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The objective of this study is to design and synthesize
2022-08-19

The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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We identified three genes KEAP NAA and
2022-08-19

We identified three genes—KEAP1, NAA38, and ABCC1/MRP1—as negative regulators of glutathione abundance in human cells. Like KEAP1, NAA38 appears to regulate NRF2 stability, as NAA38 deletion increased NRF2 protein levels and the expression of NRF2 target genes. NAA38 is a component of the NatC N-ter
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br Introduction Fructose bisphosphatase FBPase EC catalyses
2022-08-19

Introduction Fructose 1,6-bisphosphatase (FBPase; EC 3.1.3.11) catalyses the irreversible reaction of hydrolysis of fructose 1,6-bisphosphate to fructose 6-phosphate and inorganic phosphate [1]. Genetic and kinetic studies so far have demonstrated that at least two distinct isoenzymes of FBPase e
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α-Cyperone br Conclusions Our in vitro and
2022-08-19

Conclusions Our in vitro and in vivo data collectively demonstrate that zifaxaban is effective in preventing thrombus formation via direct and specific inhibition of FXa in a dose-dependent manner. Furthermore, zifaxaban has a potency that is similar to that of rivaroxaban and shows a similar or
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br Anti Factor Xa methods for DiXaIs
2022-08-19

Anti-Factor Xa methods for DiXaIs measurement in plasma Concerning Anti-Factor Xa methods, there is an excellent correlation between the 1-stage and 2-stage Anti-assays as shown in Fig. 6, and the concentrations measured are very similar with all methods. These methods and the DiXaI concentration
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STI571 In summary our results support the model
2022-08-19

In summary, our results support the model that the histone demethylase KDM5 is a critical host transcriptional regulator that maintains immune homeostasis and is responsible for preservation of the normal commensal microbial community structure and behavior. Neurodevelopmental disorders such as ID a
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br Acknowledgments We thank Prof Alexander D Johnson and
2022-08-19

Acknowledgments We thank Prof. Alexander D. Johnson and Suzanne M. Noble for kindly providing SN strains. This work was supported by Chinese National Natural Science Foundation Grants 31370105 and 31300057, and Shanghai STCSM Grant 12JC1409300. Introduction Organisms modulate gene expression
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Heavy alcohol consumption reported by
2022-08-19

Heavy alcohol consumption, reported by three of five referred patients with chronic HCV infection and cirrhosis, is a risk factor for cirrhosis in p.C282Y homozygotes [19], [47] and adults with chronic HCV infection [48]. Although none of the present referred patients were diagnosed to have porphyri
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NPxY was recognized as the first short signal
2022-08-19

NPxY was recognized as the first short signal sequence motif in the cytoplasmic domain of membrane receptors and proteins with critical roles in internalization and trafficking of receptor molecules [130]. Including LDL receptor, beta-1 integrin, megalin, beta-amyloid precursor protein, EGF receptor
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The CNP pGC B cGMP pathway has been reported to
2022-08-19

The CNP/pGC-B/cGMP pathway has been reported to be potent inhibitor of fibrosis, from an intrinsic compensatory protective response as well as a therapeutic in cardiorenal injury and disease states [6,12,13,22,30]. Indeed, fibrosis is a progressive process leading to increased risk for morbidity and
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br GnRH receptor expression is altered within GnRH
2022-08-18

GnRH receptor expression is altered within GnRH neuronal cells Kisspeptin failed to stimulate GnRH expression in our line of GT1-7 cells. Instead, we have found that kisspeptin increased the expression of the GnRH receptor in these Lauric Acid (Sukhbaatar et al., 2013). Based on the results of e
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Given that inactivation of GLO
2022-08-18

Given that inactivation of GLO1 by 4BAB is an active site directed mechanism, as the transition state analogue CHG protects GLO1 against inactivation by 4BAB (Figs. 2D and S6b), we next set out to determine the amino ligand gated channels that is covalently modified by 4BAB. From the X-ray crystall
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We noticed that the spontaneous
2022-08-18

We noticed that the spontaneous openings of the D97R α1 GlyR appeared to be quite similar to those elicited by a maximally-effective glycine concentration on wildtype GlyR; both generated similar open and shut dwell-time histograms, both exhibited openings grouped into clusters with Popen values gre
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Rifampicin that is methyl piperazinyl imino
2022-08-18

Rifampicin, that is 3-[[(4-methyl-1-piperazinyl) imino] methyl]-rifamycin (Fig. 1), is a semisynthetic antibiotic drug. It is one of the most potent and broad drug against bacterial pathogens and tuberculosis [9]. In recent years, rifampicin has also been reported to have inhibitory effects on Taq R
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Young et al described the role of
2022-08-18

Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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