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In the present work we
2021-06-28
In the present work, we have investigated the reactivity of N-aryl-N′-hydroxyguanidines 1a–d (see Scheme 1 for structures) with the water-soluble Cu(II) complex 8. Using EPR and UV–Visible spectroscopy, we have shown that the studied N-aryl-N′-hydroxyguanidines 1a–d can bind and transfer electrons t
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In this study using REMD with the crystal environment
2021-06-28
In this study, using REMD with the crystal environment, we investigate the effect of cryo-cooling on the crystal structure of Escherichia coli DHFR. DHFR is an important model enzyme (for review, see, e.g., (30)), and has been studied for decades (31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43).
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The secondary objective of the present study was
2021-06-28
The secondary objective of the present study was to evaluate the pharmacokinetics, safety, and tolerability of multiple oral doses of 450-mg delafloxacin to reach steady state in healthy male and female subjects. After multiple dosing of oral delafloxacin, steady state was reached after 4 days of do
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The significant CRF increase in the
2021-06-28
The significant CRF increase in the DS and the overall changes in the CRF system observed in the VM and DS during the development of sensitization suggest that this neuropeptide (and possibly urocortin) contributes to the specific molecular alterations occurring in the mesolimbic pathway that suppor
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On top of the hardware ASTS employs
2021-06-28
On top of the hardware, ASTS employs Linux SUSE with High-Availability (HA) Extension: a COTS OS provided with two clustering software (Pacemaker Cluster Resource Manager (CRM) and Corosync) responsible for resources orchestration, failure diagnosis, nodes coordination, and fail-over management. The
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br Steroid biosynthesis br Steroid hormone metabolism in
2021-06-25
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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Four m thick sections of formalin fixed paraffin embedded ti
2021-06-25
Four-μm thick sections of formalin-fixed paraffin-embedded tissue samples from uterine cervical cancers were cut with a microtome and dried overnight at 37 °C on a silanized-slide (Dako, Carpentaria, CA, USA). The protocol of the universal Dako Labeled Streptavidin–Biotin kit (Dako) was followed for
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The question remains however as
2021-06-25
The question remains, however as to the downstream signaling by Epacs that contributes to persistent sensitization of sensory neurons. Activation of the Ras family of GTPases by Epac1 (RapGEF3) or Epac2 (RapGEF4) (Bos, 2003, de Rooij et al., 1998) is linked to a number of downstream signaling effect
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To develop novel EPAC inhibitors Zhou and co workers optimiz
2021-06-25
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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We can think of two ways
2021-06-25
We can think of two ways in which collagen binding could activate DDR (Figure 8). A single collagen triple helix could interact with both DS domains in the DDR dimer (“composite binding site”) and thereby activate the receptor, similar to the situation exemplified by the growth hormone-growth hormon
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Mouse Cyp a is a homologous isoform of the
2021-06-25
Mouse Cyp3a11 is a homologous isoform of the human CYP3A4 gene, and both are highly expressed in the liver (Hart, Cui, Klaassen, & Zhong, 2009). CYP3A4 is the most abundant CYP450 in hepatic microsomes responsible for drug and xenobiotic metabolism (Zanger & Schwab, 2013), and it is the most active
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The concept of GPCRs and
2021-06-25
The concept of GPCRs and EGFRs existing as heteromers is consistent with previous studies. Co-immunoprecipitation studies have shown that agonist stimulation (both AngII and EGF) promotes a multi-protein complex containing the AT1R and EGFR, however these endpoint assays were not in live cells or in
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br Rationale and hypothesis To discover an allosteric
2021-06-25
Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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EBI and its ligand s EBI was found
2021-06-25
EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines
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br Experimental Procedures br Author Contributions br
2021-06-25
Experimental Procedures Author Contributions Acknowledgments We acknowledge Géraldine Le Goff and Mathieu Canales for blood sampling, Cécile Gameiro and Jean-Pierre Aubry for flow cytometry technical assistance, Giuseppe Pantaleo for support, and Britta Engelhardt, Gisella Puga-Young, Nicol
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