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br Introduction Activation of the
2022-02-22
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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The pharmacokinetics of was obtained
2022-02-22
The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indi
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For some agonists these stable GPR responses were
2022-02-22
For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer
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ion channel To determine the functional consequences
2022-02-22
To determine the functional consequences of HIV gp120 binding to vaginal epithelial cells, an annotation clustering of the differentially expressed genes was performed. The top enriched biological processes included an inflammatory immune response, defense response and the pathways included the SODD
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The DNA cleavage activity assay in the
2022-02-22
The DNA cleavage activity assay in the present study also demonstrated the DNA glycosylase activities of SMUG1, NEIL1, TDG, and NTHL1 for 5OHU paired with A. While our findings on the activities of SMUG1 and NEIL1 were consistent with the results reported from previous studies [25], [50], the activi
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Finally the results in this article indicate that atomistic
2022-02-22
Finally, the results in this article indicate that atomistic MD in conjunction with computational electrophysiology and ion-permeation simulations provide a useful tool for the functional annotation of ion-channel structures. In particular, they exemplify how MD simulations in native lipid membranes
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Introduction Histamine was generally accepted as a neurotran
2022-02-22
Introduction Histamine was generally accepted as a neurotransmitter in 1984, when histamine was first identified to be located in tuberomamillary nucleus (TM) of the brain (Watanabe et al., 1984). In mammals, histaminergic neurons play an important role in regulating multiple physiological activiti
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br Materials animals and methods br Results br
2022-02-22
Materials, animals and methods Results Discussion This study presents mice with a missense point mutation in R258 of FFAR1 that has functional consequences. Firstly, in islets of Ffar1R258W/R258W mice, both the physiological agonist palmitate and the synthetic agonist TUG-469 were unable to
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Epidemiological studies revealed that vitamin D deficiency w
2022-02-22
Epidemiological studies revealed that vitamin D deficiency was associated with a wide range of neuropsychiatric disorders and neurodegenerative diseases, in particular, Alzheimer's and Parkinson's disease (Annweiler et al., 2013; Knekt et al., 2010), dementia and cognitive function impairment (Balio
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br Acknowledgements This work was supported by the
2022-02-22
Acknowledgements This work was supported by the Science and Technology Department of Hubei Province (No.2016CFB368) and the National Natural Science Foundation of China (No. 81201053). Introduction L-Glutamate (glutamate) is the most important excitatory neurotransmitter of the central nervou
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However it is unclear whether the parent and
2022-02-22
However, it is unclear whether the parent and transition metal substitution in Keggin-type phosphomolybdic dapivirine will reveal the best effects on α-glucosidase. Therefore, the Keggin-type H3PMo12O40 (abbreviated as PMo12) and three transition metal-substituted POMs (Na4PMo11VO40, Na6PMo11FeO40
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Recently unimolecular multi functional peptides that combine
2022-02-22
Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with PH-797804 and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control and weight
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br Preclinical development of GIP agonists Since the action
2022-02-22
Preclinical development of GIP agonists Since the action of DPP IV is not limited to GIP, the most specific pharmacological approach for GIP would be modification at the N-terminus to disrupt DPP IV-mediated degradation. Indeed, it has been shown that GIP analogues with N-terminal modifications a
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Discrepancies in the reported results
2022-02-22
Discrepancies in the reported results and conclusions from different groups regarding studies in ghrelin−/− and ghsr−/− mice are likely explained by the mixed background of the mutant mice used in the different studies [35]; although in the case of mice exposed to HFD, exposure to a HFD immediately
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br During cardiac ischaemia a decrease in GJ coupling is
2022-02-22
During cardiac ischaemia, a decrease in GJ coupling is observed, which results in slower conduction of electrical impulses and a higher risk of arrhythmias.[13], [20] In Huntington’s disease an increase in the Pregnenolone Carbonitrile of 5 Cxs was observed in the astrocytes in the brain, suggest
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