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Another small compound targeting IBAT has been
2021-09-06
Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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br Conflict of interest br Acknowledgments The
2021-09-06
Conflict of interest Acknowledgments The research was funded by the Major Programs of Pharmaceutical research project of Jiangsu Province (Q2018044). Introduction Lipids are important regulators of cell death. In mammalian cells, both apoptotic and non-apoptotic cell death pathways can be
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Another important outcome of reducing hypothalamic HIF in DI
2021-09-06
Another important outcome of reducing hypothalamic HIF in DIO was the increase in gliosis and hypothalamic inflammation. Both experimental and human studies have shown that hypothalamic inflammation plays an important role in obesity by inducing resistance to anorexigenic signals, such as insulin an
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br Materials and methods br Results br Discussion
2021-09-06
Materials and methods Results Discussion Accurate HER2 assessment for patients with invasive breast cancer is crucial to determining which patients may benefit from HER2-targeted therapy. The most recent ASCO/CAP guidelines have again redefined HER2 gene amplification as determined by dual-
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We recently reported that the human derived PancCa cell line
2021-09-06
We recently reported that the human-derived PancCa cell line PANC-1 and the human-derived hepatocellular HepG2 cell line express GPR55 mRNA and protein [21]. In PANC-1 and HepG2 cells, knockdown of GPR55 with specific siRNAs abrogates cellular uptake of Tocrifluor 1117, a selective GPR55 ligand [21]
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br Materials and methods br Results
2021-09-06
Materials and methods Results Discussion According to the literature, zaprinast is a high-affinity agonist of GPR35 (Berlinguer-Palmini et al., 2013, Divorty et al., 2015, Taniguchi et al., 2006, Zhao et al., 2010). GPR35 Bay 11-7085 has been identified within discrete regions of the nervo
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In previous work we showed that benzophenanthridines do not
2021-09-06
In previous work we showed that benzophenanthridines do not affect the surface expression of GlyT1 (Jursky and Baliova, 2011). The results from the surface biotinylation studies reported in Fig. 3 show that the surface expression of the Y370F mutant is not significanly affected by the alkaloids in t
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Acknowledgements This work is partially supported by the Nat
2021-09-06
Acknowledgements This work is partially supported by the Natural Science Foundation of China(81273353), and the National Science & Technology Key Projects of China (2009ZX09103-085). Glyoxalase I (GLO I) is a key enzyme in the pathways leading to glutathione (GSH)-mediated detoxification of meth
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The effects of these steroids
2021-09-03
The effects of these steroids, namely the decrease in the peak and acceleration of desensitization could be observed in IGly activated by 100 μM glycine (concentration close to EC50). However, with an increase in glycine to 500 μM (a concentration close to saturating), the effect of steroids on the
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br Mechanisms of action Ghrelin is
2021-09-03
Mechanisms of action Ghrelin is a 28-amino tetracaine hydrochloride peptide hormone primarily produced in the oxyntic mucosa of stomach, but also in other gastrointestinal tissues [7] (Fig. 1). It acts as the endogenous ligand for the ghrelin receptor [GHS-R1a] and causes the release of growth h
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The modulation of the activity of
2021-09-03
The modulation of the activity of the Gardos channel by the chemokines IL-8 and RANTES was observed in the Duffy-positive but not in the Duffy-negative SSRBCs. This finding is consistent with the previous observation on normal red blood KPT-276 (AARBCs) described by Rivera et al. [10]. Altogether,
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br Acknowledgements br Introduction Galanin shows
2021-09-03
Acknowledgements Introduction Galanin shows widespread distribution in the central nervous system (CNS) and peripheral nervous system (PNS) as well as in the immune, endocrine and endothelial vascular systems (Lang et al., 2007). Galanin controls diverse physiological processes such as arousal
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Also a large number of small molecules are
2021-09-03
Also a large number of small molecules are potent G-quadruplex ligands that exhibit anti-proliferative activity in cells [39,48]. Several small molecules, for example cyclic naphthalene diimide derivative [43], cationic porphyrins [2,[49], [50], [51], [52]] and pentaheteroaryls [53], quinacridines [
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Consistently with the above discoveries it has
2021-09-03
Consistently with the above discoveries, it has been also shown that in cardiomyocytes with shRNA-down-regulated FBP2, mitochondria are more susceptible to depolarisation (Gizak et al., 2012a) and H2O2-induced oxidative stress (Wiśniewski et al., 2017). In Adapalene synthesis overexpressing FBP2 (c
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In the FARM motifs of GGPPSs hydrophobic amino
2021-09-03
In the FARM motifs of GGPPSs, hydrophobic pdk 1 are replaced by aliphatic amino acids, which are more flexible residues and allow the entrance of longer substrates into the pocket (Wang and Ohnuma, 2000). It has been reported that the lepidopteran Manduca sexta CA possesses GGPP synthase (GGPPS) act
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