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In the present study both experimental and
2022-08-02
In the present study, both experimental and theoretical studies were performed to explore the inhibitory mechanisms of indomethacin and its analogues towards GLOI. A remarkable correlation (=0.974) was derived for the four structurally similar NSAIDs and two curcumins between the experimental bindin
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Through a large scale phylogenetic analysis of UDG
2022-08-02
Through a large-scale phylogenetic analysis of UDG superfamily in more than 1000 completely sequenced genomes, it is shown that family 3 Coenzyme Q10 can be separated into two clades with the traditional family 3 SMUG1 as one of them (Fig. 1) [31]. UDG enzymes in another clade are present in eubacte
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The effect of the selected compounds
2022-08-02
The effect of the selected compounds on NF-kB transrepression was assessed using the well-studied HeLa B2 cell line that expresses endogenous GR and NF-kB family members and responds properly to glucocorticoids and pro-inflammatory cytokines (such as TNF). Our data revealed that the two hit compound
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The elective controlled fasting study
2022-08-02
The elective controlled fasting study in our patient provides further metabolic profiling in patients with GCGR defect. Despite her lean body mass with low weight, at the age of 7 years old she demonstrated a good tolerance for fasting with hypoglycemia Bardoxolone methyl synthesis level, insulin,
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One effective approach to fine tuning the lipophilicity
2022-08-02
One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Oseltamivir acid scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well
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The knowledge that piroxicam competes with ligands that bind
2022-08-02
The knowledge that piroxicam competes with ligands that bind to FPR may be of importance for a deeper understanding of the anti-inflammatory effects possessed by this NSAIDs. It has recently been reported that not only phagocytes but also platelets express FPR on their cell surface and that these re
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Considering the conformational preferences of the SRSRY sequ
2022-08-02
Considering the conformational preferences of the SRSRY sequence in the x-ray structures of soluble uPAR (SuPAR) [18], [19], [20], [50], [51], it is included in a quite flexible linker delimited by Cys76 and Cys95 residues. The SRSRY sequence adopts either α-turned or β-extended conformation. In any
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Current studies have identified five orphan G protein couple
2022-08-02
Current studies have identified five orphan G protein-coupled receptors (GPCRs) that can be activated by free fatty acids (FFAs), GPR40, GPR41, GPR43, GPR84, and GPR120. Short-chain fatty acids (FAs) are specific agonists of GPR41 and GPR43 [21] and middle-chain FAs agonize GPR84 [22]. Long-chain FAs
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br Conflict of interest br Acknowledgments The research was
2022-08-02
Conflict of interest Acknowledgments The research was funded by the Major Programs of Pharmaceutical research project of Jiangsu Province (Q2018044). Introduction Lipids are important regulators of cell death. In mammalian cells, both apoptotic and non-apoptotic cell death pathways can be
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Autophagy plays a multifaceted role in regulating both the
2022-08-02
Autophagy plays a multifaceted role in regulating both the quality and quantity of protein (e.g., protein half-life and activity) and organelles (e.g., mitochondrial number and function), thus determining cell fate [15]. The induction of autophagy has been generally considered a programmed cell surv
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Tyr phosphorylation of AnxA was first
2022-08-02
Tyr23 phosphorylation of AnxA2 was first reported to be involved in endocytosis, particularly in the internalisation of the insulin receptor [20]. Phosphorylated Tyr23 seems to be necessary for the stable association of AnxA2 with endosomes, and for their early-stage transport [14]. The role of AnxA
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DLS only provides a Z average size based on
2022-08-02
DLS only provides a Z-average size based on spherical model, hence the size of nanorods was determined as 300 nm by DLS measurement. However, the size of length is nearly 400 nm while width is about 100 nm, which was clearly observed by transmission electron microscopy (TEM) (D). Meanwhile, the TEM
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Based on our results we propose three possible
2022-08-01
Based on our results, we propose three possible mechanisms of HER2 loss after trastuzumab-based therapy (Fig. 3). The first possibility is a result of the differential effects of treatments on clonal subsets. In breast cancer, such selective pressure has been suggested to preferentially eradicate HE
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AEE788 receptor br Acknowledgments This research was funded
2022-07-30
Acknowledgments This research was funded by generous grants from the Singapore National Medical Research Council (NMRC CBRG grant NMRC/CBRG12Nov114 (BD)). WJC is supported by NMRC Clinician Scientist Investigator award and partly supported by a Singapore Cancer Syndicate Grant, the National Resea
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br Conclusions br Introduction Astrocytes contribute to phys
2022-07-30
Conclusions Introduction Astrocytes contribute to physiological ivosidenib function on many levels. They help maintain the physiological composition of the extracellular medium by, for instance, buffering potassium and uptake of neurotransmitters. They can also provide neurons with energy sub
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