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The H R antagonist cimetidine Tagamet became the first billi
2021-10-03
The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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br Conflict of interest br Acknowledgements
2021-10-03
Conflict of interest Acknowledgements A Class of Unconventional, Dimerization-Activated GTPases GTP-binding proteins, or GTPases, are a superfamily of proteins that regulate numerous cellular pathways 1, 2, 3, 4. Pioneering work on the extended Ras subfamily of GTPases, exemplified by Ras,
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br Materials and methods br Results br Discussion
2021-10-02
Materials and methods Results Discussion Reduced glutathione is considered to be one of the important regulators of REDOX balance in the biological system. The cellular concentration of 4-HNE under physiological conditions ranges from 0.1 to 3μM and has no detrimental effect in the biologic
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The GPR receptor is also
2021-10-02
The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Also
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br Materials and methods br Results
2021-10-02
Materials and methods Results and discussion Conflict of interest Introduction In the presence of continuous and excessive levels of nutrients, adipocytes become hypertrophic and release several pro-inflammatory adipocytokines such as interleukin-6 (IL-6), monocyte chemoattractant protei
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Acknowledgements br Introduction The neurotransmitter glycin
2021-10-02
Acknowledgements Introduction The neurotransmitter glycine acts through two receptors: a strychnine-sensitive glycine receptor (GlyA) and a strychnine-insensitive glycine receptor (GlyB). GlyA is localized to the neuronal membrane post-synaptic to inhibitory glycinergic neurons, whereas GlyB is
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br Results and discussion br Conclusion
2021-10-02
Results and discussion Conclusion In conclusion, we designed and synthesized a novel series of thiosemicarbazide-1,2,3-triazole hybrids 10a-o. Further, α-glucosidase inhibitory activity of the synthesized compounds 10a-o was evaluated. The obtained results showed that all the synthesized thios
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Cortisol targets many organs and tissues and has certain eff
2021-10-02
Cortisol targets many organs and tissues and has certain effects on metabolism, including promoting glycolysis. It can cross the blood NVP-AEE788 barrier and act centrally to regulate HPA axis activity by activating negative feedback mechanisms effectively, cortisol inhibits its own production (Fai
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br Conclusion br Conflict of Interest JJH
2021-10-02
Conclusion Conflict-of-Interest JJH has collaborated with several different pharmaceutical companies during the last 30 years; is currently receiving speaker honoraria from NovoNordisk and MSD and is on advisory boards for NovoNordisk. The author is currently supported by an independent grant
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A model substance often used
2021-10-02
A model substance often used in the studies of oxidative processes in erythrocytes is tert-butyl hydroperoxide (t-BHP), which, being lipophilic, passes easily across the erythrocyte membrane [9]. In erythrocytes treated with t-BHP (0.1–3mM) for less than 1h, a dramatic decline in the reduced glutath
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As with the GSIs there are again
2021-10-02
As with the GSIs, there are again major concerns that GSM therapy in patients with symptomatic AD is almost certain to fail, unless the compound has additional mechanism of action not linked to Aβ that prove to beneficial [52]. Although Aβ1–42 or other longer Aβ peptides are critical for initiating
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Sumoylation of transcription factors has been generally link
2021-10-01
Sumoylation of transcription factors has been generally linked to transcriptional repression and, in a few cases, to transcriptional activation [60] Accumulating evidence implies that corepressor complex subunits, including CoREST, CtBP, Daxx, NCoR1, SMRT and histone deacetylase complexes (HDACs), p
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The molecular mechanisms underlying VSMC ETB receptor
2021-10-01
The molecular mechanisms underlying VSMC ETB receptor upregulation have been studied after 24–48h organ culture in both coronary and cerebral arteries. The increased expression of contractile ETB receptor at these time points has been shown to depend on transcriptional mechanisms and PKC and the ext
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Our previous work demonstrated that KDM regulates cellular
2021-10-01
Our previous work demonstrated that KDM5 regulates cellular oxidative stress in Drosophila (Liu et al., 2014, Liu and Secombe, 2015). It is known that gut epithelial BMS 753 receptor contacted by enteric commensal bacteria generate reactive oxygen species in response to microbial signals (Jones and
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According to previous methods several mobile phase compositi
2021-10-01
According to previous methods, several mobile phase compositions and gradient programmes were assayed to get the best resolved peaks for HA and MHA [12], [13], [24]. Considering the slightly structural differences of the analytes, a mobile phase consisting in two eluents of different polarity and pH
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