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The role of Epac in the
2020-11-20
The role of Epac in the regulation of intracellular Ca homeostasis and contractility is still matter of debate. In rat adult cardiomyocytes, acute Epac stimulation decreased the amplitude of Ca transients [6], [9], [10] with either no changes [6] or increments [9] in cell shortening, suggesting an e
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In addition to providing substantial insight into substrate
2020-11-20
In addition to providing substantial insight into substrate recognition, structural studies have revealed important details about mechanisms of glycosylation and HCF-1 cleavage [28,30,33]. Activation of the nucleotide-sugar is accomplished through interactions of the β-phosphate with the N-terminus
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Compared to ET all agonists tested showed a fold
2020-11-20
Compared to ET-1, all agonists tested showed a 2–4 fold bias for the G protein constrictor assay compared to the β-arrestin assay (Table 1). This preliminary analysis indicated that at least modest pathway bias for endogenous ET peptides is possible, however the physiological significance of this, i
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br Abbreviations br Introduction br Collagen induced
2020-11-20
Abbreviations Introduction Collagen-induced DDR activation A key feature of DDRs is their ability to bind both fibrillar and non-fibrillar collagens (Shrivastava et al., 1997, Vogel et al., 1997). DDR1 and DDR2 recognize the GVMGVO (O, hydroxyproline) motif within fibrillar collagens I–III
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br Analytical improvements Since our review of Oxysterol
2020-11-20
Analytical improvements Since our review of “Oxysterol Metabolomes” in 2011 [7], there have been a number of improvements in analytical methods for the analysis of oxysterols and related compounds. McDonald and colleagues in Dallas have refined their LC-MS methods which are now applicable for ana
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These studies suggested that PV PVH might promote bone forma
2020-11-20
These studies suggested that PV/PVH might promote bone formation activities and/or inhibit bone resorption activities probably due to its anti-inflammation activity; however, the underlying mechanism remained unknown. Furthermore, it is unclear if PVH shows better activity than that of PV; this is i
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There is a functional ubiquitin association UBA domain at th
2020-11-20
There is a functional ubiquitin association (UBA) domain at the N terminus of MCPIP1. Liang et al. have discovered that MCPIP1 may be a deubiquitinase and defined a novel DUB domain of MCPIP1 [22]. Ubiquitin and deubiquitin modification emerge as the key mechanisms that regulate the virus-induced ty
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The repair pathway of DNA DSBs through HR and
2020-11-20
The repair pathway of DNA-DSBs through HR and the role of BRCA1 in repair kinetics by HR is also an important factor to unravel the radiation sensitization of novel small molecule inhibitors. The involvement of the breast cancer susceptibility gene 1 (BRCA1) in tumorigenesis and its role in facilita
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The Rev protein is a crucial
2020-11-20
The Rev1 protein is a crucial regulator of TLS activity because of its structural function [10]; therefore, we focused on Rev1 to investigate how Dot1/Rad53 function impinges on TLS-dependent mutagenic bypass of MMS-induced lesions. In particular, we examined Rev1 localization to chromatin by immuno
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BR stimulated PA formation via
2020-11-20
BR-stimulated PA formation via the DGK pathway might have many effects in regulation of cell metabolism. For example, PA originated from DGKs pathway plays important roles in activation of NADPH oxidases, thus turning on ROS signaling [23]. PA is also connected to regulation of respiration processes
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We have reported previously that
2020-11-20
We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHOD
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Some pyrimidine analogs are substrate based inhibitors that
2020-11-20
Some pyrimidine analogs are substrate-based inhibitors that bind to the dihydroorotate binding site, but most reported inhibitors of DHODH bind to the site occupied by the ubiquinone co-factor., , , , , , , , , , , , , , , , , X-ray crystallographic studies of inhibitor complexes with DHODH and DHOD
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Eosin Y Indeed a significant difference was observed
2020-11-19
Indeed, a significant difference was observed for the binding of glycated α-synuclein. Thus, g-α-synuclein bound to other part of GAPDH in 4 of 10 simulations (Fig. 2F, brown, yellow and dark-green chains, and Fig. 2G, brown chain). This additional binding site is located on the interface between O
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Introduction Cytochrome P CYP A is the most
2020-11-19
Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The Zebularine level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and toxicity. A m
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Stressful life events are modulators of mood and can trigger
2020-11-19
Stressful life events are modulators of mood and can trigger a variety of destructive behavior, including drug abuse and relapse in addicts (Association, 2013; Chen et al., 2012; Sinha, 2009). Likewise, drug-associated stimuli evoke a negative affective state in abstinent drug users. Compelling evid
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