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br Conflict of interest br Funding br Introduction Heme
2021-11-08
Conflict of interest Funding Introduction Heme is an essential molecule for cellular metabolism involving oxygen and electron transfer [1]. However, free heme is a potent pro-oxidant that catalyzes the generation of reactive oxygen species (ROS) leading to cellular damage [2]. Heme oxygenas
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The Y H D A variant was resistant to all
2021-11-08
The Y56H/D168A variant was resistant to all tested PIs, and the inhibitor binding mode determined the molecular mechanism of resistance. Prior to the development of grazoprevir, PIs typically contained large heterocyclic P2 moieties that strongly interacted with S2-subsite residues (Ali et al., 2013
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Erythromycin It appears that different agonists for GPR
2021-11-06
It appears that different agonists for GPR55 activate different signalling pathways [25]. GPR55 activation through LPI has been shown to trigger ERK 1/2 phosphorylation 22, 23, 25, 33. Conversely, endogenous cannabinoid compounds AEA and 2-AG have been shown to have no effect on ERK 1/2 signalling 2
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Almorexant In contrast to UDG SMUG exhibits
2021-11-06
In contrast to UDG, SMUG1 exhibits dramatically lower product yield in its excision of U, and this is not dependent on sequence context. Though we cannot rule out that a small amount of the product is derived from a duplex contaminant, our extensive purification techniques limit the amount of contam
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A considerable body of evidence
2021-11-06
A considerable body of evidence suggests that alcohols, volatile anesthetics and inhaled drugs of abuse act at discrete sites on glycine and GABAA receptors, specifically within circumscribed protein pockets (Mascia et al., 2000, Mihic et al., 1997, Beckstead et al., 2000). An amino adenosine 5 trip
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Molecular dynamics studies have proved an effective means of
2021-11-06
Molecular dynamics studies have proved an effective means of characterising transition state pathways between the inward- and outward-facing states, and providing the relative propensity for each state. For example, long-timescale simulations of the membrane-embedded LeuT dimer, totalling ∼21 μs, ha
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Serotonin hydroxytryptamine HT is a monoamine with
2021-11-06
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine with dual functions in the developing and matured brain. 5-HT regulates development of the Oligomycin Complex as a neurotrophic factor and is involved in emotion and cognition as a neurotransmitter in adulthood (Gaspar et al., 2003; Daubert and C
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Developmental studies have reported that some subunits of
2021-11-06
Developmental studies have reported that some subunits of GABAA receptors like α2 and α3 are predominantly expressed during in-utero development, and then substituted for α1 around birth in the rat hippocampus (Brooks-Kayal et al., 2001; Fritschy et al., 1994; Golshani et al., 1997; Kapur and Macdon
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In the intestine ethanol exposure can
2021-11-06
In the intestine, ethanol exposure can change the composition of gut microbiota and promotes the growth of intestinal gram-negative bacteria, which results in the accumulation of endotoxins such as, LPS. Ethanol also impacts the integrity of the gastrointestinal mucosal barrier, increasing intestina
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Malotilate Lenvatinib is an orally available multi targeted
2021-11-06
Lenvatinib is an orally available, multi-targeted tyrosine kinase inhibitor against VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT [11,12]. In a recent phase III trial for patients with previously untreated uHCC (REFLECT study), lenvatinib showed statistical non-inferiority of overall survival compared to
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It should be noted that the current studies were
2021-11-06
It should be noted that the current studies were performed in female rats. Although the oestrous cycle has been shown to modulate inflammatory processes in the periphery, data from our group has demonstrated that the phase of the oestrus cycle does not significantly alter TLR3-mediated neuroinflamma
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The overall response rate to
2021-11-06
The 13% overall response rate to afatinib is comparable to a 19% response rate reported by Peters et al. [20] in a separate retrospective series investigating the use of afatinib in more heavily pretreated patients with HER2-mutant lung adenocarcinomas. Our 13% response rate is also comparable to an
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Though studied less extensively than in cholangiopathies
2021-11-06
Though studied less extensively than in cholangiopathies and fatty liver diseases, the Hh pathway is active in other forms of human liver disease, such as Schistosomiasis[58], [101] and chronic viral hepatitis,[100], [125] as well as in several animal models of liver disease, including drug-induced
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br Conclusions br Introduction G protein coupled receptors
2021-11-05
Conclusions Introduction G protein-coupled receptors (GPRs) share common structural motifs, including seven transmembrane helices, and the ability to activate heterotrimeric G proteins such as Gs, Gi, Gq and G12/13. A variety of GPR cellular functions are mediated by second messengers such as
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A further generally applicable approach for the synthesis of
2021-11-05
A further generally applicable approach for the synthesis of N-linked glycopeptides involves the convergent Lansbury aspartylation of glycosylamines. Here, the detrimental formation of aspartimides during the activation of the side chain aspartate can be prevented through the use of Ser/Thr pseudopr
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