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br Acknowledgement We like to thank the
2022-07-25

Acknowledgement We like to thank the Austrian Federal Ministry of Science, Research and Economy for financial support (GZ402.000/00014-WF/V/6/2016 within the Sino-Austria project) as well as Andrea Szabo and Patricia Haiss for support regarding the drawing of figures and tables. Farnesoid X Re
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br Results br Discussion Our studies highlight MUFAs as
2022-07-22

Results Discussion Our studies highlight MUFAs as key lipid modulators of both non-apoptotic and apoptotic cell death. Recent studies show that a more mesenchymal phenotype, de-differentiation, and acquired resistance to targeted inhibitors, can all promote a ferroptosis-sensitive cell state (
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As for all DOACs measurement of
2022-07-22

As for all DOACs, measurement of DiXaIs activity requires the use of dedicated specific calibrators and controls. Each drug needs its own calibration and control material in a like to like manner. In no case can a drug concentration be extrapolated with the use of a calibrator established for anothe
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In neurons and neuroendocrine cells the
2022-07-22

In neurons and neuroendocrine cells, the productive fusion pathway is thought to initiate with the Munc18-1/Syx1 complex (Ma et al., 2013, Hughson, 2013, Lai et al., 2017). The Munc13-1 MUN domain is able to catalyze opening of Syx1 (the transition from the Munc18-1/Syx1 complex to the SNARE complex
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Within a live organism cells need to transfer information to
2022-07-22

Within a live organism, cells need to transfer information to each other. Exocytosis is one of the critical mechanism which releases variety of ligands into the extracellular space. When cells export material via exocytosis, they first pack into vesicles, then cause the vesicles to tether at the pla
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br Hippo Signaling in Autoimmunity An imbalance of T cell
2022-07-22

Hippo Signaling in Autoimmunity An imbalance of T cell subsets, such as immunosuppressive regulatory T caffeic acid sale (Treg) and inflammatory TH17, has a key role in autoimmune diseases. Recently, investigations found that TAZ but not YAP enhances TH17 differentiation but attenuates Treg diff
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However despite medicinal chemistry efforts lead to consider
2022-07-22

However, despite medicinal chemistry efforts lead to considerable improvement in potency and selectivity of new HO-1 inhibitors, still have not identified inhibitors in the low nanomolar range. Therefore, due to the possible in vivo non-specific effects at high dosage, novel strategies should be dev
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br General aspects of HDACs br General
2022-07-22

General aspects of HDACs General aspects of HDAC inhibitors Based on the previous elements, inhibitors designed for HDAC have in common a well-admitted pharmacophore model (Fig. 7A). This model is composed of a zinc binding group (ZBG), attached to a linker chain mimicking the lysine side chai
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Glutathione transferases EC also referred to as glutathione
2022-07-22

Glutathione transferases (EC 2.5.1.18; also referred to as glutathione S-transferases, GSTs) are ubiquitous and promiscuous enzymes that catalyze various kinds of reactions involving a wide variety of substrates that are toxic and chemically reactive (Angelucci et al., 2005). The primary function of
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This variant has also been related to
2022-07-22

This variant has also been related to a better treatment response in patients with metastatic colorectal cancer subjected to irinotecan-based chemotherapy (Kweekel et al., 2008). Inheritance of this metabolic variability has also been stated to influence better treatment outcomes in breast cancer pa
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Table shows the distribution of all
2022-07-22

Table 3 shows the distribution of all studied groups regarding mutation of GSTP1 gene polymorphism in each group. From 15 COPD smoker patients in group (A), 12 (80%) had heterozygous mutation, from 15 COPD non-smoker patients in group (B), 5 (33.3%) had heterozygous mutation, from 10 control subject
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br Introduction Marijuana remains the
2022-07-21

Introduction Marijuana remains the most widely used illegal drug (Murray et al., 2007), and its validated targets include plasma membrane cannabinoid receptors, many of which are found in the central nervous system. The diverse physiological effects produced by marijuana and cannabinoid ligands s
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EZLink Sulfo-NHS-SS-Biotin Kit Recently a G protein coupled
2022-07-21

Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of
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Thermal analysis of the NQ
2022-07-21

Thermal analysis of the NQ21 peptide was performed with the Solar CM2203 spectrofluorometer. We prepared three 1 μg/mL peptide solutions with different Doxofylline levels (5.0, 7.4, 8.5) in 0.01 M phosphate buffers. Each solution was slowly heated up from 28 °C to 54 °C with a step of 1 °C. Spectra
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As preclinical toxicity and efficacy both appear to be
2022-07-21

As preclinical toxicity and efficacy both appear to be associated with GlyT1 inhibition, it remains to be determined whether on-target toxicity can be separated from efficacy. The present study evaluated a series of GlyT1 inhibitors for target potency, mode of inhibition, residence time, activity in
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