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Finasteride has been shown to be a mechanism based inhibitor
2023-08-01

Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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In conclusion we have produced some
2023-08-01

In conclusion, we have produced some highly potent inhibitors of P450 in comparison to the standard tolbutamide receptor KTZ. Also, due to the limited specificity of these compounds against lyase in comparison to the 17α-OHase component, these compounds would be expected to have a major impact on c
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Our sample is representative of mRCC treated with sunitinib
2023-08-01

Our sample is representative of mRCC treated with sunitinib. However, the results from CCC setting have limited inference due to small exploratory sample (n = 51). Additionally, the significance of survival differences in CCC according to AXL staining is tangential. Unfortunately, we were unable to
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Thirty six of the analogs synthesized showed ATX inhibition
2023-08-01

Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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Recent studies have indicated that V ATPase activity negativ
2023-08-01

Recent studies have indicated that V-ATPase activity negatively regulates vacuolar fusion in vivo[17]. Since we have demonstrated that the pah1Δ Dyngo-4a have a more acidic vacuolar pH than the WT cells, and the genes involved in the pump activity are upregulated compared to WT, the pah1Δ cells' ac
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IGF is an anabolic growth factor that
2023-08-01

IGF1 is an anabolic growth factor that induces hypertrophy and blocks atrophy in skeletal muscle by activating the PI3K/AKT/mTOR pathway (Egerman and Glass, 2014). In addition to its anabolic and anti-catabolic effects, IGF1 stimulates fatty BPTES (FA) uptake and glucose metabolism (Clemmons, 2012)
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The importance of the ATM Tel to ATR
2023-08-01

The importance of the ATM/Tel1 to ATR/Mec1 switch in the response to DSBs remains to be determined. Noteworthy, resection-defective S. cerevisiae cells, such as sae2Δ, exo1Δ, fun30Δ or sgs1Δ mutants, fail to turn off the checkpoint in response to an unrepaired DSB [56], [127], [128]. Moreover, the s
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Here we investigate the ATM to ATR switch
2023-08-01

Here, we investigate the ATM to ATR switch in normal human fibroblasts (82-6 cells) after irradiation with γ-rays, or high LET 56Fe and 28Si and moderate LET 16O particles. Our data provide important evidence of LET dependence on the transition of ATM to ATR as well as end resection at the sites of
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Functional enhancers are often composed of binding
2023-08-01

Functional enhancers are often composed of binding motifs of multiple key transcription factors to confer spatial and temporal regulation of genes in a certain context. In the uterus, the difference between the number of genes that have associated PGR occupancy and that of progesterone responsive g
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Fourth non canonical sites may be targeted
2023-08-01

Fourth, non-canonical sites may be targeted. Classical benzodiazepines require the presence of a γ subunit for high-affinity binding, which limits their activity to a specific large pool of receptor isoforms, leaving other isoforms unaffected. In particular, δ subunit-containing receptors, as well a
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Calcineurin has been established to be
2023-08-01

Calcineurin has been established to be a ubiquitous Ca2+-activated serine phosphatase in the nervous system (Pyrzynska et al., 2001). It has been reported that the activation of calcineurin protects aromatase from autophagy-mediated protein degradation, implying that calcineurin-dependent dephosphor
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Apelin APJ triggers a variety of cellular signaling
2023-08-01

Apelin/APJ triggers a variety of cellular signaling pathways (Fig. 1). Recent studies from our laboratory showed that apelin-13 induces vascular smooth muscle cell (VSMC) proliferation by the upregulation of Cyclin D1 expression, which is involved in an ERK-dependent activation of Jagged-1/Notch3 si
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br The role of apelin in hypertension diseases
2023-08-01

The role of apelin in hypertension diseases The role of apelin and its receptor APJ in cardiovascular diseases has been described in numerous studies (Table 2) [36,37]. It has been revealed that exogenous apelin may lower blood pressure. Tatemoto et al. [6] have discovered that different forms of
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The reasons why antibiotic treatment may be
2023-08-01

The reasons why antibiotic treatment may be detrimental are diverse. First, it may result in disruption of multifaceted microbe–microbe, as well as microbe–host, interactions that are key for the maintenance of homeostasis within this ecosystem. This can lead to the expansion of pathogenic microorga
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The first evidence in supporting
2023-08-01

The first evidence in supporting the hypothesis that MAS receptors mediate the effects elicited by AT1 antagonists was provided by Iwai et al. (2012). The authors found that AT1 receptors triggers neointima formation after polyethylene-cuff placement around mouse femoral artery by reducing local ACE
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