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Recently roflumilast has been approved
2019-09-11
Recently, roflumilast has been approved as the first selective PDE4 inhibitor for the treatment of chronic obstructive pulmonary disease (COPD) [2]. Roflumilast has been suggested to target several different pathogenetic mechanisms, including inflammation, fibrotic, emphysematous and vascular remode
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In human neuroblastoma SH SY
2019-09-11
In human neuroblastoma SH-SY5Y filipin and in lymphoma Jurkat cells, Yamanaka et al. [56] showed that exogenously added 24(S)-hydroxycholesterol could be efficiently esterified by ACAT1. These results suggest that both ACAT1 and ACAT2 can control the oxysterol levels by directly esterifying them, i
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br Experimental Procedures br Author Contributions br Acknow
2019-09-11
Experimental Procedures Author Contributions Acknowledgments Introduction Oxysterols came to prominence in the late 1970\'s with the oxysterol hypothesis which proposed that the suppressive effect of cholesterol on its own synthesis is mediated through oxysterols not by cholesterol itsel
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FOX proteins constitute a large class of
2019-09-11
FOX proteins constitute a large class of transcription factors with multiple functions, from development and organogenesis to regulation of metabolic and immune functions. The Fox transcription factor is characterized by a 100-amino-acid wing helix or forkhead DNA-binding domain. In addition, the FO
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E is encoded by the largest and most conserved open
2019-09-11
E1 is encoded by the largest and most conserved open-reading frame (ORF) of the PV genome. The protein ranges in size from 600 to 650 amino acids, depending on the PV type. Overall, the protein can be divided into three functional segments: an N-terminal regulatory region that is essential for optim
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Because conventional KO mice die within h
2019-09-11
Because conventional KO mice die within 24h of birth, it is difficult to analyze higher Cyanidin Chloride clinical functions using them. Therefore, in this study, we generated brain-specific conditional DGKδ-KO mice and used these mice to perform behavioral and pharmacological tests. Results
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Quantum walks can be connected to
2019-09-11
Quantum walks can be connected to extended CMV matrices as follows. If all Verblunsky coefficients with even index vanish, then the extended CMV matrix becomes which resembles the matrix representation U. One may notice, however, that in the extended CMV matrix , whereas in the quantum walk matri
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Recently several Pt IV complexes as prodrugs
2019-09-11
Recently, several Pt(IV) complexes as prodrugs have been designed and studied to enhance anti-tumor efficacy of traditional Pt(II) drugs, improving their cellular uptake and blood-circulation time [26], [27], [28], [29]. Compared with their Pt(II) counterparts, six-coordinated Pt(IV) complexes with
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A widely accepted mechanism to differentiate hESCs into card
2019-09-11
A widely accepted mechanism to differentiate hESCs into cardiomyocytes is through perturbation of the canonical Wnt/β-catenin pathway. Initial Wnt activation is required to form the UNC 0631 [3]. Thereafter, it is believed that inhibition of the canonical Wnt/β-catenin pathway is pivotal for cardiom
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In some pancreatic and non pancreatic tissues the chloride
2019-09-11
In some pancreatic and non-pancreatic tissues, the chloride and calcium channels are heavily regulated by phosphorylation by protein kinases, such as PKC, cyclic AMP-dependent protein kinase (PKA), PKCaMKII, PI3K and protein tyrosine kinases [7,36,37]. Since the interaction of triterpenes with recep
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While these previous correlative studies have
2019-09-10
While these previous correlative studies have measured tDDR1 protein by IHC, these studies have not considered that pDDR1 could also be an important marker of cancer prognosis. A phosphoproteomic survey of lung cancer tissues did identify pDDR1 as one of the most commonly phosphorylated receptor kin
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br Results br Discussion The structures presented
2019-09-10
Results Discussion The structures presented here were solved at high mechlorethamine and show in detail how DDR1 achieves high affinity for imatinib and ponatinib, respectively. Both type II inhibitors bind in their more potent extended conformations to the inactive DFG-out conformation of th
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The pharmacokinetics properties of compound were
2019-09-10
The pharmacokinetics properties of compound were evaluated in male Sprague Dawley rats following IV (0.7mg/kg) and oral (2.0mg/kg) dosing. The total body clearance and the terminal half-life were 0.73 L/h/kg and 5.1h, respectively. After oral administration the compound showed good bioavailability (
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br Clinical trials of CRM
2019-09-10
Clinical trials of CRM1 inhibitors KPT-330 clinical trials have been initiated with promising very early results. One trial includes patients with advanced solid tumors whose disease has progressed after at least one prior therapy for metastatic disease (NCT01607905). Another trial includes patie
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br Materials and methods br
2019-09-10
Materials and methods Results Discussion Consistent with previous reports (Barr et al., 2010, Vuong et al., 2010), the current study demonstrates that rats treated with amphetamine exhibit heightened anxiety states during withdrawal. Furthermore, icv. infusion of a CRF2 receptor antagonist
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