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As well as the above studies Meier and
2021-09-08
As well as the above studies, Meier and coworkers used TUG-891, alongside omega-3 fatty acids, to show a potential role for FFA4 in inhibiting proliferation of DU145 prostate cancer cells [68]. Given that these cells express both FFA4 and FFA1 and the current view that TUG-891 may not be sufficientl
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Niacin nicotinic acid is widely used
2021-09-08
Niacin (nicotinic acid) is widely used to regulate abnormalities in plasma lipid and lipoprotein metabolism, as evidenced by its potential for reducing atherosclerotic cardiovascular disease risks (Guyton, 1998), due to its ability to reduce circulating triglycerides and apolipoprotein-B containing
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br Discussion The pattern of activity exhibited
2021-09-08
Discussion The pattern of activity exhibited by SSR 504734 and Lu AA21279 in the MEST test was very similar. Both compounds were inactive at the lowest dose (3.0mg/kg), but exhibited robust increases (∼150%) at 10mg/kg followed by a maximal detectable response at 30mg/kg. Based on the magnitude o
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In summary we discovered azaindole substituted hydroxypyrido
2021-09-08
In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that b
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Fig A demonstrates the body weight gain
2021-09-08
Fig. 2A demonstrates the body weight gain of the pregestational females. High-fat diet in wild-type mice increased body weight in 2 weeks and sustained this increase over 8 weeks. A similar effect was noted in glut3 mice in response to a high-fat diet. Fig. 2B depicts fat and muscle mass as assessed
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A number of models have
2021-09-08
A number of models have been proposed in order to explain the mechanisms of protein transport through nuclear pore complexes. One theory is that the transport is mediated by specific peptide signals known as NLSs. The classical NLSs are short sequences containing a high proportion of the positively
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In the liver ghrelin has opposite effects to insulin
2021-09-08
In the liver, ghrelin has opposite effects to insulin on the expression of the enzyme PEPCK, thereby promoting gluconeogenesis and also causing a decrease in glucose uptake and fatty KU-0063794 oxidation (Rigault et al., 2007). Ghrelin also stimulates hepatic lipogenesis de novo in a GH-independent
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Inhibitors of the G rdos effect
2021-09-08
Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic
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br Involvement of gap junctions and Panx in spinal
2021-09-08
Involvement of gap junctions and Panx1 in spinal cord processing of pain information Several studies indicated that GJs in the CNS contribute to pain. A common finding in such studies is that intrathecal administration of GJ blocker attenuates pain behavior. For example, intrathecal CBX attenuat
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br Introduction The fibroblast growth
2021-09-08
Introduction The fibroblast growth factor receptor (FGFR) pathway is an important oncogenic driver in malignant cancer. It controls cellular processes such as cell proliferation, differentiation, migration, Caspase-9 Colorimetric Assay Kit synthesis progression, metabolism, and survival. In non–s
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Till date the first line treatment of T DM
2021-09-08
Till date, the first line treatment of T2DM is oral metformin followed by oral sulfonylureas, dipeptidyl peptidase-IV-inhibitors, and TZDs. As the disease progresses, injectable glucagon-like peptide-I analogues or ultimately insulin become necessary to maintain glycaemic control. Despite the establ
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Through experimental models and clinical experiments those f
2021-09-08
Through experimental models and clinical experiments, those four drugs above can shown efficacy-enhancing and toxicity-reducing effects after compatibility. Our preclinical studies showed that XFC has a definite effect on relieving joint symptoms in RA patients. XFC can improve joint pain, swelling,
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A large body of literature
2021-09-07
A large body of literature have reported that various cellular pathways are dysregulated in NPC [19]. Among these pathways, Akt is frequently hyperactivated in NPC and regulates diverse cellular processes including tumor cell growth, proliferation, metabolism, survival and invasion, as well as angio
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In the CNS histamine is known to regulate
2021-09-07
In the CNS, Paeonol is known to regulate sleep and wakefulness, learning and memory, feeding, and energy. Here, we address its actions in relation to CNS disorders, and emphasize potential clinical applications of histamine receptor ligands (Table 1). In addition, as the effect of histamine on neur
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Oxaprozin receptor br Hippo Signaling in Autoimmunity An imb
2021-09-07
Hippo Signaling in Autoimmunity An imbalance of T cell subsets, such as immunosuppressive regulatory T Oxaprozin receptor (Treg) and inflammatory TH17, has a key role in autoimmune diseases. Recently, investigations found that TAZ but not YAP enhances TH17 differentiation but attenuates Treg dif
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