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Funding sources This study was funded by European
2020-08-21

Funding sources This study was funded by European Community’s Seventh Framework Programme under grant agreement No. 305662 (Project: Community-based scheduled screening and treatment of malaria in pregnancy for improved maternal and infant health: a cluster-randomized trial ‘COSMIC’). Acknowledg
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Studies of LRRK tagged with green fluorescent protein
2020-08-21

Studies of LRRK2 tagged with green fluorescent protein revealed the presence of monomeric LRRK2 in the Rosiglitazone HCl of living cells, while LRRK2 oligomers were found in the proximity of the plasma membrane, suggesting that both oligomerization status and compartmentalization of LRRK2 defines i
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As previously reported azole class
2020-08-21

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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Resveratrol is a phytoalexin that occurs
2020-08-21

Resveratrol is a phytoalexin that occurs in relatively large amounts in peanut, berries, grapes, and red wine (Soleas et al., 2001). A recent study showed that resveratrol prevents social deficit in an animal model of autism, indicating its potential for possible therapeutic use in children with aut
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br Acknowledgements This work was supported in
2020-08-21

Acknowledgements This work was supported in part by JSPS KAKENHI Grant Number 26292031. Introduction The Cys-loop receptors constitute an important superfamily of ligand-gated ion CGP 57380 (LGICs) and mediate synaptic transmission in both invertebrate and vertebrate nervous systems (Jones e
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Another potential source of variable affinities is inherent
2020-08-21

Another potential source of variable affinities is inherent in the method of RBA determination. While several reports simply use relative IC50 values as RBAs [11], [12], [13], [14], [15], these are only an approximate measure of relative affinity since IC50 varies due to experimental and biological
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Given that dimethylamine substitution was tolerated as
2020-08-21

Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated Cinobufagin 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
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Cantharidin is a natural element extracted
2020-08-21

Cantharidin is a natural element extracted from blister beetles, and has been proven to be effective in cancer [16]. NCTD, the demethylated analog of cantharidin, has been synthesized and been shown to have an equal anti-cancer effect with fewer side effects than cantharidin [39]. It was confirmed
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doxercalciferol Dehydrogenation by a KSTD is
2020-08-20

— 1(2)-Dehydrogenation by a Δ1-KSTD is also a crucial step during doxercalciferol degradation of the steroid core. Several Δ1-KSTDs were shown to be active under either aerobic or anaerobic conditions [27,29,47,50,66]. Furthermore, the last common intermediate of both aerobic and anaerobic steroid
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ApicomplexansApicomplexans are unicellular and spore forming
2020-08-20

ApicomplexansApicomplexans are unicellular and spore-forming obligate intracellular parasites that occupy diverse host niches (Mogi and Kita 2010). They have remodeled mitochondrial carbon and energy metabolism through reductive evolution. The development of novel drugs is now a very serious challen
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br Materials and methods br Results br Discussion In
2020-08-20

Materials and methods Results Discussion In this study, we developed a new CysLT1 and CysLT2 receptors-mediated 7α,25-dihydroxy Cholesterol guinea pig model for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. Unlike human CysLT2 receptors, which are equally stimulated by
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It has been reported that CysLT
2020-08-20

It has been reported that CysLT2 receptors negatively regulate CysLT1 receptor-mediated response in allergic airway inflammation in mice. Knockdown of CysLT2 receptors augmented CysLT1 receptor-mediated mast cell proliferation [31] and eosinophilic airway inflammation induced by antigen challenge in
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Prostaglandins PGs are lipid mediators
2020-08-20

Prostaglandins (PGs) are lipid mediators that exhibit a variety of physiological properties by interacting specific G protein-coupled receptors (GPCRs) [10]. PGD2 is synthesized from PGH2 through two distinct PGD synthases; lipocalin-type PGD synthase (L-PGDS) and hematopoietic PGD synthase (H-PGDS)
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In rodent models the loss of
2020-08-20

In rodent models, the loss of estrogens through ovariectomy has been shown to promote the development of intracranial aneurysms. Conversely, the administration of an Luciferase Reporter Assay Kit receptor beta agonist restores its protective effect, but is abolished with the introduction of a nitri
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Sodium Orthovanadate sale br Effects of estrogen on
2020-08-20

Effects of estrogen on vascular function Atherosclerosis is a chronic inflammatory condition of the vascular wall (Figure 1) that can be converted to an acute clinical event by the induction of plaque rupture or erosion, leading to thrombosis [58]. This perpetuating process is characterized by ph
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