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The H R antagonist cimetidine Tagamet became the
2022-05-30
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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The comparatively low number of H R agonists is
2022-05-30
The comparatively low number of H1R agonists is contrasted by the high number of diverse H1R antagonists. Based on pharmacological classification, they are grouped into different generations by considering their target as well as side effects profile. The first generation “antihistamines” consist of
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The electroconductive or electrocatalytic properties of cond
2022-05-30
The electroconductive or electrocatalytic properties of conductive moieties including polymers in combination with carbon or metal-based nanomaterials have also been explored. For example, Dong et al. (2017) developed a portable electrochemical immunosensor by creating a film of Prussian blue chitos
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Introduction Hepatocellular carcinoma HCC is the fifth most
2022-05-30
Introduction Hepatocellular carcinoma (HCC) is the fifth most lethal malignant tumor worldwide and is the second leading cause of cancer-related death [1]. For HCC patients, Paprotrain virus (HBV) infection is the important causative risk factor in Asia-Pacific regions [[2], [3], [4]]. In China, m
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The isoenzyme hGSTP is an attractive drug
2022-05-30
The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t
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Increasing number of experimental data reveal that both ROS
2022-05-30
Increasing number of experimental data reveal that both ROS and RNS are multifunctional molecules playing a substantial role in plant physiology and particularly in seed biology (Bailly et al., 2008; Šírová et al., 2011; Yu et al., 2014). Dual function of RNS can be described by the model of “nitros
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NP118809 Various inhibitors have been developed to target mo
2022-05-30
Various inhibitors have been developed to target molecules present in these pathways. They include both man-made monoclonal NP118809 as well as small molecule membrane permeable inhibitors that often target kinases or phosphatases [5], [338], [348], [364]. In summary, these pathways are frequently
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The diseases of ocular surface and the cornea are very
2022-05-30
The diseases of ocular surface and the cornea are very common in ophthalmological practice and as a result there is a continuous, need for novel therapeutic options. Here, we demonstrated a corneal distribution of GPR35, a potential molecular target for new drugs (; ). The search for the expression
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Excessive adiposity is also a
2022-05-30
Excessive adiposity is also a key pathogenic factor in the development of CVD. Through reductions in bodyweight, GPR120 agonism is therefore also implicated as a potential therapy for obesity and heart and vessel disease. In addition to weight loss, when compared with their wild-type littermates, GP
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The importance of FXR FGF signaling in BA
2022-05-30
The importance of FXR-FGF15/19 signaling in BA homeostasis is illustrated by various BA malabsorption syndromes. Clinically, BA malabsorption causes diarrhea due to high BA concentrations in the colon that lead to secretion of water and electrolytes and stimulation of propulsive contractions [36]. P
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br Regulation of Glu transporters The pivotal role
2022-05-30
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino Rapalink-1 calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcript
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PRL-3 Inhibitor In this study we describe the expression of
2022-05-27
In this study, we describe the expression of galr2a and galr2b in zebrafish embryos using whole-mount in situ RNA hybridization. To further analyze the distribution of GALR2b and its interactions with galanin, we generated Tg(galr2b:egfp) zebrafish, which express EGFP under the control of a galr2b p
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br Results br Discussion Glucose homeostasis is regulated by
2022-05-27
Results Discussion Glucose homeostasis is regulated by a complex and intricate signaling network involving multiple organs. The BA nuclear receptor FXR is integrated into this regulatory network and participates in glucose handling and metabolism. Intestinal FXR favors glucose Oxaprozin sale
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Binding of FGFs to FGFRs
2022-05-27
Binding of FGFs to FGFRs leads to receptor dimerization, resulting in the transphosphorylation of a tyrosine in the activation loop of the kinase domain. Subsequently, the activated FGFRs phosphorylate their intracellular receptor substrates, particularly FGFR substrate 2 (FRS2) and phospholipase Cγ
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Data are expressed as means SE Statistical significance was
2022-05-27
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 angiotensin ii causes expressing human FPPS. Western blot analysis showed a clear band, which indicated the overexpression of FPPS, in U87MG cells (A, in
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