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Poziotinib br Discussion In our study the prevalence of seve
2022-02-05

Discussion In our study the prevalence of severe periodontitis in patients with HIV infection was 66%, almost twice as high as in uninfected controls. Our results are in line with the prevalence of severe periodontitis found in HIV-infected patients in London, United Kingdom in the pre-cART era:
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Drosophila is a well established model to
2022-02-05

Drosophila is a well-established model to investigate the molecular and cellular defects underlying human neurodevelopmental disorders (Oortveld et al., 2013, van der Voet et al., 2014). Here, we establish Drosophila as a model for understanding the mechanisms linking mutations in KDM5 family protei
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Although some PAHs that are human carcinogens have
2022-02-05

Although some PAHs that are human carcinogens have been found in the sugarcane soot (Zamperlini et al., 1997), there are no data about cancer incidence among sugarcane workers. To the best of our knowledge, this is the first report of an evaluation of internal exposure, comparing the harvesting (whe
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Introduction The brain contains abundant fatty acids which s
2022-02-04

Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial cells, suggesting that fatty acids play a crucial role in dev
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GOAT belongs to the super family of membrane bound O
2022-02-03

GOAT belongs to the super family of membrane-bound O-acyltransferases (MBOATs). It is encoded by the gene MBOAT4 in human. The protein GOAT is highly conserved from zebrafish to human (Yanagi et al., 2018). GOAT is ubiquitously expressed with abundant expression in the stomach and intestine (Sakata
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br Electron crystallographic structures of connexins The str
2022-02-03

Electron crystallographic structures of connexins The structures of gap junctions are good targets for electron microscopy because they exhibit the characteristic features of self-assembly. Early studies examined the three-dimensional (3D) structures of native gap junction PLX7904 receptor from
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Compounds and were evaluated for their pharmacokinetic
2022-02-03

Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure wa
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It is important to note that histamine H
2022-02-01

It is important to note that histamine H1 and H2 receptors are coupled to different G proteins and that their crossinterference induced by histamine H1 and H2 receptor inverse agonists depends on the cointernalization mechanism. To date, histamine H1 and H2 receptor inverse agonist have shown to int
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The ability of FFA to elevate intracellular levels of
2022-02-01

The ability of FFA4 to elevate intracellular levels of Ca2+5, 38, 39, 40 provided early predictions of a key role of the phosphoinositidase C-linked G proteins Gq and/or G11 in transduction of signals from this receptor, while later studies that examined production of inositol phosphates [41] provid
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The calculations for the R substrate showed that
2022-02-01

The calculations for the R substrate showed that, like the S substrate, the coordination shell of the Zn BMS265246 is more symmetric than in the HIC-SG crystal structure. This symmetry indicates that the enzyme could use the same reaction mechanisms as for the S substrate, but with exchanged roles
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In this study we also
2022-02-01

In this study, we also profiled the expression of the transporters in wild-type RBL-2H3 cells, RBL-2H3 Sc98 cells, and rat peritoneal mast cells. OCT1 and PMAT were expressed at high levels in both RBL-2H3 Sc98 and RBL-2H3 cells. However, OCT2 and OCT3 were weakly or least detected in RBL-2H3 Sc98 c
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Herein we report the discovery of AM AM maintains the
2022-02-01

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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br Redox regulation in the
2022-02-01

Redox regulation in the brain Reactive oxygen species are generated in 2-deoxy-d-glucose by the mitochondrial respiratory chain, which occurs on the inner mitochondrial membrane (Murphy, 2009, Jensen, 1966, Dickinson and Chang, 2011). Interestingly, although most cancer cells are thought to prim
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In a series of experiments the clotrimazole concentration wa
2022-01-31

In a series of experiments, the clotrimazole concentration was varied and the NSVDC channel conductances were calculated from Eq. (1) to obtain the dose-response relation (Fig. 3). The data were fitted to the Michaelis–Menten-type activation curve (Eq. (3)) and gave an EC50 value of 14 μM and a dose
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br During cardiac ischaemia a decrease in GJ coupling
2022-01-31

During cardiac ischaemia, a decrease in GJ coupling is observed, which results in slower conduction of electrical impulses and a higher risk of arrhythmias.[13], [20] In Huntington’s disease an increase in the duvelisib of 5 Cxs was observed in the astrocytes in the brain, suggesting an adaptive
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