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br Materials and methods br Results br
2022-01-28
Materials and methods Results Discussion Recently, we characterized the interaction of the PH domains of various Lbc family RhoGEFs with the activated small GTPase, RhoA, and demonstrated that this could serve as a positive feedback mechanism for robust activation of RhoA (Medina et al., 20
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Here we show that CT
2022-01-28
Here, we show that CT229 recruits multiple Rab GTPases and Rab effector proteins to the inclusion; the CT229 Inc protein redirects and intercepts host clathrin-coated vesicles (CCVs). CT229 is required for recruitment of transferrin (Tfn) positive CCV’s from the recycling pathway to the periphery of
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br Acknowledgements br Introduction The glutathione S transf
2022-01-28
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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Apart from the different assays used biased agonism could
2022-01-28
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 (3S,5S)-Atorvastatin sodium salt mg stably transfected with human GPR55. They found that the effect of both ligands
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Several studies have proposed that high levels of KYNA
2022-01-28
Several studies have proposed that high levels of KYNA in the GSK2606414 contribute to cognitive dysfunctions presented by patients who suffer from schizophrenia [30], [31], [32], [33]. Considering that: (i) KYNA is a known GPR35 agonist [2], (ii) cognitive impairments in patients with schizophreni
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br Concluding remarks Several orphan GPCRs have expression p
2022-01-28
Concluding remarks Several orphan GPCRs have expression profiles that indicate they are worthy of consideration as therapeutic targets. This view can be supported via various transgenic techniques, and it would be interesting to have wide-ranging phenotypic information on GPR35 knockout mice. Bas
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GPR is a member of the G protein coupled
2022-01-28
GPR119 is a member of the G protein-coupled receptor family, and is highly expressed in pancreatic β-cells and intestinal endocrine cells. It has been proposed that GPR119 agonists modulate glucose homeostasis by indirectly stimulating glucose-dependent insulin release through enhancing pancreatic c
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br Evolution of multiple GnRH forms
2022-01-28
Evolution of multiple GnRH forms and GnRH receptors across vertebrates GnRH is an evolutionary ancient peptide that first appears prior to the protostome-deuterostome split, and is a member of the GnRH-adipokinetic hormone-corazonin superfamily of peptides (Roch et al., 2011, Roch et al., 2014).
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br Materials and methods br Results br Discussion In this
2022-01-27
Materials and methods Results Discussion In this study, we demonstrated, for the first time, that manipulation of AKR1D1 expression and activity is able to regulate glucocorticoid availability in liver and non-liver cell lines. AKR1D1 over-expression leads to increased glucocorticoid cleara
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Following an endoproteolytic cleavage of C secretase
2022-01-27
Following an endoproteolytic cleavage of C99, γ-secretase trims the remaining fragment Aβ49 or Aβ48 in successive, mostly three-residue steps. Aβ49 typically gives rise to Aβ46, Aβ43, and Aβ40; whereas Aβ48 usually yields Aβ45 and Aβ42 [59]. The physical basis for this characteristic cleavage patter
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br Discussion and concluding remarks FPR is considered
2022-01-27
Discussion and concluding remarks FPR1 is considered to be a promising drug target for treating inflammatory and immunological diseases. Thus, natural compounds that could block and/or regulate FPR1 activity may be an important source of novel therapeutics for modulating inflammatory processes. H
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inspire you Tail group SAR of the imidazole derived analogs
2022-01-27
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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br Acknowledgements We thank Kathy Spindler
2022-01-27
Acknowledgements We thank Kathy Spindler for helpful review of the manuscript. Expert technical assistance from Joel Whitfield in the University of Michigan Cancer Center Immunology Core is greatly appreciated. This research was supported by the American Heart Association (16GRNT30250013) and by
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br Experimental br Results and discussion One of the
2022-01-27
Experimental Results and discussion One of the major challenges of oral drug delivery via nanocarriers is the fairly low efficiency of crossing the intestinal barrier. While there is the possibility of a paracellular transport for polar substances below 1000 Dalton [26], the key mechanism of o
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br Acknowledgments This work was supported
2022-01-27
Acknowledgments This work was supported by the National Natural Science Foundation of China (31100111), the Nature Science Research Project of Anhui Province (1508085MC43), the subject construction project from Anhui Academy of Agricultural Sciences (14A1110). We would like to acknowledge the tec
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