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Artificial permutations have also been
2021-08-23
Artificial permutations have also been exploited by protein engineering to manipulate protein scaffolds, in order to improve catalytic activity, alter substrate or ligand binding affinity, reduce proteolytic susceptibility, increase stability, generate different aggregation states and improve fluore
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Main Text Post translational modifications by ubiquitin Ub a
2021-08-23
Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p
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External factors such as protein partners can also activate
2021-08-23
External factors, such as protein partners, can also activate DUBs by either reinforcing the stimulatory effects of intramolecular factors or by other means. The intramolecular activation of the USP7 CD by its HUBL domain is allosterically potentiated by external factor GMP synthase (GMPS), which co
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Pol is responsible for the
2021-08-20
Pol ε is responsible for the bulk of leading-strand synthesis in vivo (Daigaku et al., 2015, Nick McElhinny et al., 2008, Pursell et al., 2007) and physically associates with CMG (Langston et al., 2014, Sengupta et al., 2013, Sun et al., 2015, Zhou et al., 2017). Furthermore, leading-strand synthesi
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br Experimental section br Author contributions br Acknowled
2021-08-20
Experimental section Author contributions Acknowledgements Introduction Many substance p in cells are sequential enzymatic reactions where the product of one enzyme serves as the substrate of a second enzyme (1, 2). Experimental evidence suggests that some of these consecutive enzyme-ca
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The CysLT receptor antagonist BayCysLT
2021-08-20
The CysLT2 receptor antagonist BayCysLT2RA significantly suppressed multiple antigen challenge-induced infiltration of eosinophils and mononuclear pd184352 australia into the lung, indicating that CysLT2 receptor activation is involved in leukocyte migration. In contrast to the present finding, Bar
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In the present study we used a
2021-08-20
In the present study, we used a new luminescent method to measure CYP activity with Luciferin-ME as a substrate which is used for wide ranges of mammalian CYPs, including CYP1A2, CYP2C8, CYP2C9, CYP2J2, CYP4A11, and CYP4F3B. As a result, no significant modulations of CYP activities in B[a]P exposure
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br CDK Inhibitors for the Treatment
2021-08-20
CDK Inhibitors for the Treatment of inflammatory Diseases Several CDKs have been implicated as regulators of inflammatory gene expression. It will thus be very important to determine the relative contributions of the various CDKs and their kinase function on a systematic basis. This work will be
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Citrus comprising some of the
2021-08-20
Citrus [29], comprising some of the most widely cultivated fruit crops worldwide, has been consumed as a food and dietary supplement. According to traditional Chinese medicine, dry pericarp of Citrus, as a Chinese herbal remedy, is capable of regulating Qi and expelling phlegm, and has been used to
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Propidium iodide Sensory gating describes a filter mechanism
2021-08-20
‘Sensory gating’ describes a filter mechanism protecting the central nervous system from sensory overload by inhibiting behaviorally irrelevant input (Boutros et al., 2004, 2008). This permits Propidium iodide to a changing contextual environment (Fruhstorfer et al., 1970; Grunwald et al., 2003). A
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CK enzymes belong to a conserved family of
2021-08-20
CK1 enzymes belong to a conserved family of serine/threonine protein kinases that plays an important and diverse role in vesicular trafficking, DNA repair, 3,4-DAA receptor progression and cytokinesis in organisms from yeast to humans [15]. In multicellular organisms CK1 enzymes also regulate develo
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This structure guided the variation of the compounds aiming
2021-08-20
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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The present study sought to determine if chlorodifluoroaceto
2021-08-20
The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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Namely the NOESY cross peaks
2021-08-20
Namely, the NOESY cross-peaks between H-7″ methylene protons ( 4.01 and 4.16) with H-6′ ( 6.76) revealed that H-2 and OH-3 are -orientated, which indicated that the relative configuration of the C2 and C3 substituents as . For the -isomers, the thermodynamically more stable conformation is when H-2
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To our knowledge this is the first report
2021-08-19
To our knowledge, this is the first report of an oncocytoma expressing alpha-enolase or causing autoimmune retinopathy and optic neuropathy. Although generally considered benign, oncocytomas have rarely been associated with paraneoplastic syndromes, including tumor-induced hypertension, erythrocytos
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