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Despite the rapid development of synthetic ligands the endog
2021-10-01

Despite the rapid development of synthetic ligands, the endogenous ligands of GPR109A, GPR109B and GPR81 remained elusive until recently. This is probably the result of their relatively low potencies and their metabolite character (Table 1). Traditionally, agonists of GPCRs were believed to belong t
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br Introduction Activation of the
2021-10-01

Introduction Activation of the lipid sensing receptor, GPR55, by lysophosphatidyl inositol (LPI) has been well documented, and implicated in endocannabinoid signaling [1]. Intracellular events resulting from GPR55 activation include; enhanced β-arrestin activity, calcium mobilization and ERK1/2 p
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It is well known that O tetradecanoylphorbol acetate TPA is
2021-10-01

It is well known that 12-O-tetradecanoylphorbol-13-acetate (TPA) is a tumor promoting agent of skin carcinogenesis in rodents [12]. TPA stimulates a variety of cellular functions in cancer cells, including cell motile activity [13], [14]. In our recent study, when liver epithelial cells were treated
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Moreover we revealed that alanine and taurine a structural a
2021-10-01

Moreover, we revealed that β-alanine and taurine, a structural analog of β-alanine, have different receptor affinity in the SG neurons of the spinal dorsal horn. Additionally, previous studies indicate that taurine regulates nociceptive information at the spinal cord level, and we have previously de
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However it is unclear whether the parent and
2021-10-01

However, it is unclear whether the parent and transition metal substitution in Keggin-type phosphomolybdic UNC 0631 will reveal the best effects on α-glucosidase. Therefore, the Keggin-type H3PMo12O40 (abbreviated as PMo12) and three transition metal-substituted POMs (Na4PMo11VO40, Na6PMo11FeO40 and
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Compound was obtained as a yellow crystal acetone
2021-10-01

Compound was obtained as a yellow crystal (acetone). And the molecular formula of was established as CHO on the basis of a quasi-molecular ion at / 331.0799 [M+H] (calcd. for 331.0818) in its HR-ESI-MS. Compound showed H and C NMR similar to those of A23187, free acid . However, The H NMR spectrum o
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Studies examining cerebral glucose metabolism in MDD
2021-10-01

Studies examining cerebral glucose metabolism in MDD using 18 F-fluorodeoxyglucose in positron emission tomography (FDG-PET) showed altered regional glucose metabolism in MDD (Dunn et al., 2002, Kennedy et al., 2001, Kimbrell et al., 2002, Saxena et al., 2001). In a recent meta-analysis by Su and co
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Recently several dual GLP GIP
2021-10-01

Recently, several dual GLP-1/GIP receptor agonists have been developed as a treatment of type II diabetes. These peptides can activate both the GLP-1 and the GIP receptor. Such dual receptor agonists are superior compared to single GLP-1 analogues such as liraglutide (Finan et al., 2013). Previously
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Before discovery of their histone demethylase function the J
2021-09-30

Before discovery of their histone demethylase function, the JARID1 isoforms were identified across diverse fields including stem cell biology and congenital disease, as detailed in Box 2. Their observed roles in cancer progression and therapy resistance have led to ongoing pursuit of inhibitors tail
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Based on the aforementioned findings variations
2021-09-30

Based on the aforementioned findings, variations of the imidazole heterocycle present in the endogenous ligand histamine (1) led to 2-(thiazol-2-yl)ethanamine (2-TEA, 2) and later to 2-(3-bromophenyl)histamine or 2-(3-(trifluoromethyl)phenyl)histamine (3) (Fig. 3). Interestingly, 2-TEA demonstrated
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There might be a hedgehog
2021-09-30

There might be a hedgehog dilemma in a broad class of games, but this paper focuses on the case where players only care about : the distance between their attitudes. Here we generalize the main example of a quadratic loss function. So, player ’s payoff is higher when the distance is closer to ’s
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Different SVR rates have been observed when
2021-09-30

Different SVR rates have been observed when comparing GT 1a- and 1b-infected patients receiving BOC or TLP therapy. The response rates in patients infected with GT 1b have generally been more favourable than in those with GT 1a [26]. In our study, persistence mutations were only observed in HCV GT 1
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With the administration of OM
2021-09-30

With the administration of OM3 fatty acids, it has previously been shown that the activation of GPR120 is linked to the secretion and circulating levels of the adipokine adiponectin [123] promoting anti-inflammation (downregulation of NF-κB) and insulin sensitivity [124]. Interestingly, Nrf2 also de
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The differential tissue and ligand dependent signaling descr
2021-09-30

The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va
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Expression and translocation of GLUT are regulated by variou
2021-09-30

Expression and translocation of GLUT4 are regulated by various mechanisms including protein kinase C isoforms (PKCs) and mitogen-activated protein kinase (MAPK) signals [22], [23], but the real mechanism that statins alter expression and function of GLUT4 has not been fully identified. It is general
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