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br Materials and methods br Results br Discussion Several
2022-02-16
Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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Starting from the hypothesis that
2022-02-16
Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [
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The replacement of the P butyl urea cap with
2022-02-16
The replacement of the P-butyl urea cap with sulfonamide derived cap had a profound effect on binding. Compound obtained by the replacement of -butyl urea P cap of compound with sulfonamide demonstrated a =34nM, a fifteen folds improvement in potency. Similarly replacement of P-butyl cap in the P cy
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We did however observe that niacin treatment
2022-02-15
We did, however, observe that niacin treatment impaired DC accumulation in skin-draining lymph nodes (Fig. 2). Attenuated adaptive immunity, assessed using a contact hypersensitivity assay (Fig. 4), was observed, as would be expected from impaired DC accumulation in lymph nodes, though other mechani
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Multiple mechanisms have been suggested
2022-02-15
Multiple mechanisms have been suggested by which glucagon can increase energy expenditure although none have been conclusively proven to be responsible. Both enhanced gluconeogenesis and enhanced protein turnover secondary to hyperglucagonaemia have been suggested as the reason for the increased met
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Introduction The Hedgehog Hh signaling
2022-02-15
Introduction The Hedgehog (Hh) signaling pathway regulates embryonic organogenesis, tissue patterning, and cell differentiation (Armas-Lopez et al., 2017, Ingham and McMahon, 2013). Aberrant activation of Hh signaling pathway contributes to tumor formation and development of various cancers includi
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br Discussion br Author Contributions br Alzheimer
2022-02-15
Discussion Author Contributions Alzheimer’s disease (AD) is an age-related, chronically progressive neurodegenerative disorder affecting more than 35million people worldwide and an estimated 5.5million in the US. Current marketed drugs such as acetylcholinesterase inhibitors and the NMDA ant
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A relatively independent review of the
2022-02-15
A relatively independent review of the history of the discovery of GABA (and L-glutamate) as neurotransmitters in the CNS can be found in ‘When and why amino acids?’ in the in 2010 by Kresimir Krnjevic , who spent a post-doc in Canberra in 1956–1958. Introduction The insect RDL GABA receptor is
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Previously we have isolated liver FBPase from
2022-02-15
Previously we have isolated liver FBPase from Pelophylax esculentus (former Rana esculenta, Frost et al., 2006) and characterized its kinetic properties (Dziewulska-Szwajkowska and Dzugaj, 1999) on the contrary the muscle FBPase has never been fully characterized. The primary aim of the present pape
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Expression of p NTR has been linked to
2022-02-15
Expression of p75NTR has been linked to several aspects of aggressive glioma growth, including migration and invasion, by various mechanisms in a large number of elegant studies [6], [7], [26], [27]. Our study adds to this literature by demonstrating specific roles in hypoxic tumor cells and regulat
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However HDACi can also increase the
2022-02-15
However, HDACi can also increase the acetylation of other transcription factors that regulate p65 transcriptional activity. The HDACi-induced activation of p65 can be negated by acetylated STAT1, which can specifically bind to p65 and inhibit its transcriptional activity 81, 82, 83. Interestingly, a
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In this study we demonstrate that
2022-02-15
In this study, we demonstrate that HHcy upregulated the expression of GSNOR in T cells. As a result, GSNOR induced denitrosylation of Akt in Hcy-activated T sorafenib tosylate in vivo and in vitro, which contributed to vascular inflammation and susceptibility to atherosclerosis in GSNOR-/-ApoE-/- m
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br Materials and methods br Results br Discussion
2022-02-14
Materials and methods Results Discussion In this report, we have analyzed the function of an orphan GPCR, and GPR84, using genetically-deficient mice. The expression of GPR84 in the T and PF 1022A in the spleen prompted us to examine the functional responses of these cells under in vitro a
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ICH induced striatal lesion produced a reduction
2022-02-14
ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino p2y receptor transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischem
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In addition this study also
2022-02-14
In addition, this study also showed no obvious increase in apoptosis but obvious increase in necrosis after WZB117 treatment. The possible reason is that apoptosis is an ATP-utilizing process which is an active and programmed form of cell death. In contrast, necrosis is an uncontrolled or pathologic
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