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Models and theories The CPA equation
2019-11-22
Models and theories The CPA equation of state is composed predominantly of two parts: physical item and the association item based on the thermodynamic perturbation theory [21], [22], [26], [27]. The physical item is used to represent intermolecular physical interaction, usually representing the SR
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The small intestine in addition to its primary
2019-11-22
The small intestine, in addition to its primary role of absorption, has the ability to metabolize drugs and other xenobiotics through phase 1 and phase 11 metabolisms [25] since almost all the cytochrome P450 ikk pathway present in the liver are also present in the small intestine although, in lowe
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In all available E E structures
2019-11-22
In all available E2:E3 structures, the RING-type domain binds the E2 on a surface that is remote from the active site Cys (and therefore from the ubiquitin thioester) (Fig. 2). The non-contiguous E3-binding and active sites on the E2 imply that the role played by a RING to facilitate ubiquitin trans
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br Introduction O Methylguanine DNA methyltransferase MGMT
2019-11-22
Introduction O6-Methylguanine-DNA methyltransferase (MGMT) is a DNA-repair enzyme that specifically transfers alkyl adducts from the O6 position of guanine to the cysteine residue (Cys145) in its active site. In cancer cells, this ability of MGMT disrupts the cytotoxic actions of alkylating antic
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CFSs are recognized as a driver
2019-11-22
CFSs are recognized as a driver of genome instability in human cells and are hotspots for deletions or translocations in cancers (Richards, 2001). The generally accepted model for their expression is that the CFS locus shows a delay in chromatin condensation in early mitosis caused by the persistenc
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Importantly in genetic studies Saccharomyces cerevisiae Pif
2019-11-22
Importantly, in genetic studies, Saccharomyces cerevisiae Pif1, a member of the SF1 family of helicases, has been implicated in BIR in conjunction with Pol δ (Chung et al., 2010, Saini et al., 2013, Wilson et al., 2013). Using highly purified S. cerevisiae proteins, a system that permits dissection
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br Experiments and Methods br
2019-11-22
Experiments and Methods Results and Discussion Conclusions Here, the interactions between two newly-synthesized carbazole derivative—cationic δ,δ′‑diazacarbazoles and DNA were characterized by several spectroscopic means, including UV–Vis and fluorescence, AFM and fluorescence imaging. The
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With the narrow SAR of the
2019-11-22
With the narrow SAR of the tail favouring the ortho sulfone group, we examined the remaining position open to substitution at the pyrazole 3-position, in an attempt to at least moderate the excessive human PPB (). Lipophilic groups in this position maintained huge shifts in potency in the absence or
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In contrast to PEGylated proteins which tend to have reduced
2019-11-22
In contrast to PEGylated proteins which tend to have reduced MRS 2578 receptor in the body relative to their native counterparts, proteins conjugated to albumin tend to accumulate in certain locales in vivo. This means that albumin-based drug carrier systems have particular applications in the fie
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Determination of relative potency EC by
2019-11-22
Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an
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br Conclusion br Declaration of interest br Introduction
2019-11-22
Conclusion Declaration of interest Introduction Glyphosate [N-(phosphonomethyl)glycine] is the main active ingredient in one of the most widely used herbicides in the world. The commercially used concentrations of glyphosate range from 1% for domestic use to 41% for conventional agricultura
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The reduction of the calcium response to AVP
2019-11-22
The reduction of the calcium response to AVP could be also due to a PKA-mediated effect of desensitization of IP3R, as described in rat megakaryocytes [41]. Furthermore, PKA activation inhibits intracellular Ca release in mouse pancreatic acinar cells [42] or in rat cerebellum [43]. The phosphorylat
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The nitrophenols b d were prepared
2019-11-22
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 Kinase Inhibitor Library gave an inseparable mixture of 34b–d and 40b–d (1:1). This synthetic problem was successfully avoided as described below.
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Elastase belongs to chymotrypsin family of proteases and it
2019-11-21
Elastase belongs to chymotrypsin family of proteases and it is responsible for the breakdown of elastin and other proteins, such as collagen and fibronectin, which are fundamental for the ECM elastic properties (Imokawa and Ishida, 2015). Misregulations of this enzyme are involved in skin ageing pro
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br Introduction Protein modification by
2019-11-21
Introduction Protein modification by ubiquitin and ubiquitin-like proteins is one of the most common and important regulatory mechanisms in biology (Finley et al., 2004, Pickart, 2004). Ubiquitination is carried out by an enzymatic cascade consisting of three steps. In the first step, ubiquitin i
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