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Fatty acids are also known to activate
2021-11-11
Fatty acids are also known to activate G-protein coupled receptors (GPCRs). LCFAs activate the GPCRs for free fatty MK2206 (FFA)1 and FFA4 (Briscoe et al., 2003; Hirasawa et al., 2005), whereas SCFAs activate FFA2 and FFA3 receptors, which are expressed in bovine neutrophils (Alarcon et al., 2018;
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Considering together the conformational docking and SAR resu
2021-11-11
Considering together the conformational, docking and SAR results of this and of previously published papers, a three points pharmacophore model can be developed considering the indispensable residues of SRSRY derived antagonists, namely Arg89, Arg91 and Tyr92. This model is shown in Fig. 10, and req
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br Histamine H R The cloning of
2021-11-11
Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other abk receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et al., 2009, Liu et al
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br Introduction Hexokinase HK is an enzyme that
2021-11-11
Introduction Hexokinase (HK) is an enzyme that catalyses the transfer of phosphate from ATP to glucose in the first step of glucose metabolism (Wilson, 1995, Wilson, 2003). In mammalian, HK has four important isozymes which are designated as HK1, HK2, HK3 and HK4 (Wilson, 1995, Wilson, 2003). HK1
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Ultimately the change of maturation ratio
2021-11-11
Ultimately, the change of maturation ratio of the Leydig cell caused reducing of INSL3 expression undoubtedly. INSL3 (insulin-like 3) is a hormone produced mainly in gonadal tissues. It was discovered to participate in development of urogenital tract. The mutations of this gene is one cause of crypt
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It is important to note
2021-11-10
It is important to note that the GC-C expression is retained in colon tumours, and therefore GC-C expression can be used as a marker to diagnose metastatic colon cancer [42]. However, expression of uroguanylin and guanylin is often lost in colorectal cancer progression [43]. Therefore, the anti-prol
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CGS 35066 Generally replacement of the aryl group was
2021-11-10
Generally, replacement of the aryl group was well tolerated, with tetrahydropyran () and hydroxyl () functionality providing potency equivalent to and . These substitutions had no effect on selectivity versus GlyT2 and taurine transporter (TauT)—no activity was observed at micromolar concentrations
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Trypanosomatid GLO enzymes are monomeric and contain
2021-11-10
Trypanosomatid GLO2 enzymes are monomeric and contain a zinc–iron binuclear metal center (Irsch and Krauth-Siegel, 2004, Silva et al., 2008), similar to all other glyoxalases II. As mentioned, in T. brucei there are two GLO2 genes but only one encodes an enzyme with glyoxalase II activity (Irsch and
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A considerable body of evidence suggests that alcohols
2021-11-10
A considerable body of evidence suggests that alcohols, volatile anesthetics and inhaled drugs of abuse act at discrete sites on glycine and GABAA receptors, specifically within circumscribed protein pockets (Mascia et al., 2000, Mihic et al., 1997, Beckstead et al., 2000). An amino Pam3CSK4 sale r
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Glucagon was described as an insulin secretagogue as early a
2021-11-10
Glucagon was described as an insulin secretagogue as early as 1965 (Samols et al., 1965). Our studies extend these findings by demonstrating that this is a direct effect mediated by distinct receptors in the mouse pancreas. Previous experiments on isolated β peptide yy clearly show that glucagon is
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FFAs concentration response curves for increasing intracellu
2021-11-10
FFAs concentration–response curves for increasing intracellular calcium and receptor phosphorylation showed a difference of ≈1 order of magnitude indicating a relatively large receptor reserve, which is expected for a transfected model, and that high receptor occupancy is necessary to induce recepto
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It is noted that knee
2021-11-10
It is noted that knee swelling was milder and the intensity of IL-4 staining (MFI) in the vehicle-treated group was lower in the second (Fig. 7a and d) than the first (Figs. 1a and 3f) AIA experiment. The variation in joint swelling between the two studies is most likely due to the models being perf
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Erythropoiesis involves the proliferation and differentiatio
2021-11-10
Erythropoiesis involves the proliferation and differentiation of hematopoietic stem NPE-caged-proton to mature RBCs. This process is a tightly-regulated to adjust rates of RBC production based on physiologic need. Fas-mediated apoptosis is one mechanism that controls erythropoiesis. The role of Fas
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3-Chlorotyrosine receptor Increasing trans epithelial transp
2021-11-10
Increasing trans-epithelial transport efficiency is another area where different strategies are being developed for overcoming transcytosis. Enhancing the affinity for the basal membrane and weakening apical exocytosis through the optimisation of surface hydrophobicity have been demonstrated [79]. S
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Accumulating evidence suggests that the NGF family of neurot
2021-11-10
Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, CHC derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [37]. BDNF knockout mice de
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