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Negative regulation of AR expression by NF B
2024-05-29
Negative regulation of AR expression by NFκB was also correlated with the ‘age-dependent desensitisation’ of androgen action in the rat liver (Supakar et al., 1995). In this case the binding site was mapped upstream of the gene to sequences −555 to −565 bp, that binds heterodimers of p65 and p50, as
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The association of male gender with increased atherosclerosi
2024-05-29
The association of male gender with increased atherosclerosis has stimulated interest in the role of androgen signalling in this condition. Androgens act (Fig. 2) by direct activation of androgen receptor (AR), a nuclear receptor that acts as a ligand-regulated transcription factor (Gao et al., 2005
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Furthermore to address the concern
2024-05-28
Furthermore, to address the concern that the observed positive in vitro activity results might be stymied by the propensity of such assays to display false positives due to the inherent noxiousness of the tested compounds, all analogs were evaluated against Vero cells in an MTT assay. Some of the mo
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Interest in natural products has
2024-05-28
Interest in natural products has led to the study of plant extracts as sources of ARIs. However, chemical complexity of natural extracts makes the identification of ARIs challenging and time-consuming. Identification of bioactive compounds with the desired biological effect from natural products, co
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In addition to the above mentioned synaptic mechanisms the s
2024-05-28
In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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br Methods br Results br Discussion First the cells isolated
2024-05-28
Methods Results Discussion First, the Cinchonidine isolated from non-PD TA tissue and PD plaque tissue were characterized. The results showed that both cell groups were positive for vimentin and negative for desmin suggesting that these cells were fibroblasts. It was also observed that tre
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br New AMPK activators Fenofibrate is a drug of the
2024-05-28
New AMPK activators Fenofibrate is a drug of the fibrate class used for the treatment of dyslipidemia [53] but is also an agent that could alleviate DN-induced alterations through AMPK activation (Fig. 2). Streptozotocin-induced diabetic rats treated with fenofibrate improved in not only renal fu
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Though we have proved that
2024-05-28
Though, we have proved that VA could suppress hepatic gluconeogenesis, the mechanisms of VA on gluconeogenesis in vivo and in vitro remain unclear. AMP-activated protein kinase (AMPK), which is called an energy receptor enzyme, is widely expressed in liver and other tissues [23]. AMPK has become ano
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trans-isomer sVRPs were more sensitive to ABT than MSRs This
2024-05-28
sVRPs were more sensitive to ABT-702 than MSRs. This result agrees with previous reports that the activation of A1 receptors more potently inhibits sVRPs than MSRs (Nakamura et al., 1997, Otsuguro et al., 2009). Importantly, sVRPs are thought to reflex C-fiber-evoked nociceptive transmission. Nocice
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Molecular docking is widely used to predict the interaction
2024-05-28
Molecular docking is widely used to predict the interaction between an enzyme and its inhibitors. This is a computational simulation approach that can be used as a tool to investigate the structure-activity relationship of ACE inhibitory peptides (Goodsell, 2009). It has been recently shown that ACE
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The present study showed for the first
2024-05-28
The present study showed, for the first time, that hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, and isocorynoxeine in yokukansan can inhibit the 5-HT3 receptor current. These data indicate that part of the effect of yokukansan against the behavioral and psychological symp
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A rational approach for the design of
2024-05-28
A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a
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BAY 11-7082 br Conflicts of interest br Acknowledgments The
2024-05-28
Conflicts of interest Acknowledgments The authors acknowledge National Institute for Medical Research Development (NIMAD) project no. 940943 and National Research Institute for Science Policy (NRISP) no. 1456 for financial support of this work. AM appreciates National Institute for Genetic Eng
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Transient transfection with ATR kinase
2024-05-28
Transient transfection with ATR kinase-dead (D2475→A) [30] and ATM kinase-dead (D2870→Ala and N2875→K) [31] constructs was performed using Fugene 6 (Roche Applied Science, Indianapolis). Three microliters of fugene 6+1μg plasmid was used in transfections using 6-well plates at 2×105 cells/well and a
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Although TP status has been shown
2024-05-28
Although TP53 status has been shown to play a role in ATR inhibition and platinum resistance [7], [27], [38], in inhibition of ATM and sensitivity to IR [39], and in the activation of Chk1 and Chk2 [3], [4], ATM and ATR signaling can occur through the p38MAPK/MK2 pathway in p53-deficient Dyphylline
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