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In addition during the preparation of this
2021-09-10

In addition, during the preparation of this manuscript, Oka et al. [7] demonstrated that LPA acts as receptor ligand for GPR35 and that LPA is more potent than KYNA in eliciting a calcium mobilization (EC50: 30nM vs. 39μM for LPA and KYNA, respectively). Other endogenous GPR35 ligands, therefore, mi
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With the administration of OM
2021-09-10

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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br Experimental br Acknowledgments This research was support
2021-09-10

Experimental Acknowledgments This research was supported by the Korea Research Foundation (2013R1A1A2007509). The authors thank to Dr. Moon Ho Son (Dong-A Pharm. Co. Ltd) for hGPR119 agonist activity assay. We also thank to Pharmacal Research Institute and Central Laboratory of Kangwon Nationa
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However even if immunological tests with the
2021-09-10

However, even if immunological tests with the NQ21 peptide are mostly positive [8], it doesn't mean that the structure of the NQ21 peptide is the same as that of the corresponding gp120 region characterized by a long alpha helix. Therefore, the aim of the current work was to check whether the NQ21 p
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Paeonol mg While the S site has been implicated in
2021-09-09

While the S2 site has been implicated in binding, it Paeonol mg is unclear whether the S2 site plays a role in the substrate transport process. Crystal structures have revealed that different drugs and detergents can bind to the S2 site of SERT [8] and LeuT [[13], [14], [15]]. However, there are no
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The functionally crucial arginine within M is
2021-09-09

The functionally crucial arginine within M2 is not encoded by the gluR2 gene, but rather arises within the pre-mRNA by editing of a codon for the neutral glutamine residue25, 26. RNA editing at the Q/R site is specific to GluR2 and is extremely efficient. In neonatal and adult rat brain, almost 100%
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In this study our result suggests that exogenous GR agonist
2021-09-09

In this study, our result suggests that exogenous GR agonist DEX and GR inhibitor RU486 can affect dopaminergic neurotransmitters in the brain. Pituitary adenylate cyclase-activating polypeptide (PACAP), an endogenous neuropeptide, can regulate the synthesis and release of catecholamine. McArthur et
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The ghrelin receptor is expressed in a number
2021-09-09

The ghrelin receptor is expressed in a number of human malignancies including prostatic carcinoma cell lines [18,19] and tissues [20], breast carcinoma tumours and cell lines [21], testicular tumours [22], and malignant ovarian cysts and tumours [23]. In addition, it has an elevated level of express
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Streptomycin sulfate br Presenilins and Wnt catenin signalli
2021-09-09

Presenilins and Wnt/β-catenin signalling Several groups have provided substantial data indicating that PS1 acts as a negative modulator of the transcriptional activity of the β-catenin/Tcf-4 complex (Fig. 4) [120], [121], [122]. β-Catenin is a multifunctional protein that was first described as a
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Optimization of the tetrahydroindazole series
2021-09-09

Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ()
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To obviate the mitogenic FGF
2021-09-09

To obviate the mitogenic FGF19 activity, several engineered FGF19 variants have been generated aiming to maintain the metabolic activity excluding the protumorigenic ones. One variant, M70, that differs from wild-type FGF19 by 5-amino acids deletion at the N-terminus and the substitution of 3-amino
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Data of initial analogs have been shown
2021-09-09

Data of initial analogs (±)-– have been shown in wherein SAR was observed for the intended change of the right-hand side pyridin-3-yl ring of to various other -containing heteroaryl ring (Ar) disposing the ring- at different directions. Based on consistent human and rat FAAH potency as well as int
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br Acknowledgments We thank Drs
2021-09-09

Acknowledgments We thank Drs. Yasuhiro Saito and Mitsuru Futakuchi for helpful discussion. We also thank Drs. Kohei Miyazono and Tadashi Matsuda for cells. This work was supported by Grant-in-Aids for Scientific Research on Innovative Area (16H06373; 16K15273) from MEXT, Japan (to M.H.) and by Pr
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The transcription factor Nrf is a master regulator
2021-09-09

The transcription factor Nrf2 is a master regulator of cytoprotective responses to endogenous and exogenous stresses caused by reactive oxygen species (ROS) and electrophiles [6]. Nrf2 promoter polymorphisms are significantly associated with the development of gastric mucosal inflammation, either in
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There is evidence for an adverse
2021-09-09

There is evidence for an adverse sympatho-stimulatory effect in the medulla oblongata mediated by the α1/β1 isoform, implying a possible benefit of selective α2/β1 activation [19]. While the stimulator BAY 41–2272 increases NO-sensitivity of both isoforms [20], a prevalence of the α1/β1 isoform comp
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