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The ability of minor groove binding agents
2021-04-09
The ability of minor groove binding agents to inhibit the activity of DNA helicases is not without precedence. Similar effective inhibition of the unwinding of DNA by the BLM and Werner's DNA helicases by the minor groove binder distamycin A has been observed. Further, and similar to RecBCD, interc
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A phenylacetic acid derivative discovered in a high throughp
2021-04-08
A phenylacetic ML 141 derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM (). Compound also inhibited CRTH2 mediated cell
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The intricate roles and neural systems and mechanisms
2021-04-08
The intricate roles and neural systems and mechanisms involved in the CRF1 and CRF2 mediation of spontaneous and stress-induced anxiety behavior remain to be defined. Of particular relevance are studies evaluating the behavioral actions of CRF1 and CRF2 receptors separately as well as together. For
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Preliminary studies evidenced the presence of CRFr
2021-04-08
Preliminary studies evidenced the presence of CRFr in gamma-aminobutyric acid-ergic (GABAergic) neurons of the hippocampus (Yan et al., 1998). In fact, in this Ibandronate sodium area, CRF inhibits glutamate release through CRF1r (Bagosi et al., 2015), leading to a decrease in the GABA concentration
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Collectively these data suggest the potential clinical utili
2021-04-08
Collectively, these data suggest the potential clinical utility of COMT inhibitors for the treatment of addiction disorders. Similar to current pharmacotherapies such as naltrexone, tolcapone's effects were not ethanol specific, therefore tolcapone may be effective in reducing other drug reinforced
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Mass spectrometry has previously been used to examine the pr
2021-04-08
Mass spectrometry has previously been used to examine the presence of Hyp in recombinant collagen, using hydrolysates to identify the individual imino acid, equivalent to an amino hedgehog signaling analysis [33], and also by analysis of mass changes to tryptic peptides [34]. The present study, how
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br Acknowledgements We would like to thank Dr Ron Mason
2021-04-08
Acknowledgements We would like to thank Dr Ron Mason (NIEHS, Research Triangle Park, NC) for helpful discussion regarding the analysis of CCl4 metabolism, to Dr Karla Thrall and Dr Rick Corley (Battelle) for helpful discussions regarding study design and data interpretation, and to Jim Merdink an
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The in vitro enantioselective metabolism of pesticides has
2021-04-08
The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective
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br Results br Discussion Oxysterols and EBI have received gr
2021-04-08
Results Discussion Oxysterols and EBI2 have received growing attention in the field of immunology, with works highlighting an important role for EBI2 in immune cell migration. However, these studies are mainly limited to animal models (Chalmin et al., 2015, Hannedouche et al., 2011, Kelly et a
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In this study we implicate SCFFBXO
2021-04-08
In this study, we implicate SCFFBXO3 E3 ligase as a critical modulator of inflammation in atherosclerosis and demonstrate the efficacy of a small molecule FBXO3 inhibitor in suppressing inflammatory responses important in atherosclerosis. Specifically, individuals carrying a hypofunctioning genetic
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br Discussion The regulation of intracellular cholesterol
2021-04-07
Discussion The regulation of intracellular cholesterol levels is a biological process of vital importance for cellular function and integrity, and involves robust transcriptional and post-transcriptional mechanisms that are sensitive to metabolic feedback control. Amongst post-transcriptional mec
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br Abbreviations br Acknowledgements br Introduction Dopamin
2021-04-07
Abbreviations Acknowledgements Introduction Dopamine β-hydroxylase (DbH) is the enzyme catalysing the conversion of dopamine to norepinephrine, two important neurotransmitters involved in the central nervous system [1]. This enzyme has been isolated from bovine chromaffin granules as a tetr
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br Regulation of DGK activity Activation of the
2021-04-07
Regulation of DGK activity Activation of the DGKs is complex and unique for each DGK isotype. In most cases, DGKs must translocate to a membrane compartment to access DAG. However, translocation does not necessarily activate the enzyme [57]. In addition, DGK activity can be modified by other cofa
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Pyronaridine Tetraphosphate Aldehyde dehydrogenase has been
2021-04-07
Aldehyde dehydrogenase has been characterized as a cancer stem cell marker, which plays a key role in various biological processes in tumor, including cell proliferation, invasiveness and chemoresistance. Recent data of Abourbih et al reported that ALDH1 expression did not correlate with primary tum
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The first transcription factor TF known to interact with one
2021-04-07
The first transcription factor (TF) known to interact with one of the cis-acting GAREs is GAMYB protein, the expression of which is induced by GA in the aleurone OSI-930 of barley (HvGAMYB) (Gubler and Jacobsen, 1992). GAMYB is an important regulator of endosperm functions during seed development a
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