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br Halogenases Enzymatic C H activation leading to halogenat
2020-01-11
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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Initially the E uses ATP to activate the
2020-01-11
Initially, the E1 uses ATP to activate the C-terminal glycine residue of ubiquitin prior to ligation. In the first step of E1 activation, the E1 catalyzes the adenylation of ubiquitin and pyrophosphate (PPi) release. In the second step, the E1 releases adenosine monophosphate (AMP) and a thioester b
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Based on the above we hypothesized that a PROTAC strategy
2020-01-10
Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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Conventional assays rely on a
2020-01-10
Conventional assays rely on a comparable transformation of the target analytes and the structurally similar (but not identical) proxy substrates and are commonly used to measure individual enzyme activities in (pre-treated) intact sludge flocs (Burgess and Pletschke, 2008a, Gessesse et al., 2003, Y
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br Expression and Tissue Functions
2020-01-10
Expression and Tissue Functions of DDRs The DDRs are widely expressed in different tissues, both during development and in adult organisms. DDR1 mRNA is found in many tissues in mice and humans, with high levels in brain, lung, kidney, spleen, and placenta (Di Marco et al., 1993, Johnson et al.,
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At present there have been relatively
2020-01-10
At present, there have been relatively few studies that evaluated potential correlations between pulmonary and pleura metastases, hilar and mediastinal GW788388 nodes, and organs associated with distant metastasis and EGFR mutations [33,34,37]. Further research on these relationships is needed, whic
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In contrast to PEGylated proteins
2020-01-09
In contrast to PEGylated proteins which tend to have reduced zvad fmk 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 field of chemo
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br The central role of DNA PK in the
2020-01-09
The central role of DNA-PK in the NHEJ NHEJ can be divided in several steps (Fig. 1A): 1) recognition and binding of Ku at each ends of the DSB following by the assembly of the DNA-PK at the break points and bridging; 2) phosphorylation of the DNA ends by DNA-PKcs; 3) ligation of the ends by DNA
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Previous studies showed that many steroidogenic
2020-01-09
Previous studies showed that many steroidogenic enzymes act when the enzyme binds to the cofactor first [30]. In the present study, we showed that HPTE inhibited both AKR1C14 and RDH2 in a mixed mode when cofactor was used. This indicates that HPTE interferes with cofactor-binding residues although
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Many studies have found that there is an aberrant DNA
2020-01-09
Many studies have found that there is an aberrant DNA methylation in the imprinting control region of development-related genes in the spermatozoa of oligozoospermic men (Kobayashi et al, 2007, Marques et al, 2004, Marques et al, 2008), which most likely results from expressional changes in the DNMT
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br Introduction In addition to the
2020-01-09
Introduction In addition to the canonical double stranded structure, DNA can form various higher order structures such as bulges, and various kinds of mismatches, triplexes, to the G-quadruplex (G4). Over the past decades, accumulating evidence has begun to emerge that these non-canonical structu
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br Introduction Fibroblast growth factors FGF are a
2020-01-09
Introduction Fibroblast growth factors (FGF) are a family of 18 secreted ligands that bind to four receptor tyrosine kinase (RTK) FGF receptors (FGFR1–4). The interaction of FGFs with their cognate receptors results in the activation of a number of downstream signaling pathways, including the MAP
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br Experimental Procedures br Acknowledgments br Introductio
2020-01-09
Experimental Procedures Acknowledgments Introduction Bisphenol A (BPA), 2,2-bis (4-hydroxyphenyl) propane, is widely used to manufacture consumer products including food and beverage containers (Vandenberg et al., 2007). It can be accumulated in human body via leaching from the polymers int
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br Thy nephritis is one of the most commonly
2020-01-09
Thy1.1 nephritis is one of the most commonly used models to study the course of immunoglobulin A and other mesangioproliferative nephropathies. To date, most of the studies have focused on mesangial and, to a lesser extent, endothelial cell recovery following capillary damage, whereas data concern
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Cryoprotectant equilibration and the response to ice concent
2020-01-08
Cryoprotectant equilibration and the response to ice concentrated media are the two facets of cellular cryobiological protocols most commonly covered by mathematical modeling. In these models, Celecoxib are typically assumed to have uniform, spatially independent extracellular concentrations and te
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