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Introduction CYP is a superfamily
2020-06-11
Introduction CYP450 is a superfamily of heme-containing monooxygenases, many of which are expressed in the liver, and they are significant phase-I GM6001 in drug metabolism and detoxification. There are three subfamilies (CYP1, CYP2 and CYP3) that are mainly involved in the metabolism of drugs in
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Both the kK and kK mediated ubiquitination leads to rapid
2020-06-11
Both, the kK3 and kK5-mediated ubiquitination leads to rapid internalisation of target proteins followed by lysosomal degradation, similar to that seen for MARCH-1/8 [77]. Ubiquitination activity of kK3 and kK5 depends on the positioning of the targeted lysine (or cysteine) residues [22]. The positi
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br Results The AR genotype frequencies are shown in Table
2020-06-11
Results The AR genotype frequencies are shown in Table 1. Alleles at the two loci are in linkage disequilibrium, as expected for such closely linked loci and consistent with previous findings (Kittles et al., 2001). The genotype frequency for the DBH 1021 polymorphism is similar to previous find
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Effect of a C C double bond
2020-06-11
Effect of a C4-C5 double bond — The presence of a double bond at the substrate’s C4-C5 position affects the reactivity of Δ1-KSTDs to varying extent, depending on the enzyme. Most 3-ketosteroids that are converted by Δ1- KSTDs have this double bond. For some Δ1-KSTDs this double bond is even require
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Recent pharmacological and clinical studies suggested that e
2020-06-10
Recent pharmacological and clinical studies suggested that estetrol (E4) should also be considered as an interesting candidate for MHT (Abot et al., 2014; Mawet et al., 2015). E4 is naturally produced from E2 and estriol (E3) via 15α- and 16α-hydroxylase by the human fetal liver during pregnancy and
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In the context of E ligase drug
2020-06-10
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 ago
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Main Text Post translational modifications by ubiquitin Ub
2020-06-10
Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p
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Given a disruption of membrane internalization and
2020-06-10
Given a disruption of membrane internalization and an increase in synaptic glutamate receptors in CPG2 knockdown neurons, one might expect an increase in dendritic spine size as membrane continues to be inserted into the spines during receptor exocytosis. However, we observed the opposite phenotype,
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Furthermore collagen could be further utilized to surface
2020-06-09
Furthermore, collagen could be further utilized to surface modification of biologically inert materials, such as polymer materials and metal materials, which are always hydrophobic, lacking functional groups and poor cell adhesion. Therefore, various strategies have been tested to improve the proper
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br In patients with type I
2020-06-09
In patients with type I diabetes mellitus poor management causes/INS; a drastic rise in glucose levels resulting in diabetic ketoacidosis (DKA). About 1% of DKA episodes can be complicated by cerebral edema. ET and its receptors are involved in the regulation of /INS;cerebral blood flow. We studie
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In contrast to drospirenone dydrogestrone acts rather neutra
2020-06-09
In Talabostat mesylate to drospirenone dydrogestrone acts rather neutral at the aldosterone-, glucocorticoid- and androgen-receptor [12]. This indicates that the assessment of a ‘net-overall effect’ on the vascular system is very difficult based on the often discussed ‘partial effects’ of the proge
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br Experimental Procedures br Acknowledgments br
2020-06-09
Experimental Procedures Acknowledgments Bisphenol A (BPA) has been recognized as one of the most potent endocrine disruptors, functioning even at very low doses. Although it is anticipated that bapta receptor (ER) would mediate these effects of low-dose BPA, studies revealed that BPA bound
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The ERR gene lacks the typical TATA and CAAT
2020-06-09
The ERRα gene lacks the typical TATA and CAAT boxes, but has multiple consensus Sp1 binding elements in the GC-rich promoter (Shi et al., 1997). Previously, our laboratory has shown that ERRα expression is upregulated in the mouse uterus by estrogen (Shigeta et al., 1997) and recently we identified
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NAD+ In cholesterol synthesis HMG CoA
2020-06-08
In cholesterol synthesis, HMG-CoA reductase is the rate limiting step in cholesterol biosynthesis. Statins or HMG-CoA reductase inhibitors are commonly used for management of hypercholesterolemia. The presence of an HMG-like moiety on these drugs allows them to competitively bind to the catalytic do
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The authors then showed that Spt interacts directly with
2020-06-08
The authors then showed that Spt6 interacts directly with the PRC2 subunit Suz12. This interaction occurs in solution but not on chromatin, suggesting that Spt6 may prevent PRC2 recruitment by binding to Suz12. They then mapped the domains in both Spt6 and Suz12 that are involved in this interaction
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