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Riociguat br Materials and methods br Results br
2022-03-21
Materials and methods Results Discussion In this study, we demonstrated, for the first time, that manipulation of AKR1D1 expression and activity is able to regulate glucocorticoid availability in liver and non-liver cell lines. AKR1D1 over-expression leads to increased glucocorticoid cleara
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br Acknowledgments This work was funded by NIH Grant
2022-03-21
Acknowledgments This work was funded by NIH Grant 2R01 MH066958 (JGT) and NSF CAREER award IOS- 1053716 (NV). We thank Dr. Greti Aguilera for the generous gift of the GRE-Luciferase construct and Dr. Louis Muglia for the generous gift of the GR-GFP construct. Introduction Prostate cancer (PCa
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Olanzapine has been reported to attenuate insulin
2022-03-21
Olanzapine has been reported to attenuate insulin secretion, cause insulin resistance (Chintoh et al., 2008) and reduce whole body carbohydrate oxidation (Klingerman et al., 2014). However, a blunting of these effects in Gcgr−/− mice would not appear to explain the protection against olanzapine-indu
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Growth hormone secretagogue receptor GHSR
2022-03-21
Growth hormone secretagogue receptor (GHSR) is a member of G-protein-coupled receptor family [3]. GHSR is predominantly expressed in human pituitary, rhypothalamus and hippocampus [4]. GHSR is also expressed in peripheral tissues including lungs, liver, kidney, and adrenal gland. In cardiovascular s
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Herein we describe the development of second
2022-03-21
Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME
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Until recently the mechanism of how GSMs shifted secretase
2022-03-21
Until recently the mechanism of how GSMs shifted γ-secretase cleavage was poorly understood. Today, building on the sequential cleavage model developed by Ihara and colleagues [14], there is evidence that GSMs act as processivity enhancers, and iGSMs as inhibitors of processivity [120]. At least for
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In the course of an internal FAAH program many very
2022-03-18
In the course of an internal FAAH, program,, , , , , , , , , , , , , many very similar compounds were profiled in vivo with particular interest paid to their ability to penetrate the BBB. The compounds profiled were heteroaryl piperazinyl and piperadinyl ureas; a class of compounds, reported on prev
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Our results on the other hand shows that there
2022-03-18
Our results, on the other hand, shows that there is no upregulation of ETBR on the spinal cord after SCI, but there is a significant difference of mRNA on days 2, 7 and 28 on the SCI group on the spinal cord and no changes on the DRG, suggesting that the spinal cord injury may reduce the renovation
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VU 0155069 Recently it has been found that treatment of huma
2022-03-18
Recently, it has been found that treatment of human phagocytic VU 0155069 or microvascular endothelial cells with NO donors inhibited the O2− generating capacity of NADPH oxidase [[8], [9], [10], [11]], which may involve down-regulation or S‑nitrosylation of the p47phox subunit (a cytosolic subunit
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miRNAs post transcriptionally regulate gene expression by cl
2022-03-18
miRNAs post-transcriptionally regulate gene bms-536924 receptor by cleaving mRNA or inhibiting translation of target gene transcripts. Vita analysis of HBV genome sequence suggested that miR-185-5p may not directly act on HBV mRNAs, which suggested that miR-185-5p might suppress HBV gene expression
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Cysteine Cys residues are frequently found to be
2022-03-18
Cysteine (Cys) residues are frequently found to be highly conserved within functional, regulatory, catalytic, or binding sites of proteins. Thiol or thiolate chemistry imparts active sites with unique properties like nucleophilicity, high affinity metal binding, and disulfide bond assisted multimeri
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Ras small GTPases are critical molecular switches that conne
2022-03-18
Ras small GTPases are critical molecular switches that connect extracellular signals to intracellular signaling pathways initiated by membrane receptors, such as growth factor receptors and G protein-coupled receptors (Simanshu et al., 2017). When shifting between active GTP-bound and inactive GDP-b
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gdc com Molecular mechanisms of decidualization have been
2022-03-18
Molecular mechanisms of decidualization have been studied for years, revealing numerous signaling pathways and transcriptional factors participated in the regulation [37,38]. As a central controller of deicdualization, FOXO1 regulates the transcription of a large number of target genes, which are in
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br Conflicts of interest br Introduction Antiretroviral
2022-03-18
Conflicts of interest Introduction Antiretroviral therapy (ART) is effective in reducing mortality (Detels et al., 1998), and preventing mother-to-child transmission (MTCT) (CDC, 1994, Connor et al., 1994) and sexual transmission of HIV (Cohen et al., 2011). However, the optimal time to start
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The amyloid precursor protein APP is a
2022-03-18
The amyloid precursor protein (APP) is a membrane protein thought to be involved in plasticity, synapse formation and repair, and export of metal ions [68]. The APP present in the brain can be cleaved by three different secretases [73], [74]. Cleavage of APP first by alpha secretase and then gamma-s
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