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PBI is an agonist of GPR and acts as
2021-10-22
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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HOAt The eradication of agonist activity in
2021-10-22
The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary HOAt as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagonize the stimu
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br Ghrelin Ghrelin was purified from rat stomach about twent
2021-10-22
Ghrelin Ghrelin was purified from rat stomach about twenty years ago as a 28-amino Bestatin hydrochloride australia octanoylated peptide and shown to be the endogenous ligand of the growth hormone (GH) secretagogue receptor (now termed GHSR1a, Howard et al., 1996, Kojima et al., 1999). GHSR1a is
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Polymerisation of HbS initiates the clinical complications o
2021-10-22
Polymerisation of HbS initiates the clinical complications of SCD (Bunn and Forget, 1986). The resulting sequelae are multiple and diverse, and their individual impact on pathogenesis is difficult to elucidate. Early changes include altered red cell membrane permeability (Gibson and Ellory, 2002, Le
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In order to test whether
2021-10-22
In order to test whether the enhanced hyperpolarization in the presence of increasing amounts of extracellular Ca2+ could be due to an ionophore effect of NS309, red cell uptake of 45Ca and partition of 45Ca into a water/n-octanol phase +/−100 μM NS309 were determined. However, no indication of iono
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In an immunohistochemical analysis of gastric
2021-10-22
In an immunohistochemical analysis of 117 gastric cancer samples, reduced Cx43 and E-cadherin expression were shown to contribute to the development of primary gastric cancer; however, increased Cx43 and E-cadherin expression contributed to lymph node metastasis [13]. In primary urothelial Fmoc-Thr(
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In addition to the four classical FGFRs there
2021-10-21
In addition to the four classical FGFRs there is an additional receptor, FGFR like-1 (FGFRL1, also known as FGFR5) (Ornitz and Itoh, 2015, Trueb et al., 2003). FGFRL1 gene was discovered in a cartilage specific cDNA library in 2000 (Trueb, 2011, Trueb et al., 2003) and thereafter it has been found i
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br Inclusion exclusion criteria br Quality assessment
2021-10-21
Inclusion/exclusion criteria Quality assessment All studies included in the qualitative synthesis were evaluated using the Quality Assessment Tool for Quantitative Studies (QATQS), which allows to determine their methodological quality. QATQS assesses 8 sections: selection bias, study design,
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The snapshots in Fig were taken at the end
2021-10-21
The snapshots in Fig. 5 were taken at the end of the first platteau i.e. for 5 Å rmsd or 4 ns time. Thus, we can see that the state of the i-motif affects the mechanism of the G-quadruplex unfolding. At acidic pH the stiff structure of the i-motif does not affect the bottom part (the innermost) of t
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Natural products are a diverse and interesting
2021-10-21
Natural products are a diverse and interesting source for the discovery of new lead structures (Newman and Cragg, 2016). After a successful era of natural product research, many pharmaceutical companies stopped their investment in natural product-driven drug discovery in the 1990s. The reason behind
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Recently accumulated evidence has revealed a close
2021-10-21
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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Because AM had limited efficacy
2021-10-21
Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to
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EZLink NHS-Biotin Kit br Acknowledgments br Introduction The
2021-10-21
Acknowledgments Introduction The incidence of cholangiocarcinoma (CCA), a malignant tumor found in both intra- and extra-hepatic biliary epithelia [1], has been increased worldwide over the past two decades [2]. The prognosis of CCA patients are generally poor, due to the lack of early detecti
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br Conclusion Whilst acknowledging that forensic science cri
2021-10-21
Conclusion Whilst acknowledging that forensic science critically needs strategic investment across every domain [27], forensic science needs to bring both ‘hedgehog’ and ‘fox’ approaches together to address the roots of the major challenges the discipline faces. Addressing these challenges in a w
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Polyunsaturated fatty acid components of brain are more pron
2021-10-21
Polyunsaturated fatty GX-674 components of brain are more prone to oxidative attack, an event called lipid peroxidation. Consistent with previous findings on neurotoxicity [58,59], colistin sulphate increased the level of MDA in the brain of rats. The elevated MDA, a consequence of overwhelmed anti
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