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In the context of E
2021-01-11
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 Val
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In the present study we used
2021-01-11
In the present study, we used linagliptin, one of the commercially available DPP-4 inhibitors, because it has more long-lasting inhibition of DPP-4 activity than other drugs of this class. We hypothesized that linagliptin may interact with intercellular components, not only with DPP-4 on the plasma
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If the factors needed for A NHEJ are not completely
2021-01-11
If the factors needed for A-NHEJ are not completely defined and the A-NHEJ reaction mechanism nebulous, it is also fair to say that the biological role(s) of A-NHEJ is even more poorly understood. Most of the current interest in A-NHEJ, however, stems from its implicated use in the chromosomal trans
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Because of the complexity of DNA damage
2021-01-11
Because of the complexity of DNA damage and its repair, several pathways are candidates in HN2-induced DPC repair. Considering the 23kDa molecular weight of MGMT, NER may be ineffective for MGMT-adduct removal. This presumption is supported by that the mRNA level of ERCC1, a core gene in NER pathway
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Significantly less is known about regulation of phytocystati
2021-01-11
Significantly less is known about regulation of phytocystatin gene expression. A genomic clone corresponding to the barley cystatin Icy gene has been characterized (Gaddour et al., 2001) and the function of its promoter region has been analysed by Martínez et al. (2005b). Bioinformatic analysis of t
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The sex dimorphic expression of
2021-01-11
The sex-dimorphic Zafirlukast of mouse CYP3A is partially due to sex-dimorphic plasma GH profile which is a decisive factor in the regulation of sexspecific CYP isoforms [14]. Nevertheless, in our study we did not observe any changes in plasma GH levels in either mouse sex with a selective ablation
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br Acknowledgement This work was supported by grant
2021-01-11
Acknowledgement This work was supported by grant form EU (FP7 grant agreement no.: 266033 SPonge Enzyme End Cell for Innovative AppLication-SPECIAL). Introduction Prolyl 4-hydroxylases (P4Hs) have central roles in the synthesis of collagens and the regulation of oxygen homeostasis [1]. The po
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The cholinergic system has been
2021-01-11
The cholinergic system has been shown to play a role in regulation of the inflammatory response [13] as well as in the influence of the metabolism of PCa cells [14]. The reduced activity of cholinesterase (ChoE) and the consequent increased amount of histamine receptor antagonist has been shown to l
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Recent studies have shown that some CLC genes
2021-01-11
Recent studies have shown that some CLC genes participate in plant salt tolerance and have speculated that they function by mediating Cl− transport across the tonoplast. For instance, AtCLCc, a vacuolar anion transporter, is shown to be involved in the regulation of stomatal movement and to contribu
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br Results br Discussion The
2021-01-11
Results Discussion The nitric oxide-cyclic guanosine monophosphate pathway plays an important role in normal EF, and oral PDE-5Is were developed in the late 90s after the discovery that ED occurs when there is a problem with this pathway. Since then, several PDF-5Is with different pharmacokine
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Kinetic isotope effects KIEs inform on bond vibrational
2021-01-11
Kinetic isotope effects (KIEs) inform on bond vibrational changes between the ground state (GS) and TS of a chemical reaction and remain one of the most powerful experimental techniques for interrogating TS structure. KIEs on enzyme reactions measured by the internal entospletinib synthesis of labe
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br Target enzyme attributes and substrate peptide selection
2021-01-11
Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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For most enolases fluoride acts as an
2021-01-11
For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby
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Because sex steroids and growth hormone play
2021-01-11
Because sex steroids and growth hormone play an important role in the development and maintenance of hepatic CYP450 enzyme expression and ER expression, it is possible that exposure to endocrine active agents during gestation and perinatally could alter expression of these proteins. Therefore, these
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Using the juxtarenal PPE the induction of juxta and supraren
2021-01-11
Using the juxtarenal PPE, the induction of juxta- and suprarenal aneurysms is described herein (Fig. 3A). The infra-/suprarenal part of the Cy5.5 maleimide (non-sulfonated) receptor can now be investigated separately, taking into account different embryological backgrounds and varying reactivity to
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