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In conclusion we designed novel E
2020-12-30

In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and ,
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HEK cells stably transfected with CysLT
2020-12-29

HEK-293 beta lactamase inhibitor 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 endocyt
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These cognitive deficits may suggest
2020-12-29

These cognitive deficits may suggest that cognitive therapy and pharmacotherapy for gambling behavior may ultimately wish to consider genotyping as a means of better targeting treatment approaches. If core cognitive deficits are shown consistently in certain subgroups of gamblers based on genotype,
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Although the presence of at least one
2020-12-29

Although the presence of at least one triple helix domain is typically the collagen signature, collagens are modular proteins composed of a succession of collagenous (COL) and non-collagenous domains (NC) that are both involved in collagen functions and in receptor binding. COL domains are linked by
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R406 free base Chk and Chk are functionally redundant protei
2020-12-29

Chk1 and Chk2 are functionally redundant protein kinases that respond to checkpoint signals emanating from the phosphatidylinositol 3-kinase family members ATM (ataxia-telangiectasia mutated) and ATR (Ataxia-telangiectasia and Rad-3 related). A concerted research effort has revealed many mechanistic
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dacomitinib For the current studies we used
2020-12-29

For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce
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br Materials and methods br Results
2020-12-29

Materials and methods Results and discussion Concluding remarks Together, the results of the theoretical kinetic simulations and of the analysis of the experimentally determined kinetic data of SoBADH performed in this work show that ignoring substrate inhibition causes potentially importan
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OxLDL down regulates eNOS and
2020-12-29

OxLDL down-regulates eNOS and up-regulates iNOS, thereby augmenting the formation of NO and protein S-nitrosylation in human endothelial neomycin sulfate [26]. Importantly, iNOS-mediated S-nitrosylation plays an increasingly significant role in cardiovascular diseases [34]. For example, iNOS-mediat
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Introduction Proteins play an important
2020-12-29

Introduction Proteins play an important role in cellular functions; however, being and remaining properly folded is necessary for their function. Understanding the stability of the protein is necessary to investigate the folding of proteins, as well as their conformation, functions and interactions
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Similar to EGFR another receptor tyrosine
2020-12-29

Similar to EGFR, another receptor tyrosine kinase (RTK), fibroblast growth factor receptor 4 (FGFR4), is gaining attention in the lung cancer setting. The protein expression of this receptor has been recently associated with a negative impact on lung cancer prognosis, supporting the idea that FGFR4
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Although our knowledge of the biochemical
2020-12-29

Although our knowledge of the biochemical and biological functions of E3 ubiquitin ligases has increased in B-cell malignancies, a deeper characterization of cell-context dependent substrate regulation and biological relevance is needed. The recent approval of a general proteasome inhibitor, VELCADE
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br Introduction In most of the
2020-12-29

Introduction In most of the angiosperms, sexual reproduction requires a process called double fertilization where the specialized cell division called meiosis produces haploid gametes combine to form diploid (2n) embryo. In CPI-169 to this, apomixis, naturally occurs in at least 400 plant familie
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br Materials and methods br Results br
2020-12-29

Materials and methods Results Discussion Although autophagy is known to be implicated in the therapeutic effect of DNA alkylating agents such as MNNG [28], [29], [30], the molecular mechanisms underlying autophagy induced by MNNG remain largely elusive. In this study, we present evidence sh
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br As DAPK is dependent
2020-12-29

As DAPK1 is dependent on Ca2+/CaM for its activity, its role in induction of autophagy is Ca2+-dependent and will be described in Section 5.1. LRRK1 and 2 were however shown to regulate autophagy in numerous studies where the role of Ca2+ was not investigated, and these mechanisms will be describe
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Doripenem In frame exon skipping of COL A has been suspected
2020-12-28

In frame exon 41 skipping of COL6A3 has been suspected to be responsible for isolated dystonia in several human kindreds without muscular defects [94]. In order to validate their hypothesis, the authors used zebrafish to selectively knock down several exons in col6a3 and found a negative impact on m
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