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br Discussion The pattern of activity exhibited by SSR and
2022-04-11
Discussion The pattern of activity exhibited by SSR 504734 and Lu AA21279 in the MEST test was very similar. Both compounds were inactive at the lowest dose (3.0mg/kg), but exhibited robust increases (∼150%) at 10mg/kg followed by a maximal detectable response at 30mg/kg. Based on the magnitude o
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br The actions of GLP on the vasculature endothelium
2022-04-09
The actions of GLP-1 (9–36) on the vasculature/endothelium The previous sections have ascribed the vascular and/or endothelial actions of GLP-1/GLP-1R agonists to potential direct actions through a canonical GLP-1R, but as mentioned previously, whether VSMCs and ECs express a full-length GLP-1R r
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FFAs concentration response curves for
2022-04-09
FFAs concentration–response curves for increasing intracellular calcium and receptor phosphorylation showed a difference of ≈1 order of magnitude indicating a relatively large receptor reserve, which is expected for a transfected model, and that high receptor occupancy is necessary to induce recepto
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Another lever to efficiently eradicate tumors including ovar
2022-04-09
Another lever to efficiently eradicate tumors including ovarian cancer might rely on their high addiction to iron [34]. In fact, ultrasmall silica-based nanoparticles, functionalized with melanoma-targeting peptide, efficiently triggered ferroptosis not only in cell culture but also in tumor bearin
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Introduction Post translational modifications to the N termi
2022-04-09
Introduction Post-translational modifications to the N-terminal tails of the histone proteins play crucial roles in genome regulation [1]. These modifications (e.g. acetylation, methylation, phosphorylation) are deposited by so-called ‘writer’ enzymes and dynamically removed by the action of ‘erase
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H R antagonism can prevent seizure development and improve
2022-04-09
H3R antagonism can prevent seizure development and improve working memory through the activation of histaminergic neurons (Huang et al., 2004, Zhang et al., 2003). In addition, we have recently found that H3R antagonism protects against ischemia-reperfusion injury via histamine-independent mechanism
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Our results demonstrated that most of the HUA rings
2022-04-09
Our results demonstrated that most of the HUA rings incubated with 100 μM TBT do not have the capacity to contract in the presence of 5-HT or exhibit very low contractions in comparison to the control. Only 23.3% of the HUA rings were able to contract. These results seem to indicate that there may b
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The newest histamine receptor to be discovered
2022-04-09
The newest histamine receptor to be discovered is the H4 receptor, which was identified in humans and cloned in 2000 (Thurmond, 2010). Genetically, the H4 receptor is closely related to the H3 receptor, but is restricted to H-Lys(Z)-OH within the spleen, intestines and thymus, and to immune cells su
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Several studies have indicated that PLD regulated PA signali
2022-04-09
Several studies have indicated that PLD-regulated PA signaling intersects with Rho-mediated cytoskeletal remodeling to drive mesenchymal-like cellular features, and it is known that Rho signaling has the potential to induce YAP/TAZ nuclear activity. Accordingly, Han et al. (2018) provide evidence th
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br S proteins and HBV induced autophagy HBV
2022-04-08
S proteins and HBV-induced autophagy HBV surface proteins (S proteins or HBs) are reported to trigger HBV-induced autophagy by inducing ER stress and UPR in host Liquidambaric acid [22]. HBx and HBV-induced autophagy HBx is a multifunctional viral protein. It can regulate virus replication,
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Acknowledgments We would like to thank Dr Greg Morriello
2022-04-08
Acknowledgments We would like to thank Dr. Greg Morriello, Mr. Lehua Chang, Mr. Chris Moyes and Mr. Nam Fung Kar for intermediate 3 syntheses. Cheng Zhu would like to thank Dr. Milana Maletic, Mr. Kake Zhao and Mrs. Wanying Sun for helpful discussions. Introduction Glucagon-like peptide-1 (GLP-
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Introduction GPR is a class A type of
2022-04-08
Introduction GPR119 is a class A type of G Protein coupled receptor, which is expressed primarily in pancreatic β-cells and the K and L loteprednol of the gastrointestinal tract [1], [2], [3]. Activation of GPR119 promotes secretion of incretins such as glucagon-like peptide-1 (GLP-1) in the intes
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Finally we investigated increasing basicity as
2022-04-08
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, ABT263 demonstrated significant improvement of values of solubility for the two media, especially for aci
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Several investigators including ourselves have previously sh
2022-04-08
Several investigators including ourselves have previously shown, that allogeneic HLA-DPB1 class II-alleles are powerful leukemia rejection Sulfamethazine mg for CD4 T-cell therapy following allogeneic hematopoietic stem cell transplantation (Herr et al., 2017, Rutten et al., 2008, Stevanovic et al.
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Cl-Amidine trifluoroacetate salt The negative impact that di
2022-04-08
The negative impact that dimers present in gp120 preparations have on overall gp120 affinity for CD4i ligands, mainly by affecting the on-rate, was addressed in this report. Indeed, when his(6)-tagged gp120 proteins, purified with nickel beads (before FPLC, containing gp120 dimers) were used to meas
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