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Although several ARIs have reached various phases of clinica
2024-06-13
Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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Cells have developed strategies aiming to enhance both
2024-06-13
Cells have developed strategies aiming to enhance both the efficiency of proteins with chaperone activity as well as their overall antioxidant capacity to maintain proteostasis under oxidative stress conditions (Miyata et al., 2012). For instance, 2-Cys peroxiredoxin is an abundantly expressed, anti
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In this study we demonstrated that DRR protein
2024-06-13
In this study, we demonstrated that DRR1 protein level in GBM tissues was significantly higher compared to normal Mupirocin tissues. This data suggested that DRR1 might play a role in the tumorigenesis of glioma. To investigate whether DRR1 could accurately predict the outcome in patients with gliom
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The decreased AR mediated response has been attributed
2024-06-13
The decreased βAR-mediated response has been attributed to different mechanisms, including an attenuation of PKA activation, an impaired generation of cyclic AMP, a reduced receptor density, and a less efficient coupling to adenylyl-cyclase [10]. However, currently there is no single molecular or ce
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br Transparency document br Introduction G
2024-06-13
Transparency document Introduction G protein-coupled receptors (GPCRs) comprise a diverse family of seven transmembrane domain-containing receptors represented by over 800 genes in humans. GPCRs respond to a range of stimuli, including peptides, hormones, growth factors, lipids, odorants, and
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Phosphodiesterase inhibition increases the intracellular lev
2024-06-13
Phosphodiesterase inhibition increases the intracellular levels of cAMP to restore spontaneous contraction (Essayan, 2001, Qi and Kwan, 1996), acting downstream of adenylyl cyclase. Therefore, cardiac arrest induced by decreased intracellular cAMP levels could be reversed by phosphodiesterase inhibi
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The srd a isoforms showed unique expression profiles in
2024-06-12
The srd5a isoforms showed unique expression profiles in early FHM development (Fig. 2). Similar to amphibian embryos, there was a high abundance of both srd5a1 and srd5a3 at 1dpf in FHMs, suggesting that mRNA for these enzymes may be maternally deposited and that these enzymes may play a key role in
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pdk1 Several dehidropregnenolone derivatives functionalized
2024-06-12
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mi
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LPA binds to six specific cell surface GPCR receptors
2024-06-12
LPA binds to six specific cell surface GPCR receptors. The receptors LPA1 (lysophosphatidic receptor 1, formerly, Edg2), LPA2 (Edg4) and LPA3 (Edg7) belong to the endothelial differentiation gene family (EDG) and share sequence homology (50–60% amino SB505124 homology) An et al., 1997, An et al., 19
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Accumulating data suggest that ROS trigger autophagy but in
2024-06-12
Accumulating data suggest that ROS trigger autophagy but, in turn, autophagy reduces ROS levels [23]. Our results are in agreement because 27-OH mediated autophagy induction interms of LC3 II formation and Beclin 1 protein expression was suppressed by treating the promonocytic cells with the antioxi
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alpha amanitin synthesis PF also a dual Aurora A and Aurora
2024-06-12
PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly alpha amanitin synthesis for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule th
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amc 7 This study evaluated the anti tumor influences of LA a
2024-06-12
This study evaluated the anti-tumor influences of LA against HepG2 amc 7 in vivro, and investigated the molecular mechanisms of inducing apoptosis. Overall, our studies suggested that LA is a promising anti-cancer drug and a possible novel therapeutic agent directed toward the mitochondrial-mediate
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Under some pathological conditions AT R internalization
2024-06-12
Under some pathological conditions, AT1R internalization is decreased when agonist exposure is prolonged. This weakens or removes the AT1R desensitization effect and leads to AT1R and downstream signal overactivation. AT1R overactivation can result in continued biological effects such as sustained v
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Interestingly we found that co treatment with losartan
2024-06-12
Interestingly, we found that co-treatment with losartan prevented the increased participation of ROS from NADPH oxidase on the contractile response to Phe observed in Hg-treated rats. Moreover, losartan also prevented the reduction in the endothelial NO modulation of this response found in treated a
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The Irbesartan Diabetic Nephropathy Trial enrolled
2024-06-12
The Irbesartan Diabetic Nephropathy Trial enrolled patients with type 2 diabetes, proteinuria of at least 0.9 g/24 h, BP >135/85 mmHg and moderate kidney impairment (creatinine 88 to 265 µmol/L in women or 106 to 265 µmol/L in men). Patients were randomized to receive irbesartan (titrated from 75 to
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