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Thus DGK active sites remain ill defined and
2021-05-11
Thus, DGK-active sites remain ill-defined and, combined with the lack of crystal structures for mammalian DGKs, have limited our understanding of substrate and inhibitor binding. As a result, current DGK inhibitors consist of compounds with poor specificity within the DGK superfamily (de Chaffoy de
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br Acknowledgements This work was
2021-05-11
Acknowledgements This work was supported by grants from Agence Nationale de la Recherche (ANR CAPHE) and from Ligue contre le Cancer. We acknowledge the continuous support of CNRS and the University of Strasbourg. We thank the technical assistance of the “Plateforme de Chimie Intégrative de Stras
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never In a cell based functional assay the antagonist proper
2021-05-10
In a cell-based functional assay, the antagonist properties of were assessed by measuring inhibition of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells. produced a concentration-dependent inhibition of CRF (1nM)-induced cAMP production with an IC
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Accurate equilibrium predictions of CO containing mixtures h
2021-05-10
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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Another significant finding in our study was the demonstrati
2021-05-10
Another significant finding in our study was the demonstration that the axon-protective action associated with CK2 inhibition correlated with preservation of mitochondrial structure and function in epacadostat (Fig. 11). Because of the consistent protection conferred by CK2 inhibition during OGD, i
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br Introduction br Conclusion br Acknowledgments and Funding
2021-05-10
Introduction Conclusion Acknowledgments and Funding Introduction Reversible protein phosphorylation is an important post-translational modification of proteins regulating many processes in the cell. Approximately one third of the cellular proteome is phosphorylated, and several sites are
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Besides the assessment of toxicological
2021-05-10
Besides the assessment of toxicological effects immediately after exposure, we also studied the potential recovery of the exposed organisms, through the quantification of ChE activity at specific time intervals after placing organisms in clean test medium. Recovery from chemical challenge, in this c
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The highest concentrations from several tens to
2021-05-10
The highest concentrations (from several tens to often hundreds or thousands ng/L) are reported in animal farm flush water, and associated runoffs and lagoons in China and in the U.S. Lower concentrations are reported in WWTP influents and effluents. In WWTP influent waters DRO, LNG, NET and PRG hav
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CHAPS receptor br Steroid biosynthesis br Steroid hormone me
2021-05-10
Steroid biosynthesis Steroid hormone metabolism in breast cancer Conclusion Steroid hormones elicit their biological actions primarily by binding to steroid receptors such as the ER, AR, PR and GR. Although classical breast cancer diagnostic panels assess the expression of the ER and PR, as
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br Introduction Maintaining the normal function of
2021-05-10
Introduction Maintaining the normal function of fetal trophoblasts is essential for a successful pregnancy. Preeclampsia (PE), a pregnancy-specific disorder, is often associated with excessive trophoblast cell apoptosis and superficial trophoblast invasion leading to insufficient spiral artery re
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The optimization of the lead compound was initiated and
2021-05-10
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic Adenine sulfate moiety with other functional groups led to loss of functional activity against EP4 recep
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br Enzyme activations Activated proteinases can unleash
2021-05-10
Enzyme activations Activated proteinases can unleash a deluge of tissue damage (Zucker et al., 2009). Once activated, the essential enzymes such as serine proteases and cysteine proteases cannot discriminate between self and non-self, burning away self-tissues (Chien et al., 2009, Laskar et al.,
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br Structure of USP Schematic representation
2021-05-10
Structure of USP7 Schematic representation of the USP7 domain architecture is shown in Fig. 3B. USP7 is a 135 kDa protein that consists of seven domains, including the N-terminal TRAF-like (Tumor necrosis factor Receptor–Associated Factor) domain, followed by the catalytic core domain and the fiv
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br ILCs anticipate neuronal derived factors
2021-05-10
ILCs anticipate neuronal-derived factors Recent studies have revealed that ILCs express receptors for neural peptides, thus enabling cross-talk with the peripheral nervous system. ILC3s express RET (Figure 2), which is a receptor for members of the glial cell-derived neurotrophic factor family of
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br RING dimerization RING type domains are found in
2021-05-10
RING dimerization RING-type domains are found in many different structural contexts. While many exist as single-chain Creatinine (Fig. 3A), a notable feature of RING-type E3s is their tendency to form homodimers and heterodimers (Fig. 3C–F). Homodimeric RING-type E3s include cIAP, RNF4, BIRC7 (s
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