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The authors identified inhibitors of SUMOylation
2020-07-14

The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u
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Cdc which is involved in filopodium
2020-07-14

Cdc42, which is involved in filopodium formation, and Rac1, which is involved in lamellipodium formation, engage in cross-talk with one another [25,26,30,31]. In general, filopodium formation precedes lamellipodium formation, and filopodium formation (Cdc42 activity) suppresses lamellipodium formati
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Are the hydrogens removed simultaneously or one by one
2020-07-14

Are the hydrogens removed simultaneously or one by one? — Δ1-KSTDs can catalyze the exchange of alkali-labile tritium or deuterium atoms at the C2 PP 3 receptor of their substrates, even when enzyme turnover was prevented by the absence of an electron acceptor for the oxidative half-reaction [97,98
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br Materials and methods br Results
2020-07-14

Materials and methods Results Discussion To our knowledge, this is the first large-scale longitudinal measurement of more than 20 cytokines in normal pregnancy. Simultaneous measurements of several cytokines with multiplex magnetic bead-based immunoassays are becoming increasingly common in
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The on target in vitro
2020-07-14

The on target in vitro pharmacology of 18 was then further explored, first in respect of murine CRTh2 receptor activity (Table 5), where similar levels of activity were found in both a binding and functional assay compared with the human orthologue, consistent with our earlier observations in the su
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The mechanism underlying the increased PON levels found
2020-07-14

The mechanism underlying the increased PON1 levels found in greenhouse workers may be accounted for by an increased protein G-15 following pesticide interaction with different nuclear receptors as also occurs with other chemicals, such as polyphenols and statins [28]. A number of nuclear receptors
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Trelagliptin Besides EGFR other tyrosine kinase receptors ar
2020-07-14

Besides EGFR, other tyrosine kinase receptors are currently gaining attention as potential therapeutic targets. Included among these is the fibroblast growth factor receptor (FGFR) family, which is involved in the progression of a variety of cancers.7, 8, 9, 10, 11 In lung cancer, fibroblast growth
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Within the BLA both CRF and the CRF
2020-07-13

Within the BLA, both CRF and the CRF1 receptor have been shown to functionally regulate synaptic activity. In vivo, CRF release into the BLA originates from projections from the CeA (Roozendaal, Brunson, Holloway, McGaugh, & Baram, 2002). Central administration of both CRF and CRF1 agonists has been
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Accurate equilibrium predictions of CO containing
2020-07-13

Accurate equilibrium predictions of CO2 containing mixtures, however, are challenging with traditional equations of state. The reason for this may be that CO2 has a large quadrupole moment. The large quadrupole moment of CO2, as well as size asymmetry, are for instance believed to be the reasons fo
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Among the various neurotransmitter systems pointed out to pl
2020-07-13

Among the various neurotransmitter systems pointed out to play a role in the mediation of defensive and antinociceptive responses elicited by environmentally aversive stimuli, the neuropeptide corticotropin-releasing factor or hormone (CRF or CRH) has attracted the interest of many researchers inves
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All known vertebrate TRIMs are
2020-07-13

All known vertebrate TRIMs are categorized in 11 distinct subclasses depending on the types of domains present at their carboxyl-terminals (Fig. 3) [29], [35]. Beyond conserved N-terminal domains, it is the C-terminal that provides specificity of interactions with other proteins. The subclass IV for
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Most enzymes involved in the addition and removal of ubiquit
2020-07-13

Most CGS 21680 involved in the addition and removal of ubiquitin bind weakly to an overlapping surface on ubiquitin. Previously, Sidhu and colleagues diversified this surface and then used phage display to screen these libraries of ubiquitin variants (UbVs) for binding to DUBs and E3 ligases (Ernst
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We also observed reduced insulinotropic effects after intrav
2020-07-13

We also observed reduced insulinotropic effects after intravenous administration of both GLP-1 and GIP with atropine, whereas no inhibition was observed by atropine of the direct effects of GLP-1 and GIP action on beta-cells in the islet experiments. This suggests that the reduction in circulating i
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In the current study cocaine did not significantly increase
2020-07-13

In the current study, cocaine did not significantly increase negative subjective effects and nepicastat did not increase these responses. This outcome is somewhat surprising given that the most commonly reported effect to date has been to increase the aversive properties of cocaine such as anxiety,
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br Conclusions There is significant interest in understandin
2020-07-13

Conclusions There is significant interest in understanding the contribution of biological mechanisms to the non-linear/bilinear dose–response curves for DNA-reactive agents. Model monofunctional alkylating agents have datasets amenable to PoD determination for genotoxic effects in both in vitro a
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