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The in vitro enantioselective metabolism
2019-11-04
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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In contrast to SQLE HMGCR could
2019-11-04
In contrast to SQLE, HMGCR could be efficiently degraded in LY 2157299 synthesis lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with o
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Recent studies have reported that
2019-11-02
Recent studies have reported that miR-454 plays an important role in various cellular processes and diseases, such as inflammation, infection, osteogenic differentiation, and cancers [25,27,29,30]. Multiple evidence has documented that miR-454 promotes the proliferation, migration and invasion, and
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In addition PK studies on
2019-11-02
In addition, PK studies on indicate that it displays excellent bioavailability, pharmacological and toxicological parameters., A concern was initially raised about compound that it may cause EPAC denaturing properties and false positives. To address this issue, Cheng and co-workers have conducted
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In the present study we
2019-11-02
In the present study, we found that the up-regulatory effects of androgens on ep1 transcripts might be mediated by Arα in the olfactory rosette of B. sinensis. However, in mammals, there is no evidence of AR expression in either the vomeronasal organ or the sensory epithelium of main olfactory epith
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br Summary and perspectives In recent decades enormous advan
2019-11-02
Summary and perspectives In recent decades, enormous advances have been achieved in the development of enzyme-activatable imaging probes, enabling the accurate detection of enzyme activity in vivo to better understand the biological function of enzymes in disease processes. Activatable probes are
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2-APB The RING domain was previously considered sufficient t
2019-11-02
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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pkm2 Intriguingly one E residue may serve
2019-11-02
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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Verapamil a calcium channel blocker used clinically as a
2019-11-02
Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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A summary of the drug CDK hydrophobic hydrogen bonding H
2019-11-02
A summary of the drug-CDK2/6/9 hydrophobic (Φ), hydrogen-bonding (H), and polar-bonding (P) interactions based upon the KLIFS residue numbers is provided in Table 5. The KLIFS system gives comparable residues from different Deoxynivalenol the same value [77], which facilitates comparisons among dif
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Phylogenetically three related CXC chemokines are classified
2019-11-02
Phylogenetically three related CXC chemokines are classified as the possible ligands for the teleost CXCR1 and CXCR2. They are referred to as CXCL8_L1 (CXCL8/IL-8/CXCa), CXCL8_L2 (CXCc) and CXCL8_L3 (Alejo and Tafalla, 2011, Chen et al., 2013, Laing et al., 2002, Laing and Secombes, 2004, Nomiyama e
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In the preclinical evaluation of CRF receptor
2019-11-02
In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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Abha et al reported Natural coumarinolignoids isolated from
2019-11-02
Abha et al. reported Natural coumarinolignoids isolated from the seeds of Cleome viscosa consist of a racemic mixture of cleomiscosins A 19, B 20 and C 21 and were screened for anti-inflammatory activity through mol. docking and QSAR studies by using reported in vivo activity of Swiss albino mice. B
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Given the potency enhancing effect
2019-11-02
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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The main advantage of exploiting paper
2019-11-02
The main advantage of exploiting paper sludges as sources of cellulose-derived energy and chemicals in comparison to other lignocellulose substrates is their amenability, which is associated with an extensive pulping process that removes the majority of the lignin and exposes Simeprevir fibers to e
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