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In addition we investigated if the previously reported papai
2020-12-08

In addition, we investigated if the previously reported papain inhibitor can inhibit rhodesain, and found that it was not active at inhibiting rhodesain. The vinyl sulfone analogue of () was then synthesized and tested, and it was also inactive towards rhodesain. We then determined the time dependen
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HEK cells stably transfected with CysLT were stimulated
2020-12-08

HEK-293 Swainsonine stably transfected with CysLT1 were stimulated with LTD and internalization was studied by confocal microscopy, FACS or cell-surface ELISA. Cells were co-transfected with wildtype and dominant negative (DN) mutants of arrestin and dynamin. Clathrin-mediated endocytosis was inve
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CDK lacks DNA binding domains and nuclear
2020-12-08

CDK6 lacks DNA-binding domains and nuclear localization sequences, and therefore will probably be transported to the nucleus by a ‘piggy-back’ mechanism and needs to contact its specific sites indirectly through DNA-binding proteins. Besides NF-κB p65, a further candidate transcription factor is PA
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In our preliminary evaluation of this
2020-12-08

In our preliminary evaluation of this series, we were surprised to discover that tranylcypromine mg was found to bind CSF-1R in a classical DFG-in binding mode (a). Dramatic conformational differences in the juxtamembrane domain and activation loops are apparent when this DFG-in structure is compa
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Indeed some studies that examined
2020-12-08

Indeed, some studies that examined the morphine response have reported that the (C) allele of rs4818 was associated with a low dose administered compared to that given for individuals with the (G) allele (Rakvag et al., 2008). In a publication about Tunisian patients with cancer by Chatti et al. (2
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The immune control of CMV replication in vivo
2020-12-08

The immune control of CMV replication in vivo is primarily driven by the T-cell-mediated response, a characteristic that has been proposed as a tool to individualize and therefore to optimize antiviral treatment [6], [7], and it has been associated with spontaneous clearance of CMV viraemia in patie
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The absence of an observable
2020-12-08

The absence of an observable time dependence of kobs on inhibitor concentration for TC-I 2000 australia 3 with AChE and compounds 1, 3 and 4 with BuChE parallels a similar absence of time dependence for some related fluoro ketones with AChE. Nair et al. found that trifluoromethyl acetophenones with
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Primary renal PNET was first
2020-12-07

Primary renal PNET was first reported by Seemayer et al in 1975. The possible etiology of rPNET is based on the theory of neural cell intussusception in the kidney during development that initiates the tumorigenesis. rPNET most commonly affects young adults, with a mean age of 30.4 years and male pr
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Protein ubiquitination occurs at the lysine residues and
2020-12-07

Protein ubiquitination occurs at the lysine residues, and is mediated by the sequential reactions of ubiquitin-activating enzyme (E1), conjugating enzyme (E2), and ligase (E3). The first step in this process comprises the ATP-dependent activation of ubiquitin by E1 to form a ubiquitin–E1 conjugate.
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Finally we assessed the utility of monitoring cfDNA in
2020-12-07

Finally, we assessed the utility of monitoring cfDNA in terms of predicting disease progression earlier than radiological progression. These patients may have a chance to receive subsequent chemotherapy before worsening symptoms. Although the number of the patients who experienced progression was re
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Downregulation of tumor suppressors is a major factor that
2020-12-07

Downregulation of tumor suppressors is a major factor that leads to tumorigenesis. Phosphatase and tensin homolog deleted on chromosome 10 (PTEN), a common tumor suppressor, the Oligomycin A of which is often downregulated or even absent in the majority of human cancers, functions as a phosphatase
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Our study provides proof of principle
2020-12-07

Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h
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In the context of E ligase drug discovery it
2020-12-07

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 MK
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br Conclusions br Acknowledgements br Introduction Liver
2020-12-07

Conclusions Acknowledgements Introduction Liver cancer was the fifth most common cancer and the second leading cause of cancer-related death worldwide [1]. Most of primary liver cancers (70–90%) occurring worldwide are hepatocellular carcinoma (HCC) [2]. Persistent hepatitis B virus (HBV) i
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br General Characteristics of the Type II Dehydrogenases Alt
2020-12-07

General Characteristics of the Type II Dehydrogenases Alternative NAD(P)H dehydrogenases conduct the reaction of the rotenone-insensitive oxidation of cytosolic and mitochondrial matrix NADH and/or NADPH (Fig. 1) (Melo et al., 2004, Rasmusson et al., 2004, Rasmusson et al., 2008). They catalyze t
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