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Following these discoveries the term ferroptosis was coined
2022-02-16
Following these discoveries, the term ferroptosis was coined in 2012 [25], to describe this iron-dependent, non-apoptotic form cell death induced by erastin and RSL3. This discovery was accompanied by the development of the first small molecule ferroptosis inhibitor, termed ferrostatin-1, and the d
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This profound cell type specificity of G a
2022-02-16
This profound cell-type specificity of G9a/GLP complex modulation of neuronal plasticity is accentuated by studies employing genetic ablation of G9a in dopamine 1 receptor (Drd1)- and dopamine 2 receptor (Drd2)-expressing medium spiny neurons (MSNs) in the nucleus accumbens (NAc). Conditional G9a kn
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This crosstalk may be responsible
2022-02-16
This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on prostaglandin agonist pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of high-
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Thus both in Drosophila and mammals the
2022-02-16
Thus, both in Drosophila and mammals, the Hippo pathway responds to cell–cell junctions via an apical NF2/Mer-containing complex. Indeed, Hippo signalling and NF2 are required for contact inhibition of growth in cell culture, which is thought to reflect an in vivo function as a sensor of tissue crow
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br Materials and methods br
2022-02-16
Materials and methods Results Discussion Myocardium reperfusion injury contributes almost half of myocardial infarct size in myocardial infarction patients, and infarct size is closely correlated with the probability of developing CPI-455 failure [1]. Despite this knowledge, myocardial rep
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In mice iNKT cells are most
2022-02-15
In mice, iNKT cells are most frequent (20–30%) among liver T lymphocytes, while they only constitute 0.4–1% of the total T cells in thymus, bone marrow, spleen, lymph node, and intraepithelial lymphocytes. In humans, iNKT cells constitute approximately only a 0.1–0.2% of the peripheral blood T lymph
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br Disclosure statement br Acknowledgements
2022-02-15
Disclosure statement Acknowledgements We thank Dr. Rona Carroll for her contribution to the preparation of the manuscript and Dr. Iosif Pediaditakis for his contribution to the preparation of the figures. This work was supported by NIHR01 HD019938 to U.B.K. Introduction The mammalian hypot
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The ion conduction pathway reported herein
2022-02-15
The ion conduction pathway reported herein accounts for all known functional properties of EAAT/GltPh anion channels. Simulations reveal unitary current amplitudes and ion selectivities (Figures 3C and 3D) that resemble experimental results (Melzer et al., 2003, Wadiche and Kavanaugh, 1998). The cal
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Compounds and were evaluated for their
2022-02-15
Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure wa
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br Conflict of interest br Author
2022-02-15
Conflict of interest Author contributions Introduction 2-Quinolones [quinoline-2(1H)-ones], while less prominent than the isomeric 4-quinolones, nevertheless enjoy significant attention as scaffolds in compounds exhibiting a variety of biological activities. These include: 4-aryl-6-chloroqu
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The HCV Ag immunoassay has been shown from previous
2022-02-15
The HCV-Ag immunoassay has been shown from previous studies to be an adequate alternative to the two-stage diagnostic process [6], [9], [16]. Kesli et al. reported a high correlation coefficient of 0.864 when comparing HCV core antigen levels with HCV RNA levels (detected using Qiagen HCV RNA test;
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Several classes of small molecules that modulate CDK
2022-02-15
Several classes of small molecules that modulate CDK8 activity have been reported in the patent literature (Fig. 1). A quinazoline derivative, Senexin B (SNX2-1–165, 1), showed CDK8 enzyme inhibitory activity with an IC50 value of 24–50 nM in different assay, and displayed potent, selective enzymati
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As part of our discovery efforts searching for small molecul
2022-02-14
As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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Finally we investigated increasing basicity as a way to
2022-02-14
Finally, we investigated increasing basicity as a way to improve solubility. We expected that conversion of the ether linkage of to an -methyl group could improve solubility. More than expected, nmda antagonist demonstrated significant improvement of values of solubility for the two media, especiall
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br Advanced Glycation Endproducts As glucose
2022-02-14
Advanced Glycation Endproducts As glucose levels rise within sensory neurons as a result of hyperglycemia, normal metabolic pathways become overwhelmed and excess glucose is shunted into other ancillary pathways that, under these conditions, become damaging. One consequence of hyperglycemia is t
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