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MRS 2578 Measurement of Chol absorption synthesis and catab
2020-06-22
Measurement of Chol absorption, synthesis and catabolism would be very helpful to determine the underlying cause of hypercholesterolemia in individual patients at risk for atherosclerosis. The information could help to determine the best therapeutic approach to reduce Chol absorption, to reduce Chol
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br Introduction The cys loop
2020-06-22
Introduction The cys-loop ligand gated ion channels (LGICs) are membrane-bound proteins mediating fast transduction from chemical to electrical signals at neuronal synapses and neuromuscular junctions [1], [2]. Each subunit that makes up the pentameric LGIC architecture possesses a dicysteine bri
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Despite the weak and transient nature
2020-06-22
Despite the weak and transient nature of E2–E3 interactions, this binding is required for the transfer of ubiquitin to the substrate. The low affinity characteristics of this interaction may be due to the fact that E2s use the same surface to interact with E1s and E3s, and hence while binding to an
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In the context of E ligase drug discovery it
2020-06-22
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 met
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A surprising second functional effect
2020-06-22
A surprising second functional effect was found in culture experiments. Inclusion of LTD4 reduced the frequency of Fas receptor (CD95) expression. Once again, this effect, although modest, was reversed by a cysLT1 receptor antagonist. The biologic significance of this effect or its mechanism remaine
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On the one hand levels
2020-06-22
On the one hand, levels of up to 20 nM P4 have been reported for a cyprinid species, Labeo rohita, in summer (Suresh et al., 2008). Similarly, P4 concentrations in tilapia, Oreochromis mossambicus, were found to range up to 27 nM (Cornish, 1998). Nevertheless in sturgeon P4 levels of approximately 3
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These studies established IAP proteins as dimeric RING
2020-06-22
These studies established IAP proteins as dimeric RING E3 ligases, but did not account for the essential role of dimerization. In IAPs and related E3s, such as RNF4 and MDM2, dimerization not only depends on contacts from the core RING domain but also residues N- and C-terminal to the RING domain (B
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br Patients and Methods Patients
2020-06-22
Patients and Methods Patients who had been initiated on a DPP-4 inhibitor (see in the online version at doi:10.1016/j.clinthera.2018.06.002) between April 2012 and June 2017, when the common threshold for dose adjustment for all non-linagliptin DPP-4 inhibitors was a creatinine clearance (CrCl)
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br The modulation of ER from SERMs to TSECs Continued
2020-06-20
The modulation of ERα: from SERMs to TSECs Continued efforts to provide women with efficacious menopausal therapies have generated interest in the development of selective gaba receptors receptor modulators (SERMs). Similar to estrogens, SERMs have been shown to bind to ERs with high affinity, de
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The nitrophenols b d were prepared as
2020-06-20
The nitrophenols 34b–d were prepared as described in Scheme 3b. Nitration of phenols 39b–d with 1equiv of sodium nitrate in the presence of hydrochloric Voriconazole gave an inseparable mixture of 34b–d and 40b–d (1:1). This synthetic problem was successfully avoided as described below. Nitration o
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Some antioxidants including N acetylcysteine and SOD have be
2020-06-20
Some antioxidants, including N-acetylcysteine and SOD, have been shown to decrease collagen deposition and protect the lungs in various animal models and even in clinical trials (Chan et al., 2013, Loomis-King et al., 2013, Rafii et al., 2013, Teixeira et al., 2008, Wang et al., 2013). Bleomycin-ind
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E ligases provide substrate recognition specificity Ubiquiti
2020-06-20
E3 ligases provide substrate recognition specificity Ubiquitination NPE-caged-proton and substrate specificity in mammals is achieved by the existence of over six-hundred E3-ubiquitin ligases that catalyze the final step of ubiquitination, compared with only one E1 and very few E2 enzymes known til
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br Introduction Vitis vinifera L is
2020-06-20
Introduction Vitis vinifera L. is one of the most worldwide-grown fruit crop and is mostly used in the wine industry (Bouquet, 2011). Domestication and history changed dramatically the biology of this species and today there are thousands of V. vinifera varieties, being many of them closely relat
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Despite the significant increase in Bdnf mRNA levels after
2020-06-20
Despite the significant increase in Bdnf1 mRNA levels after DNMT inhibition, the expression of Bdnf4 and Bdnf9 was unaltered. It is particularly surprising that Bdnf4 is not affected by the DNMT inhibitor, as the promoter of the Bdnf4 exon is known to be susceptible to epigenetic changes (Kotera et
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The field of synthetic cytokine
2020-06-19
The field of synthetic cytokine biology continues to grow through molecular, physiological and pathophysiological insights, as well as via new methodical advances. The approval of chimeric antigen receptor (CAR) T cell immunotherapy by the US Food and Drug administration (FDA) in August 2017 for rel
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