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Some of the earliest LOX inhibitors were redox inhibitors
2024-02-05
Some of the earliest 12-LOX inhibitors were redox inhibitors, including nordihydroguaiaretic 960 8 (NDGA), BW 755C, and baicalein 48, 49, 50. Redox inhibitors block the oxidation of the nonheme iron at the cataylytic site, preventing its conversion from the inactive (Fe2+) to the active (Fe3+) stat
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br Conclusion There have been multiple clinical trials and
2024-02-04
Conclusion There have been multiple clinical trials and pre-clinical studies that have tested the utility of 5ARIs in treating prostate disease, as summarized in Fig. 1. Inhibiting androgen action through the use of finasteride and dutasteride has been established as a valuable resource for physi
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br Regulation and pharmacology of mPGES mPGES
2024-02-04
Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the
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As we previously observed in
2024-02-04
As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall
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Phospholipases cleave membrane phospholipids from
2024-02-04
Phospholipases cleave membrane phospholipids from inflammatory cells, activated platelets, erythrocytes, adipocytes and cancer folate analogue (Aoki et al., 2008, Neidlinger et al., 2006). Several reports have analysed the role of LPA and its receptors in the pathogenesis of RA. Zhao et al. reporte
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Y 134 br Conflicts of interest br Introduction
2024-02-04
Conflicts of interest Introduction Phosphatidic Y 134 phosphatase (PAP) enzymes are responsible for catalyzing the reaction that dephosphorylates phosphatidic acid (PA), which in turn produces diacylglycerol (DAG) and a phosphate group during phospholipid regulation (Fig. 1A) [1]. Subsequentl
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It has been proposed that
2024-02-04
It has been proposed that a PrP pathogenic mechanism is a toxic gain of function secondary to the misfolding of mutated PrP. However, such a mechanism might not apply to all mutant PrP species, since some mutations had little effect on the stability and folding kinetics of PrP (Swietnicki et al., 19
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The functions of HMGN protein are modulated
2024-02-04
The functions of HMGN1 protein are modulated by various post-translational modifications, including phosphorylation , , , acetylation , and glycosylation . Phosphorylation in HMGN1 may influence its binding affinity to DNA or nucleosome-associated proteins and affect the sub-cellular localization an
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Although the interactions of PhLP with G and
2024-02-04
Although the interactions of PhLP with Gβγ and its other partners have been convincingly documented through in vitro studies, it is not clear how PhLP controls Phosphocreatine disodium salt signaling in vivo. C. elegans provides a powerful genetic model to analyze Phosducin function and study its i
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The renin angiotensin system RAS is a hormonal
2024-02-04
The renin-angiotensin system (RAS) is a hormonal system which plays a role in the regulation of blood pressure and body fluid Tamoxifen [14]. The main bioactive peptide of RAS is angiotensin II (Ang II) whose biological functions are interposed through angiotensin type 1 receptor (AT1R) and angioten
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Interestingly we noticed that LPS exposure was associated wi
2024-02-04
Interestingly, we noticed that LPS exposure was associated with decreased phosphorylation of AMPK and increased phosphorylation of p70S6K1, suggesting that AMPK inactivation and the subsequent mTOR activation might be involved in the development of LPS-induced inflammation. On the other side, treatm
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br Conclusions br Acknowledgments The
2024-02-02
Conclusions Acknowledgments The authors are thankful to Hugo Santos, Olga Martinez and Ricardo Lacerda for the technical assistance provided in the maintenance of the aquaria. This work was supported by national funds, through FCT and co-funded by the European Regional Development Fund (ERDF)
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Role of APPL in endosomal signaling pathways
2024-02-02
Role of APPL in endosomal signaling pathways Endosomes consist of distinct membrane subdomains within individual organelles and assist in the translation of extracellular stimuli via cytoplasmic transduction cascades to the nucleus [3], [74]. Endosomal abnormalities are associated with the pathogen
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The present work has implications for
2024-02-02
The present work has implications for our thinking about the effects of antidepressant (e.g. SSRIs) use on maternal care in depressed mothers which consist of approximately 10–20% of all mothers (Gjerdingen and Yawn, 2007, Susser et al., 2016), and more than 40% of depressed mothers are prescribed w
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Toxicity is the main reason for
2024-02-02
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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