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Recently two distinct small molecule inhibitors
2024-07-24
Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer xanthine oxidase with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the
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br Comparison to IWG In
2024-07-24
Comparison to IWG In addition to the NIA AA, the other group that has established diagnostic guidelines for AD that incorporate biomarkers is the IWG [64,74,75]. In the most recent formal IWG document, published in 2014 [75], the diagnosis of AD required the presence of cognitive symptoms plus an
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HsALDH enzyme has been purified for the first time
2024-07-24
HsALDH enzyme has been purified for the first time in our laboratory from human saliva and has been kinetically characterized using different aromatic substrates [35]. Also, the effect of some common substances frequently encountered by the enzyme in the oral cavity (such as ethanol, hydrogen peroxi
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br The AHR functions in the immune
2024-07-24
The AHR functions in the immune system – a tsunami of exciting findings The research of recent years has convincingly established an important function of the AHR in linking chemical environmental cues to immune responses [21,22], and reviewed in [1,23]. As a side effect, a view of the AHR as “Th
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The AhR molecule is composed of
2024-07-24
The AhR molecule is composed of multiple functional domains [38]. In the N-terminal end, the AhR contains bHLH domain which is involved in DNA binding, dimerization with ARNT and association with chaperone proteins. The PAS domain, which is situated next to the bHLH domain consists of two structural
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Mt a known to be upregulated by
2024-07-24
Mt2a, known to be upregulated by ozone (Inoue et al., 2008), was also increased in vehicle-pretreated rats exposed to ozone, however, this effect was markedly reduced by both PROP and MIFE, suggesting that the neuroendocrine response is linked to ozone-induced acute phase protein expression. In huma
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Sperm total motility and hyperactivated motility are
2024-07-24
Sperm total motility and hyperactivated motility are mediated by PLD-dependent dopamine hydrochloride polymerization [20]. Reduction of PIP2 synthesis inhibited actin polymerization and motility, and increasing PIP2 synthesis enhanced these activities. Furthermore, sperm demonstrating low motility
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br Acknowledgments br Introduction Hypospadias is a
2024-07-24
Acknowledgments Introduction Hypospadias is a common congenital malformation in males, in which the urethral orifice is found on the ventral side of the penis as a result of incomplete fusion of urethral folds. The mean prevalence in per 10,000 live births from 1910 to 2013 were: Europe 19.9,
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Finasteride was the first steroidal reductase inhibitor
2024-07-24
Finasteride (13) was the first steroidal 5α-reductase inhibitor approved by the US Food and Drug Administration (FDA) in 1992 for treatment of BPH. In fact, long term clinical studies with this drug demonstrated a sustained reduction of the prostatic specific antigen and an overall improvement in BH
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br Contemporary understanding for alcoholic cardiomyopathy U
2024-07-24
Contemporary understanding for alcoholic cardiomyopathy Up-to-date, a number of theories are postulated for alcoholic cardiomyopathy including generation of mitochondrial reactive oxygen species (ROS), oxidative stress, neurohormonal overactivation (catecholamines and angiotensin II), apoptosis a
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IC values were obtained for
2024-07-24
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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br Experimental section br Competing interests br Author
2024-07-24
Experimental section Competing interests Author's contributions Acknowledgement This research is partially supported by a seed fund for the Center for Drug Discovery and Translational Research (LS) and a research grant by Fujifilm (VPS and LS). The Sponsors played no roles in study desig
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In this study we found that
2024-07-24
In this study, we found that ACL silencing is sufficient to impair myoblast differentiation and that this effect is accompanied by a decrease in MYOD early in the myogenic process and by a subsequent decline in fast MyHC protein sodium butyrate at a later stage of differentiation (Figure 4J). Furth
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In the nineties we knew that baclofen was the stereo
2024-07-24
In the nineties we knew that (-)baclofen was the stereo-selective ligand for the GABAB receptor which had been recognised by Norman Bowery as a receptor for GABA, which was different from the GABAA receptor (Hill and Bowery, 1981). GABAB receptor antagonists were also synthesised and made available
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br Aromatase the key enzyme for estrogen formation
2024-07-24
Aromatase: the key enzyme for estrogen formation in adipose tissue Estrogens are synthesized from androgens by aromatase, a member of the cytochrome P450 superfamily, which is the rate-limiting enzyme in estrogen biosynthesis (Santen et al, 2009, Simpson et al, 1994). At the cellular level, aroma
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