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SCH is a H R receptor
2021-12-17

SCH-497079 is a H3R receptor antagonist introduced by Schering-Plough, without any publicized pharmacological and structural information. A Phase II clinical trial assessment of SCH-497079 on weight has been completed in a multicenter, randomized, parallel-group and placebo-controlled study in obese
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br Conclusions br Acknowledgement br Introduction The macrop
2021-12-17

Conclusions Acknowledgement Introduction The macrophage is an important cell species that plays key roles in innate immune responses and inflammatory reactions through phagocytosis of foreign bodies and secretion of inflammatory mediators such as interleukin (IL)-1, tumor necrosis factor (T
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br Acknowledgements br Introduction The study methods consis
2021-12-17

Acknowledgements Introduction The study methods consisted of the review of articles included in the Pubmed and Medline databases and in the clinicaltrials.gov clinical trials register between 2013 and 2016, and of the preliminary results of therapies presented at international trichology confe
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Our inhibitor studies revealed the presence of a signaling n
2021-12-17

Our inhibitor studies revealed the presence of a signaling network triggered by dicarbonyl stress. Nevertheless, p38-MAPK activation was clearly necessary for NADPH-oxidase mediated production of ROS. This is consistent with data from other groups using different cell culture systems [37], [38], [39
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To verify DNA glycosylase AP lyase activity
2021-12-17

To verify DNA glycosylase/AP lyase activity we have employed a simple and efficient method to investigate based on fluorescein-labeled duplex oligonucleotides read on an automated sequencer (Allgayer et al., 2013, Lopes et al., 2007, Lopes et al., 2008). This approach using purified CpMutY proteins
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pd 0332991 Acarbose and voglibose the classic glucosidase in
2021-12-17

Acarbose and voglibose, the classic α-glucosidase inhibitors, were clinically used to inhibit α-glucosidase activity for the treatment of type 2 diabetes. However, the intake of these drugs may cause some undesirable gastrointestinal side effects and weight gain (Xu et al., 2015). The synthetic drug
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In the present study compared to diabetic control
2021-12-17

In the present study, compared to diabetic control rats, hepatic glucose-6-phosphatase activity was significantly decreased in both SE and METF treated diabetic animals, with the latter producing greater reduction in glucose-6-phosphatase activity. This observation is consistent with the claim of Ta
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Having identified initial leads and further lead optimizatio
2021-12-16

Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic rtks derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl, chloro and CF
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br Introduction Initial studies of
2021-12-16

Introduction Initial studies of cancer metabolism in the early 1920s showed that the cancer phenotype for glucose metabolism is unique, with increased abilities to take up glucose and produce lactate, even under aerobic conditions [1]. This pathway, called aerobic glycolysis or the Warburg effect
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br Concluding remarks Several orphan GPCRs have
2021-12-16

Concluding remarks Several orphan GPCRs have expression profiles that indicate they are worthy of consideration as therapeutic targets. This view can be supported via various transgenic techniques, and it would be interesting to have wide-ranging phenotypic information on GPR35 knockout mice. Bas
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The ability of FFA to elevate intracellular
2021-12-16

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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In our study we evaluated
2021-12-16

In our study we evaluated adenovirus type 5 (Ad5) as a vehicle for delivering Cre recombinase in conditional transgenic mouse based on the Cre-loxP system, in order to achieve GlyT1 gene modulation in a specific thalamic region in the adult animal. GlyT1 is a sodium- and chloride-coupled glycine tra
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Olanzapine has been reported to attenuate insulin secretion
2021-12-16

Olanzapine has been reported to attenuate insulin secretion, cause insulin resistance (Chintoh et al., 2008) and reduce whole body carbohydrate oxidation (Klingerman et al., 2014). However, a blunting of these effects in Gcgr−/− mice would not appear to explain the protection against olanzapine-indu
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It was previously proposed that glucagon acts in the liver
2021-12-16

It was previously proposed that glucagon acts in the liver, in which a signal is produced and relayed to the capmatinib via vagal nerves [8], [36], [37]. The concept that the liver is the primary target site was supported by the studies reporting that the glucagon receptor is localized in the liver
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br NLS and NES Mapping
2021-12-16

NLS and NES Mapping Sequence Comparison of Gli NLSs—NLSs in ZF Domains Alignment of the Gli NLSs of representative metazoan animals suggests that the amino Nutlin 3 residues in the ZF domains are strongly conserved (Figure 4.2, Figure 4.3B). However, the length of the intervening amino acid se
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