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br Conflict of interest br Introduction Since
2022-03-12
Conflict of interest Introduction Since its discovery in 1958 [1]the Ca2+-dependent K+ efflux in human red blood ST 2825 (RBC) (further referred to as the Gárdos effect) has been extensively studied (see 2, 3for review) and has been helpful in understanding the role of the Ca2+-activated K+ ch
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Our own search towards aryl imidazole
2022-03-12
Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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br Materials and methods br Results
2022-03-12
Materials and methods Results and discussion Conclusions Notes Declaration of interest statement Acknowledgment This work was supported by the National Natural Science Foundation of China (No. 21775132, 21505112), Scientific Research Foundation of Hunan Provincial Education Departm
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br Acknowledgments We apologize for
2022-03-12
Acknowledgments We apologize for the omission of primary citations owing to space limitations. This work was supported by grants from National Natural Science Foundation of China (81772801 and 81472455 to C.D.), the Key Program of Zhejiang Provincial Natural Science Foundation (LZ17H160002 to C.D
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Ras pathways are involved in the regulation of virulence
2022-03-11
Ras pathways are involved in the regulation of virulence in Cryptococcus neoformans [7] and Candida albicans [8,9]. To verify the importance of Ras in the survival response of the fungus in the host, a pathogenicity test of P. brasiliensis was performed before and after treatment with the Ras inhibi
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br Acknowledgements br Introduction The glutathione S
2022-03-11
Acknowledgements Introduction The glutathione S-transferase (GST, EC 2.5.1.18) family of multifunctional enzymes plays a particularly important role in cellular detoxification [1]. Over-expression of the GSTP1 isoform characterizes many human tumor cell lines derived from stomach, brain and co
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AG-1024 Our study has strengths and limitations We believe
2022-03-11
Our study has strengths and limitations. We believe we are the 1st to report a novel model of secondary hypogonadism. Several animal models for hypogonadotropic hypogonadism (kisspeptin and the kisspeptin receptor knockout) exist but we are unaware of animal models of secondary hypogonadism with dif
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br Cholecystokinin CCK CCK is secreted by enteroendocrine
2022-03-11
Cholecystokinin (CCK) CCK is secreted by enteroendocrine I-cells of the duodenum and jejunum in response to amino acids and lipids [14]. There are two forms of the CCK receptor, CCK1 which is expressed on pancreatic α- and β-cells while CCK2 is located on somatostatin-secreting δ-cells [8]. CCK r
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GPR is a G protein coupled receptor that
2022-03-11
GPR55 is a G protein-coupled receptor that has pro-oncogenic properties and whose expression correlates with tumor aggressiveness and increased activation of extracellular signal-regulated kinase (ERK) cascade [12]. Elevated expression of GPR55 has been linked to aggressiveness in human pancreatic,
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We recently reported that the human
2022-03-11
We recently reported that the human-derived PancCa cell line PANC-1 and the human-derived hepatocellular HepG2 cell line express GPR55 mRNA and protein [21]. In PANC-1 and HepG2 cells, knockdown of GPR55 with specific siRNAs abrogates cellular uptake of Tocrifluor 1117, a selective GPR55 ligand [21]
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The manuscript provides mechanistic insights into the suppre
2022-03-11
The manuscript provides mechanistic insights into the suppression of EGFR, BCRP, PKM2, and other cancer biomarkers in response to pharmacological inhibition of GPR55 with MNF and CID (Fig. 7). Firstly, inactivation of ERK has been previously demonstrated following treatment of PANC-1 LDN193189 Hydro
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Apart from the different assays used
2022-03-11
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 LY2874455 stably transfected with human GPR55. They found that the effect of both ligands on intracellular Ca2+ was
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Finally we investigated increasing basicity as a way
2022-03-11
Finally, we investigated increasing basicity as a way to improve solubility. We expected that conversion of the ether linkage of to an -methyl group could improve solubility. More than expected, amitriptyline hydrochloride receptor demonstrated significant improvement of values of solubility for
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The main results whose proofs depend on
2022-03-11
The main results, whose proofs depend on the explicit calculation of , include To set our work into the historical context, we note that the transporter category algebras are skew group algebras, and thus are fully group-graded algebras. This work is partially motivated by the papers on fully group
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Because sleep and metabolism are
2022-03-11
Because sleep and metabolism are intimately linked, the authors next move to study whether Eaat2 also controls metabolic rate. First, we must ask how sleep and metabolism are connected at a functional level. The Apocynin allocation hypothesis of sleep posits that organisms temporally partition spec
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