinct and specifically involvement of zd 14 and veins in the tumor angiogenesis of all tumor grades is unclear. Our results indicate that the relation between EphrinB2 and EphB4 stained blood vessels was
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Little information is available regarding the
2019-09-19
Little information is available regarding the expression of the different EP receptor subtypes on human monocytic cells, particularly those that are involved in downregulating cytokine production. The receptors are controlled by the respective genes for each receptor i.e. PTGER1–PTGER4 for EP1–EP4 r
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The majority of serpins inhibit serine proteases but serpins
2019-09-19
The majority of serpins inhibit serine proteases, but serpins that inhibit caspases or papain-like cysteine proteases have also been identified [4], [5]. Inhibitory serpins are ‘suicide’ or ‘single use’ inhibitors that use a unique conformational change to inhibit proteases. This conformational tran
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Based on the above background
2019-09-19
Based on the above background, gliptins may exert natriuretic and diuretic effects as well [[112], [119]]. In accordance with this, Girardi and co-workers have demonstrated a physical interplay between DPP-4 and the NHE3 exchanger in the brush-border epithelium of the proximal renal tubule, suggesti
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br Acknowledgments br Introduction Heterocyclic chemistry ha
2019-09-19
Acknowledgments Introduction Heterocyclic chemistry has become one of the most important fields of research in pharmaceutical industry due to their many fold applications. Amongst all, heterocyclic lipid metabolism containing nitrogen and oxygen have shown most potent biological activities. It
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