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Some family I DNA ligases can
2020-12-22
Some family I DNA ligases can use dATP as nucleotide cofactor. For instance, human benzbromarone receptor I uses dATP with a catalytic efficiency that is only 36-fold lower in comparison to ATP [9]. EhDNAlig is unable to use dATP as a nucleotide cofactor, indicating a more constrained active site in
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Mitochondrial depolarization induced by DHODH inhibition
2020-12-22
Mitochondrial depolarization induced by DHODH inhibition (Figure 5A) may also contribute to the selective effects of DHODH inhibitors on KRAS mutant cells. If so, the effect may arise more from pro-apoptotic effects of mitochondrial depolarization (Lemasters et al., 1998) than from impaired oxidativ
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Hepatocyte proliferation is accompanied by changing gene exp
2020-12-22
Hepatocyte proliferation is accompanied by changing gene expression [1,2]. as two of the three estrogen receptors are transcription factors: Estrogen Receptor alpha (ERα) and ERβ [[3], [4], [5]]. The most potent ligand estradiol, binds to ERα/ERβ and exerts changing cognate gene transcription [5]. O
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br Benefits and risks of traditional combined oestrogen
2020-12-22
Benefits and risks of traditional combined oestrogen–progestogen HRT regimens Combined oestrogen–progestogen regimens were developed to reproduce the short- and long-term benefits of oestrogen replacement therapy (ERT) and to simultaneously provide appropriate protection against oestrogen-related
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Overall we found that all hormone treatment groups were
2020-12-22
Overall, we found that all hormone treatment groups were able to learn spatial working and reference memory tasks, as shown by their performance across days on the WRAM (days 2–12, collapsed across the 4 trials) and the MWM (days 1–5, collapsed across the 4 trials). During the acquisition phase of t
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Daptomycin The Ewing sarcoma breakpoint region gene EWSR is
2020-12-22
The Ewing sarcoma breakpoint region 1 gene (EWSR1) is a partner in a large, diverse range of mesenchymal (and some nonmesenchymal) tumors (Tables 1 and 2). As the 5′ partner, EWSR1 is able to fuse with an array of genes. These fusions can generate genetically different but phenotypically identical n
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hsp90 inhibitors Our previous high throughput screening HTS
2020-12-22
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based hsp90 inhibitors assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22
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A number of chemical strategies have been developed to desig
2020-12-22
A number of chemical strategies have been developed to design activatable optical imaging probes and have been summarized in several excellent reviews 11., 12., 13., 14., 15.. Fluorogenic enzyme substrates are one of the most explored activatable probe types for enzyme detection. These probes contai
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br Enzyme catalysis A biochemically spontaneous process proc
2020-12-22
Enzyme catalysis A biochemically spontaneous process proceeds in a direction where free nf-κb inhibitor of the system decreases. However, every spontaneous or energetically favorable reaction needs to overcome an energy barrier known as the activation energy barrier because of the formation of a
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Anaesthetized mice of one eNOS KO strain showed
2020-12-22
Anaesthetized mice of one eNOS-KO strain showed a paradoxical decrease in blood pressure (BP) in response to i.p. administration of the NOS-inhibitor L-NA suggesting a role for non-endothelial isoforms of NOS in maintaining BP [1]. Alternatively, diminution in the activity of the renin-angiotensin s
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The majority of serpins inhibit serine proteases but serpins
2020-12-22
The majority of serpins inhibit serine proteases, but serpins that inhibit caspases or papain-like cysteine proteases have also been identified [4], [5]. Inhibitory serpins are ‘suicide’ or ‘single use’ inhibitors that use a unique conformational change to inhibit proteases. This conformational tran
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br Materials and methods br Results br
2020-12-22
Materials and methods Results Discussion Studies have suggested that the Hh signaling pathway, which plays as an essential autocrine viability factor for MFBs [10], [11], is a potential therapeutic target for liver fibrosis. Previously reported works have proven the effectiveness of the Hh
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The development of C S mutation
2020-12-22
The development of C797S mutation has been reported in vivo in a small cohort (15 subjects) of EGFR T790M positive patients progressing after Osimertinib: this tertiary mutation was found, using a droplet digital PCR (ddPCR) assay, in 40% of patients after AR to this agent, while 33% of the cases ex
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Interestingly our analyses of human
2020-12-22
Interestingly, our analyses of human PBMCs using a monoclonal antibody against EBI2 showed that the expression pattern of human EBI2 is largely overlapping with that in mice. Especially Th17 ANA 12 showed homogeneous high expression of EBI2 compared with Th1 cells, which contained a fraction of cel
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Studies have focused on a hydrophobic
2020-12-22
Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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