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The RING domain was previously considered sufficient to conf
2021-04-15
The RING domain was previously considered sufficient to confer ubiquitination by RING-type E3 ligases. However, recent reports have shown that sequences closest to the RING domain are also important in E3 ligase function. Residues like Tyr193 in RNF4 [40], Phe296 and Arg294 in BIRC7 [31], and Lys65
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br RING type E s
2021-04-15
RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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A range of inhibitors were therefore synthesized containing
2021-04-14
A range of inhibitors were therefore synthesized containing either carboxylic Biotin-16-dCTP or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively (). Analys
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Quetiapine Fumarate The discoidin domain receptors DDR and
2021-04-14
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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orphan receptor It is worth mentioning that in this
2021-04-14
It is worth mentioning that, in this study we only observed the responses of CYP450 to the short-term exposure of DSP toxins (12 h). However, the toxic effects of DSP toxins to bivalves appeared to abate with longer exposure (Pinto-Silva et al., 2005; Flórez-Barrós et al., 2011; Prego-Faraldo et al.
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NECA Bovine collagen type II a
2021-04-14
Bovine collagen type II, a fibrillar collagen mainly found in cartilage, comprises 24 potentially glycosylated lysine residues within its collagen domain. Detailed analysis revealed that 22 out of 23 of these lysine residues are hydroxylated and carry variable numbers of Gal(β1-O) and Glc(α1-2)Gal(β
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br Casein Kinase II CK Casein Kinase II
2021-04-14
Casein Kinase II (CK2) Casein Kinase II (CK2) is a ubiquitous serine/threonine-selective pro-oncogenic protein kinase that has become a more prominent target for research due to its effects and key role in tumorigenesis (Gowda et al., 2017a, Pinna, 2002). CK2, a well-conserved, pleiotropic kinase
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br Conclusions Enzyme prodrug therapy mediated by implantabl
2021-04-14
Conclusions Enzyme prodrug therapy mediated by implantable biomaterials combines the benefits offered by the site specific drug delivery techniques and the systemic administration of drugs. From the former, SMEPT inherits the localized mode of drug delivery with lower systemic distribution of the
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The human serotonin hydroxytryptamine HT
2021-04-13
The human serotonin (5-hydroxytryptamine; 5-HT) receptor family consists of 14 receptor subtypes to date, which are primarily G protein-coupled receptors (GPCRs) with 5-HT3 being the sole ligand-gated ion channel (Alexander et al., 2017). These receptors are widely distributed in the central and per
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1530 The outcome of DGK function
2021-04-13
The outcome of DGK function will thus depend on the binding partners of each DGK isoform, and the effects that they exert can be quite different. A clear example of this concept has been demonstrated for the type IV DGKs, ζ and ι, which are structurally very similar but have opposing effects on Ras
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As part of a program to explore
2021-04-13
As part of a program to explore the key binding interactions between the core of 1 and DGAT-1 a systematic analysis of the aminopyrimidine subunit was initiated. A potential approach to improving passive permeability within this series would be to increase lipophilicity via incorporation of substitu
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br Introduction The discoidin domain
2021-04-13
Introduction The discoidin domain receptors (DDRs), DDR1 and DDR2, are unique among the receptor tyrosine kinases (RTKs) in being activated by interaction with the extracellular matrix [1], [2]. Binding to triple-helical collagen is mediated by the receptor extracellular domains that include an N
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br Materials and methods br Results br Discussion
2021-04-13
Materials and methods Results Discussion NB has been shown to induce cancers in many tissues including the kidney, liver, and thyroid, following chronic inhalation in animals (Hsu et al., 2007). The available data indicate that a lager majority of studies on NB evaluate the effects of toxic
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Another breakthrough towards the understanding of the mechan
2021-04-13
Another breakthrough towards the understanding of the mechanisms responsible for stress-induced relapse to drug seeking behaviour is the evidence published by the group of Wise [34] in which they show that the activation of VTA CRF2 and not CRF1 receptors is responsible for stress-mediated relapse t
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Taken together our results demonstrate
2021-04-13
Taken together, our results demonstrate that the changes of striatal dopamine release and locomotor activity observed following chronic nicotine treatment and consequent acute withdrawal are mediated by CRF1, but not CRF2. Previous studies have already indicated that blocking CRF1 would prevent some
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