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GS-9137 br Heme oxygenase inhibitors Historically the first
2022-02-28

Heme oxygenase-1 inhibitors Historically, the first class of competitive HO-1 inhibitors was represented by MPs, heme analogs in which the central iron GS-9137 of heme is exchanged by another element, such as zinc, cobalt, tin, or chromium. These molecules compete with heme for binding to the en
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Following nerve injury Shh expression is upregulated in neur
2022-02-28

Following nerve injury, Shh expression is upregulated in neuronal cell bodies of the facial and sciatic nerves. Additionally, Shh appears to be required for normal regeneration in vivo, and promotes motor neuron survival in vitro (Martinez et al., 2015; Akazawa and Kohsaka, 2007). Based on these obs
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br Background To treat chronic HCV genotype
2022-02-28

Background To treat chronic HCV genotype (GT) 1-infected patients, telaprevir (TLP) or boceprevir (BOC), first generation protease inhibitors (PIs), were used in combination with pegylated-interferon (PEG-IFN) and ribavirin (RBV) triple therapy [1], [2]. The main weaknesses of the first-generatio
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Human GPR hGPR was originally
2022-02-26

Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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In the present study both experimental and
2022-02-26

In the present study, both experimental and theoretical studies were performed to explore the inhibitory mechanisms of indomethacin and its analogues towards GLOI. A remarkable correlation (=0.974) was derived for the four structurally similar NSAIDs and two curcumins between the experimental bindin
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Herein we report the discovery of AM AM maintains
2022-02-26

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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Recent studies revealed that synthetic
2022-02-26

Recent studies revealed that synthetic oligomeric Aβ1-42 decreased GLT-1 expression and promoted mislocalization of GLT-1 from the cell surface of primary astrocytes, leading to glutamate dyshomeostasis in synapses (Abdul et al., 2009, Scimemi et al., 2013). To address the cause for reduction of as
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Up to now the research
2022-02-26

Up to now, the research about the effect of PAs on inhibiting carbohydrase activity in vitro or reducing blood sugar level in vivo was mainly reported in PAs from grape seeds, Lepisanthes alata (Malay cherry) leaves, sorghum, pomegranate, cranberry and persimmon (Banerji and Banerjee, 2016, Barrett
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Recently accumulated evidence has revealed a close link of F
2022-02-26

Recently, accumulated evidence has revealed a close link of FXR to gluconeogenesis. For example, activation of FXR by its agonist GW4064 improved hyperglycemia in db/db mice by repressing gluconeogenesis [15], and FXR agonist CDCA decreased transactivation activity of key gluconeogenic genes by indu
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br Financial support This work was supported by Fondation
2022-02-26

Financial support This work was supported by Fondation pour la Recherche Médicale (Equipe labellisée, DEQ20150331724), Inserm, University of Lille, and Agence Nationale pour la Recherche (ANR-10-LBEX-46 and ANR-10-INBS-08; ProFI project, “Infrastructures Nationales en Biologie et Santé”; “Investi
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Previously we have isolated liver
2022-02-26

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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Data are expressed as means SE
2022-02-26

Data are expressed as means±SE. Statistical significance was determined by the Student's -test or ANOVA with post hoc Bonferroni test. A value of FPPS in the paclitaxel-induced apoptotic cell death of human glioblastoma U87MG cells, we established stable transfectants of U87MG Chaetocin expressing
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The ETB receptor has been shown to
2022-02-26

The ETB receptor has been shown to decrease sodium transport in the renal medullary collecting duct and medullary thick ascending limb of Henle10, 11, 12, 13, 18. However, both inhibitory and stimulatory effects of endothelin have been reported in the proximal tubule16, 47, 48, 49. In the rat, endot
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br Conclusion Our data allow pharmacological
2022-02-26

Conclusion Our data allow pharmacological discrimination of diverse of H3 Fmoc-Thr(tBu)-OH antagonists that can be linked to their differential efficacy in preclinical and clinical disease settings (Fig. 6). Moreover, we identify the sigma-1 receptor as a common “off target” for H3 antagonists, a
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br Introduction The role of histamine in allergic responses
2022-02-26

Introduction The role of histamine in allergic responses, anaphylaxis, and gastric Biotin-azide secretion has been well described in both human and veterinary medicine. New roles for histamine and its receptors, however, have been elucidated over the last two decades (Smuda and Bryce, 2011), and
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