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GPR shares a amino acid
2021-12-27
GPR81 shares a 52% amino Azaserine sequence identity in humans to GPR109A [1], [2], [3]. In addition, GPR81 is localized more specifically to the adipose tissue [3]. In 2008, lactate was discovered to be the endogenous ligand for GPR81 [9], [10]. Plasma lactate levels reach concentrations capable o
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65 0 We have previously established the pharmacokinetic prof
2021-12-27
We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in 65 0 and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The compound CID
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Apart from the different assays used biased agonism could
2021-12-27
Apart from the different assays used, biased agonism could also explain the inconsistent pharmacology of GPR55. Indeed, one study compared the effect of LPIs and Virodhamine in HEK293 Vacuolin-1 stably transfected with human GPR55. They found that the effect of both ligands on intracellular Ca2+ wa
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br Experimental br Acknowledgments This
2021-12-27
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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br Introduction The generic antifibrinolytic
2021-12-27
Introduction The generic antifibrinolytic drug tranexamic folate analogue (TXA) inhibits the protein-protein interaction between plasminogen and fibrin [9]. TXA is frequently used to reduce bleeding in various hemorrhagic conditions, such as during surgical procedures in the heart [19]. However,
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In conclusion we demonstrated that the atypical high basal a
2021-12-27
In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 XMD17-109 results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This network acts as “Cl− lo
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One way to approach this unifying hypothesis will be
2021-12-27
One way to approach this unifying hypothesis will be to compare the effects of the PBR/VDAC ligands on these processes. Recent studies have demonstrated that the three ligands of peripheral-type benzodiazepine receptor, i.e. PK 11195, Ro5-4864 and diazepam reduce membrane transport and conductance i
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More recently Dal Peraro and coworkers carried out
2021-12-24
More recently, Dal Peraro and coworkers [38] carried out 4 μs CG MD simulations of GS with six randomly placed C9915-55 peptides embedded into a synaptic plasma bilayer model. This lipid raft model was constituted by 32 different Ro 31-8220 synthesis and cholesterol (54.74%). In this study, the aut
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In summary two new flexible amine functionalized quinolinium
2021-12-24
In summary, two new flexible amine-functionalized quinolinium derivatives with far-red region emitting were prepared. The shorter-chain fatty amine side chain in the scaffold of was found to be a more promising G-quadruplex DNA fluorescent probe, suggesting the amine side group plays an important r
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Immunohistochemistry using anti FFAR antibodies revealed imm
2021-12-24
Immunohistochemistry using anti-FFAR1 antibodies revealed immunoreactivity for FFAR1 in association with the cell membrane of the hepatocytes (Figure 2). However, the anti-FFAR2 antibody was not suitable for immunohistochemistry under the tested conditions (data not shown). Fatty liver is an import
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The anti platelet functions of ZGR were confirmed by
2021-12-24
The anti-platelet functions of ZGR were confirmed by the mechanistic studies such as the activation of PKC, intracellular Ca2+ mobilization, and the expressions of P-selectin and PAC-1. Further, rivaroxaban prolonged the generation of thrombin and reduced the thrombin burst produced in the propagat
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Two typical properties of Gi o protein coupled receptors
2021-12-24
Two typical properties of Gi/o protein-coupled receptors, namely an increase in 35S-GTPγS binding (Strange, 2010) and an inhibition of exocytotic noradrenaline release (Schlicker and Göthert, 1998), were not shared by H4 receptor activation on cortical membranes (guinea-pig and mouse) and cortical s
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It has been reported that expression
2021-12-24
It has been reported that expression of murine haspin is found only in post-meiotic spermatids and that overexpression of murine haspin in HEK-293 cells leads to reduced cell proliferation. Therefore, it was suggested that haspin functions to bring about BIIE 0246 australia arrest in haploid germ c
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Significan http www apexbt com media diy images wb
2021-12-24
Significant DNA damage was observed in hemolymph of molluscs exposed to raw composite tannery effluent as evident from comet assay images. DNA damage was evaluated by the presence of tail resembling that of comet in single strand DNA. Break in DNA strand was reported in the liver and gill EZ Cap Rea
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Mice with GSTP knock out show increased risk of skin
2021-12-24
Mice with GSTP1 knock out show increased risk of skin cancer when exposed to carcinogens like polycyclic aromatic hydrocarbons [23]. Most of the genetic association studies have focused on GSTP1 c.313G > A variant which results in isoleucine to valine substitution at amino Cy5 Firefly residue numbe
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