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br Genetic rescue of GluR A dependent spatial
2022-09-16
Genetic rescue of GluR-A-dependent spatial working memory Spatial working memory performance in GluR-A−/− mice can be restored by the forebrain-specific Oxybutynin of GluR-A subunits labeled with green-fluorescent protein (GFP) on an otherwise GluR-A knockout background (Schmitt et al., 2005). Th
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The role of the ER EK variant which is
2022-09-16
The role of the ER22/23EK variant which is associated with relative resistance to GC, as shown by a reduction of transactivating capacity in vitro and less suppression of rgd peptide levels after 1mg DST in vivo. Relative GC resistance associated with the ER22/23EK polymorphism might protect from th
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Palomid 529 The effect of the selected compounds on NF
2022-09-16
The effect of the selected compounds on NF-kB transrepression was assessed using the well-studied HeLa B2 cell line that expresses endogenous GR and NF-kB family members and responds properly to glucocorticoids and pro-inflammatory cytokines (such as TNF). Our data revealed that the two hit compound
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Attempting to further elucidate the role of glucagon
2022-09-16
Attempting to further elucidate the role of CZC-25146 and activation of the Gcgr without the influence of GLP-1, we used DT-Gcg mice with acute knockdown of all proglucagon products. This mouse model has previously been shown previously to have a normal total islet area as well as β cell area compa
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We note that zinc speciation at and
2022-09-15
We note that zinc speciation at and 2 mol. equiv. of myristate is already markedly different; this means that FFAZn2+ crosstalk is in operation under normal physiological conditions. At present, there are few data to allow tracking of the effects of such physiological crosstalk, although there are s
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These observations are of particular interest in the context
2022-09-15
These observations are of particular interest in the context of recent conceptual changes regarding the mechanisms by which different types of leukocytes contribute to atherogenesis. Over the last decade, the paradigm of the predominant circulatory origin of lesional macrophages has been challenged
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Magtanong et al observed that caspase dependent apoptotic li
2022-09-15
Magtanong et al. (2019) observed that caspase-dependent apoptotic lipotoxicity of saturated fatty acids is suppressed by exogenous MUFAs. This may explain the ability of MUFAs to prevent atherosclerosis, in contrast to the pathogenicity of saturated fatty acids. Moreover, MUFAs may promote while PUF
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In Apicomplexan parasites such as Toxoplasma
2022-09-15
In Apicomplexan parasites such as Toxoplasma gondii isoprenoids are biosynthesized through the DOXP/MEP pathway as illustrated in Scheme 2. In addition, T. gondii possesses a bifunctional FPPS/GGPPS (TgFPPS) that is able to catalyze the formation of both FPP and GGPP.5, 6 The FPPS gene appears to be
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Sperm exocytosis or acrosome reaction AR is
2022-09-15
Sperm exocytosis or acrosome reaction (AR) is a regulated secretion with special characteristics essential for fertilization. The AR relies on the same highly conserved molecules that drive intracellular membrane fusion and exocytosis in all other snx (see [59] for a recent review). Two such molecu
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Nowadays it is accepted that ligands which have been
2022-09-15
Nowadays, it is accepted that ligands which have been classically described as inverse agonists, due to their negative efficacy at modulating the G protein pathway, could also display some positive efficacy regarding receptor desensitization, internalization, or even signaling though another pathway
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The synthetic pathway of the target
2022-09-15
The synthetic pathway of the target compounds , , , and is presented in . The intermediate was synthesized according to a reported method. The intermediate was prepared by mixing UA with an equimolar concentration of KCO, a catalytic amount of KI, and more than two equivalents of 1,2-dibromoethan
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In this investigation the NlVg relative transcript level was
2022-09-15
In this investigation, the NlVg relative transcript level was also prompted by 1.3-fold compared to the untreated control in the TZP treatment, while there was a slight increase of 13.6% for NlVgR (Fig. 7A and B). One underlying molecular mechanism for the TZP-induced fecundity is the significant up
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Theoretically the majority of resistance mechanisms identifi
2022-09-15
Theoretically, the majority of resistance mechanisms identified so far could be targeted by compounds that are already available, such as inhibitors of ER, PIK3CA/mTOR or FGFR1. However, the potential therapeutic advantage of combining these agents with standard HER2-targeting treatments must be wei
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P Benzoxaborole substituted macrocyclic compounds based on
2022-09-14
P4-Benzoxaborole-substituted macrocyclic compounds based on ITMN-191 scaffold were prepared using a general scheme as shown in . ITMN-191 was prepared by following a patent procedure. The P4 BOC group was removed by treatment with TFA in dichloromethane to give amine . The coupling of the amine to 6
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br Mechanisms of HDAC inhibition dependent cardioprotection
2022-09-14
Mechanisms of HDAC inhibition-dependent cardioprotection Multiple preclinical studies have demonstrated potent cardioprotective benefits of HDAC inhibition in murine models of myocardial stress, including I/R [19,25,29,30]. TSA reduces myocardial infarct size by up to 50% [19,25]. In addition, tr
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