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Experimentally the ECD spectrum of showed three
2024-01-23
Experimentally, the ECD spectrum of 1 showed three ECD bands: positive ones at 260 and 200nm, and a negative one at 230nm (Fig. 4). Meanwhile, there is only one broad positive ECD band starting from 300nm in the ECD spectrum of 2. ECD spectra of 1 and its derivatives attracted great interest because
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Plant defensins Vriens et al and linear AMPs
2024-01-23
Plant defensins (Vriens et al., 2014) and linear AMPs (Domingues et al., 2015, Liu et al., 2008) have been shown to present several modes of action. Among these different mechanisms, permeabilization of the fungal membrane has been described as a secondary effect of plant defensin action (Vriens et
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br Materials and methods br Results br
2024-01-23
Materials and methods Results Discussion We demonstrate reduced angiogenic activity in NDRG1 overexpressing malignant glioma leading to reduced glioma growth. This antiangiogenic phenotype is paralleled by a significant upregulation of the antiangiogenic gene TNFSF15. TNFSF15 upregulation i
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br Conclusions and perspectives In view
2024-01-23
Conclusions and perspectives In view of the evidences supporting that Calcium Gluceptate MAS receptors mediate the effects of AT1 antagonists (Iwai et al., 2012, Ohshima et al., 2014, Pernomian et al., 2015, Schuchard et al., 2015), the prime targets from the perspectives on future directions in
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proton pump inhibitor Since the first studies of betaine
2024-01-22
Since the first studies of betaine aldehyde oxidation in rats [13], the participation of betaine in the detoxification of homocysteine has well described, considering the activity of other proton pump inhibitor as betaine homocysteine methyltransferase and methionine synthase. But, there is a lack
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Differentiation of skeletal myoblasts is
2024-01-22
Differentiation of skeletal myoblasts is a tightly orchestrated process that involves myoblast proliferation, screening libraries withdrawal, expression of muscle-specific genes, and fusion into multinucleated myofibers (Horsley and Pavlath, 2004; Krauss, 2010). The maintenance of muscle mass is im
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AHR mediated MMP upregulation has been
2024-01-22
AHR-mediated MMP1 upregulation has been shown in response to tobacco smoke [32]. Tobacco smoke contains various AHR ligands such as benzo[a]pyrene. Both benzo[a]pyrene [15] and FICZ [13] are high-affinity ligands for AHR and upregulate CYP1A1 and CYP1B1. FICZ is rapidly degraded by CYP1A1 [20], [33]
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Further evidence for action mechanism was provided by
2024-01-22
Further evidence for action mechanism was provided by assays using [3H]nisoxetine, a selective NET inhibitor used as standard radioligand for competitive binding experiments. The results showed dose-dependent blocking of [3H]nisoxetine binding by both xylazine and dexmedetomidine. Nisoxetine binds t
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br Conclusions Triptans are HT B D
2024-01-22
Conclusions Triptans are 5-HT1B/1D/(1F) receptors agonists and are considered as the gold standard for acute migraine treatment that have been proven effective. Unfortunately, they are contraindicated in patients with cardiovascular diseases due to their vasoconstrictor (side) effects (MaassenVan
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br Concluding Remarks The effects of point mutations of the
2024-01-22
Concluding Remarks The effects of point mutations of the four ARs on ligand binding affinities, functional potencies, and efficacies constitute a valuable source of pharmacological information. We analyzed the existing data and mapped it on the collection of available AR crystal structures, allow
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We investigated the role of ABT treatment
2024-01-22
We investigated the role of ABT 702 treatment in MAPKinase activation in mouse microglia in vitro. In Fig. 7D immunocytochemistry results revealed that Iba1 and p-ERK1/2 co-localized in LPS induced mouse microglia. In our previous study we have reported that LPS activates ERK1/2 phosphorylation (Ahm
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Previous studies have demonstrated the presence of
2024-01-22
Previous studies have demonstrated the presence of soluble NTPDases, 5′-nucleotidase and adenosine deaminase in rat blood serum as well as in human blood (Doleski et al., 2016; Oses et al., 2004; Yegutkin, 1997; Yegutkin et al., 2007). In addition, our earlier reports have shown that these membrane-
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Taken together our results indicated that LOX can
2024-01-22
Taken together, our results indicated that 5-LOX can be induced in mice by MPTP injection, and the 5-LOX inhibitor MK-886 reduced the death of dopaminergic neurons. MK-886 also reduced the LTB4 SKI-606 australia induced by MPTP. The development of the novel 5-LOX or FLAP inhibitors may provide a new
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Thus one possible target for
2024-01-22
Thus one possible target for CRPC treatment is the enzyme 17,20-lyase, which plays a crucial role in androgen biosynthesis. This is because inhibition of 17,20-lyase would be expected to decrease serum androgen levels secreted not only by the testes but also by the adrenal glands.7, 8, 9 In recent
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PF also a dual Aurora A and
2024-01-22
PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly 4sc 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 the MTD was defined as
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