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Apart from the different assays
2022-03-03
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 GANT 58 stably transfected with human GPR55. They found that the effect of both ligands on intracellular Ca2+ was bl
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br Conflict of interest statement br Acknowledgments The aut
2022-03-03
Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). GPR35 is an orphan G protein-coupled receptor (GPCR) implicat
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We started our investigation by evaluating the impact of cha
2022-03-03
We started our investigation by evaluating the impact of changes to the piperidine moiety of (). As demonstrated with morpholine and piperazine , attenuation of nitrogen basicity resulted in complete loss of activity, suggesting that a basic heterocyclic nitrogen is important for potent inhibition
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br Acknowledgements This work was supported by
2022-03-03
Acknowledgements This work was supported by grants from la Ligue Nationale Française Contre le Cancer « Equipe LNCC 2016 » and Electricité de France RB 2016-17 (to M.S.), NU ORAU (http://www.nu.edu.kz) and Ministry of Education and Science of the Republic of Kazakhstan, program 0115RK03029 (to B.
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br Introduction Given the growing acceptance of ergothionein
2022-03-03
Introduction Given the growing acceptance of ergothioneine (ET) as a biologically important agent with potential therapeutic applications [[1], [2], [3], [4]] it is increasingly important to clearly establish the role of the organic cation transporter (novel) type 1 (OCTN1). OCTN1 was discovered
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In order to consolidate our genetic
2022-03-03
In order to consolidate our genetic funding, we performed several in silico analysis regarding the p.R85W mutation. The high conservation of R85 residue in all species suggests that it has an important role in glucokinase function. Pathogenic effect of the p.R85W is supported by in silico prediction
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br Ghrelin and energy balance To characterize
2022-03-02
Ghrelin and Measures balance To characterize the physiological role of ghrelin in energy homeostasis, ghsr−/− and ghrelin−/− mice were generated [33], [36], [41], [47]. Although ghrelin regulates the amplitude of episodic GH release, ghsr−/− mice were not dwarfs, and in fact appear identical to
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In summary the SAR of a series of phenylpropanoic acid
2022-03-02
In summary, the SAR of a series of phenylpropanoic acid-free fatty AZ20 synthesis receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust
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Studies have revealed that ferroptosis is
2022-03-02
Studies have revealed that ferroptosis is non-apoptotic and peroxidation-driven form of cell death that requires abundant and accessible cellular Fe2+, and thus, the balance of Fe2+ metabolism is of great significance in regulating the process of ferroptosis (Cao and Dixon, 2016; Xie et al., 2016; Y
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br Acknowledgements This work was in
2022-03-02
Acknowledgements This work was in part supported by the FöFoLe program by Ludwig-Maximilians-Universität München (to T.S.), the Deutsche Forschungsgemeinschaft (DFG) CO 291/5-2, the Human Frontier Science Program (HFSP) RGP0013, the Helmholtz Validation Funds (Helmholtz Association of German Rese
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Finally the optimized leads and were tested in rat
2022-03-02
Finally, the optimized leads (−)- and (−)- were tested in rat model of CIPN (3 and 30 mg/kg, po, qd, administered for 7 days) and the results have been shown in . Under acute set up, after single oral administration at 30 mg/kg, both the compounds exerted significant improvement of the NP condition
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beta amyloid The first phase of insulin secretion is
2022-03-02
The first phase of insulin secretion is due to calcium signaling because of glucose sensing, increased cytoplasmic ATP levels, cellular depolarization, calcium influx and activation of calcium sensing molecules that eventually causes the fusion of the insulin granules to plasma membrane (exocytosis)
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To validate the effects of
2022-03-02
To validate the effects of the G9a HMT inhibitors on HMEC-1 L-745,870 trihydrochloride synthesis and transcriptional responses we generated knockdown cells for G9a using an shRNA approach. Upon transduction of HMEC-1 and doxycycline activation of the shRNA, both G9a HMT mRNA and protein expression w
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Here we dissect X chromosome dosage compensation
2022-03-02
Here, we dissect X chromosome dosage compensation (DC) in C. elegans to determine the effect of chromatin modifications on higher-order chromosome structure during long-range gene regulation. DC is exemplary because it controls hundreds of genes simultaneously, it distinguishes X chromosomes from a
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Conflicting data concerning the involvement
2022-03-02
Conflicting data concerning the involvement of H2R on glycaemia has also arisen. Its antagonism was reported to decrease [35], not affect [36], [37] and increase [38], [39] Mirin levels. In comparison, the clinical experience with antipsychotic drugs generated clearer evidence for the involvement o
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