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br Results and Discussion br Experimental Procedures br Ackn
2021-06-11
Results and Discussion Experimental Procedures Acknowledgments The ubiquitin–proteasome system (UPS) is important for biological processes such as protein degradation and protein function regulation. In general, poly-ubiquitinated proteins are degraded by proteasomes, and some proteins ac
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UBA belongs to the non canonical E enzymes that
2021-06-11
UBA5 belongs to the non-canonical E1 enzymes that lack a defined Cys domain but have the active-site Cys within the adenylation domain [24]. Similar to other E1 enzymes, UBA5's adenylation domain comprises an eight-stranded beta sheet that is surrounded by helices [21]. Moreover, like the ancestral
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One of the critical functions
2021-06-11
One of the critical functions of the product of the AR gene is to activate the expression of target genes. This transactivation activity resides in the N-terminal domain of the protein encoded in exon 1, which contains polymorphic repeats. These trinucleotide repeats, (CAG) and (GGC), encode polyglu
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The discoidin domain receptors DDR and DDR are receptor
2021-06-10
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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To overcome problems with the biochemical reconstitution of
2021-06-10
To overcome problems with the biochemical reconstitution of these heterodimeric cytokines fusion strategies linking both subunits together have been proposed inspired by the “hyper-IL-6” [28]. Much like fusing a protein to a solubility enhancing protein such as MBP or SUMO, fusing two subunits of a
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br Materials and methods br Results br
2021-06-10
Materials and methods Results Discussion In this study we characterized in more detail the interrelationship between the expression levels of the B. malayi Bm-cpl-3 and Bm-cpl-6 cysteine proteases and the fitness of Wolbachia, and consequently that of the parasite. Our present in vitro data
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br Materials and methods br Results br Discussion In
2021-06-10
Materials and methods Results Discussion In this study, we developed a new CysLT1 and CysLT2 receptors-mediated umbelliferone guinea pig model for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. Unlike human CysLT2 receptors, which are equally stimulated by both LTC4 and
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Steady state mRNA levels of CYP
2021-06-10
Steady-state mRNA levels of CYP3A isoforms were not changed during liver insufficiency. Suppression of these isoforms was observed only at the protein and activity levels, suggesting a nongenomic mechanism of CYP3A isoform downregulation during liver insufficiency. Nonetheless, transcriptional activ
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Introduction Globally lung cancer has
2021-06-10
Introduction Globally, lung cancer has the highest morbidity and mortality rates of all types of cancer, with 1.5 million patients newly diagnosed annually [1]. Approximately 85% of lung cancer cases are non-small cell lung cancer (NSCLC) [2]. The first-line treatment for NSCLC is surgical resectio
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In the course of our
2021-06-10
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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Where a a a and
2021-06-10
Where a, a, a and b, b, b are respectively, repulsive friction constants and attraction friction constants. c represents the quadratic repulsive friction constant and P is critical pressure (bar). CPA equation of state CPA model is an EOS that simply combines a cubic EOS (SRK-EOS) and an associ
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In our ongoing investigation of the structure activity
2021-06-10
In our ongoing investigation of the structure activity relationship of benzenesulfonamide anti-inflammatory activity, we designed and synthesized a novel set of benzenesulfonamide derivatives starting from commercially available sodium saccharin. The pivotal features of our approach aimed to do some
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Two additional hydrogen bonds are formed by the substituted
2021-06-10
Two additional hydrogen-bonds are formed by the -substituted methoxy-group with Ser and Asp. Ser exerts the role of a gate keeper in CK1: Entry of the ATP in the binding-site causes a conformational change into the closed form by Ser, which locks the binding-site and prevents ATP-diffusion out of th
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The most common adverse events in relation to udenafil
2021-06-10
The most common adverse events in relation to udenafil treatment are headache and facial flushing; other possible adverse events are febrile sensation, dyspepsia, and visual disturbances. No severe adverse event related to udenafil has been reported thus far. The adverse event rate recorded in the p
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SIN-1 chloride br Materials and methods br Results br Discus
2021-06-10
Materials and methods Results Discussion In this study, the N&B analysis showed new evidence regarding the proportion and the oligomerization state of the AT1 and the ETA receptors near or on the plasma membrane. Althought, preliminary studies suggest that the AT1 and the ETA receptors occu
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