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Because of the important role of the
2020-04-06

Because of the important role of the DDB1-CUL4B interaction for CUL4B-based E3 ligases, disruption of the DDB1-CUL4B interaction could be an effective approach to treat cancer. Therefore, we developed an in vitro HTS assay based on yeast cell growth inhibition to identify compounds that could disrup
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hedgehog signaling ICT is a product of icariin via
2020-04-06

ICT is a product of icariin via the metabolism of intestinal bacteria with estrogen-like activities [33]. ICT as a bone-protecting agent can enhance osteoblast differentiation while suppressing osteoclastic differentiation in vitro [19], and stimulate osteogenic differentiation and inhibit adipogene
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In the course of carbohydrate metabolism pyruvate the end pr
2020-04-06

In the course of carbohydrate metabolism, pyruvate, the end product of glycolysis, is converted to acetyl-CoA, which fuels the citrate cycle for further generation of energy. In the case of elevated levels of acetyl-CoA, acetyl-CoA is converted into malonyl-CoA by the action of acetyl-CoA carboxylas
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br Experimental br Declaration of
2020-04-06

Experimental Declaration of interest Introduction Material and methods Results and discussion Conclusion By screening the NMR Picrotoxin library an initial hit was found for an inhibitor of the PPI between the α-β subunits of CK2 with an IC50 of 900 μM. This compound was modified a
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A number of chemical strategies have been developed to
2020-04-06

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 Conflict of interest br
2020-04-06

Conflict of interest Acknowledgements This work was supported by Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP: 2014/00926-3). Introduction The metacestodes of Taenia solium are the causative agent of cysticercosis, which mainly resides the skeletal muscles and the central n
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BRD 7552 In summary the metabolism of GEF in HLM and MLM
2020-04-06

In summary, the metabolism of GEF in HLM and MLM was extensively studied using a LC–MS-based metabolomic approach. This study identified a total of 34 metabolites and adducts related to GEF (Fig. 10) and identified three new potential reactive metabolites, including two aldehydes and one iminium. Pr
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In vitro studies in NSCLC cell lines expressing
2020-04-06

In vitro studies in NSCLC cell lines expressing EGFR mutants (T790M mutation, exon 19 deletion E746-A750, L858R/T790M double mutation), demonstrated that Rociletinib potently inhibits proliferation in the mutant EGFR NSCLC scr 11 with Growth inhibition (GI50) values ranging from 7 to 32 nmol/L. In
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br Introduction The protein Epidermal Growth Factor
2020-04-06

Introduction The protein Epidermal Growth Factor Receptor Tyrosine Kinase (EGFR-TK) play important role in non small-cell lung carcinoma (NSCLC) and vital therapeutic progress withinin the treatment of this ailment has revamped the past ten years through the exploitation of this insight (Mok et a
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One of the most fundamental distinctions between Ub signals
2020-04-06

One of the most fundamental distinctions between Ub signals is substrate monoubiquitination versus polyubiquitination. With the exception of the E2, UBE2W, which represents a special case because it (S)-Crizotinib only ubiquitinates the flexible N-termini of substrates [5], [6], [20], most examples
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In the original ELF study patients were considered eligible
2020-04-03

In the original ELF study [7], patients were considered eligible if they were due to undergo liver biopsy for the investigation of chronic liver disease, defined as abnormal biochemical liver function tests persisting for more than 6 months, ability to provide informed consent and age between 18 and
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The assessment process is even more difficult when Commercia
2020-04-03

The assessment process is even more difficult when Commercial-Off-The-Shelf (COTS) components – whose internals are partially or totally unknown – come into play. COTS are being increasingly used by the industry to reduce costs and to shorten development (and possibly deployment) time. However, sinc
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br Conclusion The past few
2020-04-03

Conclusion The past few years have witnessed substantial progress in understanding the structural mechanisms of substrate recognition and the reactions catalyzed by the O-GlcNAc-cycling enzymes, but more work remains. In particular, future research will be needed to establish how OGT and OGA inte
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Previous studies reported that NE
2020-04-03

Previous studies reported that NE and MHPG are deeply involved in depression and that NE reuptake inhibitors are approved for use in patients with depression (for review, see [2]). We found increased hippocampal content of NE and MHPG in the CORT-treated CRTH2−/− mice (Fig. 3). In the hippocampus, a
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br Methods br Results Our study focused on
2020-04-03

Methods Results Our study focused on consecutive postural adjustments (CPAs) between IS and BS (the shaded areas on Fig. 2); that is to say, the Rx kinetics that occur after the end of an upper limb movement. It was dedicated to examining the main features of CPAs and the influence of movement
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