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An AmDH is engineered by mutating two conserved amino acid
2020-10-17

An AmDH is engineered by mutating two conserved amino 486 2 residues in the active site of an amino acid dehydrogenase (AADH). Starting from the leucine dehydrogenase (LeuDH) from Bacillus stearothermophilus, substituting a serine and leucine at the K68 and N261 positions, respectively, resulted in
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TNF a major cytokine that is critical
2020-10-17

TNF-α, a major cytokine that is critical in acute and chronic inflammation, is responsible from chemotaxis, acute phase reactions and endothelial activation (Mahalingam and Karupiah, 1999). Our study showed that TNF-α is increased significantly in the pyelonephritic rats and montelukast displayed an
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THZ1 As previously reported azole class antifungal drugs inh
2020-10-17

As previously reported, azole class antifungal drugs inhibit fungal CYP450 14α-demethylase, as this interrupts the conversion of lanosterol to ergosterol, a component of the fungal cell membrane (Hof, 2006). Furthermore, correlation between fluconazole dose, the extent of hepatic hypertrophy, the le
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van Linden et al developed a comprehensive guide
2020-10-17

van Linden et al. developed a comprehensive guide that describes drug and ligand binding to more than 1200 human and mouse protein kinase domains [77]. Their KLIFS (kinase–ligand interaction fingerprint and structure) directory includes an alignment of 85 potential ligand binding-site residues occur
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To determine the time course of ZD P CPG
2020-10-17

To determine the time course of ZD2767P+CPG2 DNA–DNA interstrand cross-link formation, HT29 and LS174T colorectal tumour transferase were exposed to the drug for 10, 30 or 60 min. The levels of DNA interstrand cross-links in HT29 or LS174T cells did not increase with exposure time, suggesting that Z
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Since the aggregation of neurotoxic forms of A plays
2020-10-16

Since the aggregation of neurotoxic forms of Aβ plays a pivotal role in AD pathogenesis, an approach that using small molecules to bind Aβ monomers and prevent their assembly into cytotoxic oligomers attracts great interest for the development of AD drugs. Therefore, the potential inhibitory activit
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We hypothesize that both IGF dependent kinase activation and
2020-10-16

We hypothesize that both IGF-1-dependent kinase activation and locally synthesized neuroestrogens interactively regulate estrogen receptor activity in neuronal donepezil hydrochloride sale in the absence of exogenously applied estradiol. The Neuro-2A cell line was chosen as the model system for thes
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In rodent models the loss of estrogens through ovariectomy h
2020-10-16

In rodent models, the loss of estrogens through ovariectomy has been shown to promote the development of intracranial aneurysms. Conversely, the administration of an SGI-1027 synthesis receptor beta agonist restores its protective effect, but is abolished with the introduction of a nitric oxide synt
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Estrogen treatment in postmenopausal women
2020-10-16

Estrogen treatment in postmenopausal women requires combination with a progestogen in order to prevent endometrial stimulation. This is not necessary, however, with tibolone as progestogenic activity is associated with its Δ4-metabolite that is formed in the liver, as well as locally in the endomet
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On the opposite side sPLA X
2020-10-16

On the opposite side, sPLA2-X has also been implicated in the pathology of cancer [167,168]. Human sPLA2-X induces lipid droplet formation in Ras-driven MDA-MB-231 triple-negative breast cancer saquinavir synthesis and promotes their survival during nutrient stress. It acts through the products of i
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Omar Farha and coworkers have recently successfully employed
2020-10-16

Omar Farha and coworkers have recently successfully employed metal-organic frameworks (MOFs) to tackle these limitations while retaining the essential characteristics of an immobilization material. MOFs consist of metal ions, or small clusters thereof, coordinated with organic ligands. MOFs are high
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The dihydroxynaphthalene derived substrates a a and a
2020-10-16

The 2,3-dihydroxynaphthalene-derived substrates 18a, 20a and 22a (Table 2) allowed only moderate growth of all members of the panel of microorganisms suggesting that these substrates were inhibitory to some extent. Strong growth of the Gram-negative microorganisms and moderate growth of the Gram-pos
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In addition to vasoconstrictor actions acute effects
2020-10-16

In addition to vasoconstrictor actions (acute effects), ET-1 exerts potent mitogenic actions on vascular smooth muscle cells and cardiac myocytes (chronic effects), hence causing vascular and cardiac hypertrophy [19,24,25]. These effects are mediated via stimulation of either ETA or ETB receptors, a
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C-type natriuretic peptide (1-22) (human, rat, swine) austra
2020-10-16

Enhanced responses to varying concentrations of bronchoconstrictors, such as MCh, and airway obstruction are characteristic of C-type natriuretic peptide (1-22) (human, rat, swine) australia and common to other clinical states, including chronic obstructive pulmonary disease, lung transplantation,
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Abdominal aortic aneurysm AAA is considered a major health c
2020-10-16

Abdominal aortic aneurysm (AAA) is considered a major health concern and is associated with extremely high rates of mortality in case of aortic rupture. The main pathophysiologic mechanisms leading to aortic dilation include the degradation of the extracellular matrix (ECM) components, such as colla
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