Addressing a Trapped High-Energy Water: Design and Synthesis of Highly Potent Pyrimidoindole-Based Glycogen Synthase Kinase-3β Inhibitors by Stanislav Andreev (11067165)

“…Surprisingly, our results demonstrate that this high-energy water was not displaced by our potent inhibitor (<i>S</i>)-3-(3-((7-ethynyl-9<i>H</i>-pyrimido­[4,5-<i>b</i>]­indol-4-yl)­(methyl)­amino)­piperidin-1-yl)­propanenitrile (<b>(<i>S</i>)</b>-<b>15</b>, IC₅₀ value of 6 nM). Instead, only a subtle shift in the location of this water molecule resulted in a dramatic decrease in the energy of this high-energy hydration site, as shown by the WaterMap analysis combined with microsecond timescale molecular dynamics simulations. …”

Addressing a Trapped High-Energy Water: Design and Synthesis of Highly Potent Pyrimidoindole-Based Glycogen Synthase Kinase-3β Inhibitors by Stanislav Andreev (11067165)

“…Surprisingly, our results demonstrate that this high-energy water was not displaced by our potent inhibitor (<i>S</i>)-3-(3-((7-ethynyl-9<i>H</i>-pyrimido­[4,5-<i>b</i>]­indol-4-yl)­(methyl)­amino)­piperidin-1-yl)­propanenitrile (<b>(<i>S</i>)</b>-<b>15</b>, IC₅₀ value of 6 nM). Instead, only a subtle shift in the location of this water molecule resulted in a dramatic decrease in the energy of this high-energy hydration site, as shown by the WaterMap analysis combined with microsecond timescale molecular dynamics simulations. …”

Simultaneous silencing of isoamylases ISA1, ISA2 and ISA3 by multi-target RNAi in potato tubers leads to decreased starch content and an early sprouting phenotype by Stephanus J. Ferreira (4249219)

Effect of anti-miR-146a LNA or miR-146a mimic upon IL-1β-induced release of inflammatory molecules. by Anand Iyer (135705)

“…Data are expressed relative to unstimulated control cells (mean ± SEM from three separate experiments). In comparison with IL-1ß alone, cultures stimulated with IL-1ß and transfected with LNA-anti miR-146a exhibited significant increase of IL-6 and IP-10 release, whereas transfection of glial cells with miR-146a mimic significantly decreased the levels of IL-6, IL-8, G-CSF, IFN-γ, IP-10, MIP-1β, and TNF-α (* p<0.05). …”

miR-184 sensor expression across a range of tissues. by Sravya Paluri (5475260)

Decreased of downstream signalling protein phosphorylation and intracellular TNF-α production in GM-CSF treated CD14⁺ cells upon TLR ligand induction. by Kambis Sadeghi (3190407)

Estimates of the differencing parameter, d, in Eq (1). by Luis Alberiko Gil-Alana (14659817)

Distribution of immigrants who settled in Estrie region between 2009 and 2020 according to incidence of tuberculosis in their home country and categories of immigrants [15]. by Jacques Pépin (3253146)

Functional characterization of skinned myocardium prepared from Epac1TG. by Yoshiki Ohnuki (576298)

Astragaloside IV reduced oxidative stress in SH-SY5Y cells and decreased iNOS expression in BV-2 cells upon IFNγ stimulation. by Yixin He (466799)

Supplementary Data S2 from SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance by Kristen Jensen-Pergakes (15090247)

Climate variable summary. by Dawn Robin Magness (6157265)

Induction of histones H3 and H4 hyper-acetylation and decreased histone H3-lys27 trimethylation follow GBM cell line treatment with HYP. by Naama Dror (459005)

A funnel plot shows the number of studies reporting a change in gut bacteria abundance in patients with an RTI compared to healthy participants. by Claire A. Woodall (10724917)

“…There were 5/5 reports of an ‘increase’ in <i>Enterococcus</i>, 5/5 reports of a ‘decrease’ in Ruminococcaceae and 6/6 reports of a ‘decrease’ in both Lachnospiraceae and <i>Ruminococcus</i> in patients with an RTI compared to healthy participants. …”

<i>Ss</i> infection is associated with decreased plasma levels of IL-2, IL-7 and IL-15 and enhanced plasma levels of IL-4 and IL-9. by Anuradha Rajamanickam (5278013)

Positive (+) and negative (-) impacts of the Covid-19 pandemic on new mothers in the Covid-19 New Mum Study. by Adriana Vázquez-Vázquez (9672972)

Temperature field without considering insulation layer deterioration (2.6 °C). by Jianqing Jia (21001506)

Stress field of surrounding rock considering the insulation layer deterioration (2.6 °C). by Jianqing Jia (21001506)

Stress field of surrounding rock without considering insulation layer deterioration (2.6 °C). by Jianqing Jia (21001506)

Temperature field considering the insulation layer deterioration (2.6 °C). by Jianqing Jia (21001506)