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JNJ-38877605 The apparent lack of effect of Fas deficiency o
2021-11-09
The apparent lack of effect of Fas deficiency on MAV-1 replication in infected mice could be due to immunoevasion by virus inhibition of Fas activation. If that were the case, Fas deficiency would likely have minimal additional effect. HAdV infection triggers Fas internalization from the cell membra
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NeuroHIV is initiated by HIV crossing the blood brain barrie
2021-11-09
NeuroHIV is initiated by HIV crossing the blood–brain barrier (BBB) to enter the CNS. This is thought to occur primarily via the transmigration of infected CD14+CD16+ monocytes (Williams, 2014), using the monocytes as “Trojan Horses” (Peluso, 1985), although some studies suggest alternate routes of
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Drosophila is a well established model to investigate the mo
2021-11-09
Drosophila is a well-established model to investigate the molecular and cellular defects underlying human neurodevelopmental disorders (Oortveld et al., 2013, van der Voet et al., 2014). Here, we establish Drosophila as a model for understanding the mechanisms linking mutations in KDM5 family protei
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Betahistine N methyl pyridyl ethylamine is a
2021-11-09
Betahistine (N-methyl-2-(2-pyridyl)ethylamine) is a well-known dual H1 PD 0332991 agonist/H3 receptor antagonist with structural resemblance to histamine. Though it has been approved long before the discovery of H3R to treat disorders of vestibular function as Menières-Disease, the evidence for thi
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However HDACi can also increase the acetylation of other
2021-11-08
However, HDACi can also increase the acetylation of other transcription factors that regulate p65 transcriptional activity. The HDACi-induced activation of p65 can be negated by acetylated STAT1, which can specifically bind to p65 and inhibit its transcriptional activity 81, 82, 83. Interestingly, a
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ICLs represent of all generated DNA adducts
2021-11-08
ICLs represent ICL Inducers in Cancer Therapy Nitrogen mustards with aromatic substituents (chlorambucil, melphalan) or a bioactivatable phosphoramide group (cyclophosphamide) were one of the first identified DNA crosslinkers. These agents are still used in combined schemes for the therapy of chr
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At days and hours after MI the
2021-11-08
At 21 days and 24 hours after MI, the protein expressions of active JNK1 (P protein thereby of p38 was down-regulated only at 21 days after MI (P Discussion This study demonstrates the role of GSTP1 in HF by inhibiting the TRAF2-induced MAPK activation and the potent inhibitory effect of GSTP1 o
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With this goal in mind we proceeded to explore
2021-11-08
With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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GDC-0994 australia In summary the SAR of a series of phenylp
2021-11-08
In summary, the SAR of a series of phenylpropanoic acid-free fatty GDC-0994 australia receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded rob
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Recently we indicated that cell motility was regulated
2021-11-08
Recently, we indicated that cell motility was regulated by the different induction of GPR120 and GPR40 in liver epithelial WB-F344 K-7174 receptor treated with chemical agents. The cell motility of WB-F344 cells was stimulated by phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA) which is a p
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Lenvatinib is an orally available multi targeted tyrosine
2021-11-08
Lenvatinib is an orally available, multi-targeted tyrosine kinase inhibitor against VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT [11,12]. In a recent phase III trial for patients with previously untreated uHCC (REFLECT study), lenvatinib showed statistical non-inferiority of overall survival compared to
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The suboptimal trypsin selectivity profile of
2021-11-08
The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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H O induced astrocyte ATP release
2021-11-08
H2O2 induced astrocyte ATP release through lysosome exocytosis. The LDH assay and electric microscope results indicated that the increase of extracellular ATP concentration was not due to the cell rupture, but the alternations in cell activities. In addition, when lysosome exocytosis was blocked by
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Meropenem trihydrate br Funding The research for
2021-11-08
Funding The research for this paper is conducted as part of a PhD thesis at Pasteur Institute of Iran and it was financially supported by Pasteur Institute of Iran and the Iranian Centre for Communicable Diseases. Conflict of interest Acknowledgments Introduction The viral enzyme integr
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The translational relevance of our findings remains uncertai
2021-11-08
The translational relevance of our findings remains uncertain at this point. On the one hand, there have been reports to suggest that boosting KDM4 activity may engender beneficial effects in vivo. For instance, Li et al. have show that KDM4 interacts with β-catenin to mediate Wnt signaling in hepat
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