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To test the compounds metabolic
2024-10-09
To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structural
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br Results br Discussion Context specific and dynamic post
2024-10-09
Results Discussion Context-specific and dynamic post-translational protein modifications are well-established regulators of the signaling pathways that protect eukaryotic DNA integrity during the tremendous task of replication. Advancements in speed, resolution, and sensitivity of MS-based tec
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Calcineurin has been established to
2024-10-09
Calcineurin has been established to be a ubiquitous Ca2+-activated serine phosphatase in the nervous system (Pyrzynska et al., 2001). It has been reported that the activation of calcineurin protects aromatase from autophagy-mediated protein degradation, implying that calcineurin-dependent dephosphor
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nebuilder Various antiangiogenic drugs have been analyzed
2024-10-09
Various antiangiogenic drugs have been analyzed over the last few years; noteworthy, bevacizumab, a monoclonal antibody against VEGF-A, alone or in combination with cytotoxic agents showed interesting results in terms of radiographic response rates and progression-free survival in initial phase 2 st
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Our observation that squalestatin caused only small
2024-10-09
Our observation that squalestatin caused only small differences in the production of Aβ40 and Aβ42 was in contrast to prior reports of the effects of other cholesterol synthesis inhibitors. This may be due to using squalestatin, a more specific cholesterol synthesis inhibitor that does not affect is
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br Expression of adiponectin mRNA in
2024-10-08
Expression of adiponectin mRNA in chickens We first sought to determine the nucleotide sequence of the chicken adiponectin cDNA. The open reading frame of the chicken adiponectin cDNA consists of 735 nucleotides that was 65–68% homologous to various mammalian adiponectin cDNAs (Maddineni et al.,
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In the current study adiponectin receptors expressions were
2024-10-08
In the current study, adiponectin receptors expressions were detected in both cell lines. AdipoR2 showed equal expression levels, whereas AdipoR1 possessed different expression levels in both cell lines. There was a significant increase in the AdipoR1 mRNA levels in cell lines according to AdipoR2 m
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NLX a k a F or befiradol exhibits
2024-10-08
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in LDN 57444 to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it has
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br GMF Remodels Actin Networks at the Leading Edge How
2024-10-08
GMF Remodels Actin Networks at the Leading Edge How are the conserved activities of GMF used in vivo to regulate branched lot xx networks (e.g., at sites of endocytosis and at the leading edge) (Figure 2A,B)? In animal cells, the regulatory effects of GMF on actin networks appear to govern lamell
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The current antifungal pipeline contains
2024-10-08
The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of
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A Belgian review on perioperative
2024-10-08
A Belgian review [9] (2011) on perioperative management of drugs recommends not using ACEI/ARBs due to the same reason. Another 2014 French [10] publication on the management of antihypertensive drugs in the perioperative period suggests withholding this medication before surgery even though they a
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bcl-2 family Obesity is defined as a body
2024-10-03
Obesity is defined as a body mass index (BMI) of 30kg/m2 or higher and is known to have a very close association with the risk of developing cancers (Hsueh and Deng, 2016). Several theories exist as to how this link is defined with respect to various cancers, one of which involves the effect of obes
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The most widely recognized effects of adenosine
2024-10-03
The most widely recognized effects of adenosine are operated through inhibiting A1R, one of the most abundant G protein-coupled receptors in Fructose tissue [53]. A1R are located presynaptically, postsynaptically and nonsynaptically [54]. Effect of adenosine in neuronal circuits of adult mammals is
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Although CP has been an important
2024-10-01
Although CP has been an important research subject in the field of antigen processing and presentation, the mechanisms of presentation of intracellular protein phosphatase by MHC II received considerably less attention. Interestingly, pioneering work by the Münz laboratory has pointed to an involve
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Compound was docked into the active site of
2024-10-01
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the d
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