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br Conclusion The following is the supplementary data
2022-06-10
Conclusion The following is the supplementary data related to this article. Conflict of interest Funding Acknowledgements Peroxiredoxin VI (Prdx6) is a dual-functioning antioxidant enzyme that acts to protect biological membranes against damage caused by lipid peroxidation , . The enz
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We show that pharmacological inactivation of GSTP
2022-06-10
We show that pharmacological inactivation of GSTP1 over a sustained period does not show any observable toxicity, and not only prevents breast tumor growth but even slows established breast tumor growth in mice. A highly potent GSTP1 inhibitor, ezatiostat (developed by Telik Inc.) has passed phase I
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br Methods br Transfollicular penetration of herbs
2022-06-10
Methods Transfollicular penetration of herbs and their active constituents used for hair loss treatment The transfollicular administration of pharmacologically active molecules is recognised as a significant element for therapeutic interest, mainly with regard to delivery to specific sites of
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GSK 650394 Introduction Molecular imprinting technology is a
2022-06-09
Introduction Molecular imprinting technology is a method that combines the material chemistry, biochemistry, and polymer chemistry and has the ability to specifically identify target analytes on shape, size and functional groups. Molecular imprinting polymer (MIP) is developed based on molecular im
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To date glycine receptors have been found in
2022-06-09
To date, glycine receptors have been found in five distinct transmembrane protein subunits (one β subunit and four α subunit (α1–α4)), combining to form two different types of functional receptors [4], [14], either α homomeric, the immature extrasynaptic glycine receptor subtype, or αβ heteromeric,
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The precise mechanisms of action of
2022-06-09
The precise mechanisms of action of 4-PBA are as yet ambiguous. Its capacity as a chemical chaperone has been thoroughly documented for the ABC transporter family in particular (Prulière-Escabasse et al., 2007; Iram and Cole, 2014; Gordo-Gilart et al., 2016; Pomozi et al., 2017). 4-PBA has been clas
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Solid tumors usually present insufficient
2022-06-09
Solid tumors usually present insufficient supply of oxygen, activating the hypoxia inducible factor-1 (HIF-1) pathway, which prompts an adaptive response on genes that regulate glycolytic metabolism, promoting glucose uptake through the transcription of GLUTs [54]. Increasing evidence indicates that
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Xenobiotic metabolizing enzymes are classified as being phas
2022-06-09
Xenobiotic metabolizing enzymes are classified as being phase I, phase II and transporter enzymes, with phase I enzymes metabolizing lipophyllic xenobiotics to make them more polar so that the phase II enzymes can perform the necessary conjugation reactions that afford elimination. Although the phas
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The widespread involvement of HH GLI
2022-06-09
The widespread involvement of HH/GLI in human malignancies has initiated a remarkable effort to identify selective HPIs. As shown in Table 2.1, most of these small molecule inhibitors target the essential effector protein SMO, which should lead to pathway abrogation by eventually decreasing the GLIA
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In accordance with its similarity to classical NLSs Importin
2022-06-09
In accordance with its similarity to classical NLSs, Importin α3 was recently reported as a nuclear transport receptor for Ci (). We therefore superimposed the Gli1 NLS model with the Importin α2 structure (3EFX), which has a structure similar to Drosophila Importin α3 () (Fig. 4.4B). Gli1 NLS fitte
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So far several methods have been used to
2022-06-09
So far, several methods have been used to monitor the level of GJC and its regulation in astrocytes studied in acute IPA-3 slices (see Giaume et al., 2012). This mainly includes approaches based either on electrophysiological properties of gap junction channels or on “dye coupling” experiments that
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Two intermediate compounds A and B in
2022-06-09
Two intermediate compounds (A and B in Fig. 1) were tested for both Aβ40 and CYP3A4 inhibition activity. Potential hydrolysis of structures I and IIin vivo may produce A which is a strong CYP3A4 inhibitor. Cyclopropanol group is a suspected liability, because nitric oxide B without it has a clean CY
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Methods Very briefly PLA polymeric nanoparticles as well as
2022-06-09
Methods Very briefly: PLA polymeric nanoparticles as well as liposomes were synthesized and loaded with three different FGFR inhibitors. The encapsulation efficiency, average size, PDI, zeta potential, stability and release kinetics were investigated. The most promising formulations were biological
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In addition we assessed the viability of
2022-06-09
In addition, we assessed the viability of 1,2,3,4-tetrahydroquinoline (13t) and 1,2,3,4-tetrahydroisoquinoline (13u) as the tail on account of our previous SAR results. To our delight, 13t and 13u each had comparable activity to that of 13c, with 13u being slightly more potent than 13c. Further stru
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Magtanong et al have demonstrated that MUFAs induce a ferrop
2022-06-09
Magtanong et al. (2019) have demonstrated that MUFAs induce a ferroptosis-resistant state in cells in an ACSL3 (acyl-CoA synthetase long-chain family member 3) dependent manner. They observed that MUFAs did not increase the expression of GPX4, which opposes ferroptosis. However, they blocked plasma
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