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Pregnane X receptor PXR is a nuclear receptor that plays
2025-01-07
Pregnane X receptor (PXR) is a nuclear receptor that plays an important role in regulation of metabolism and disposition of structurally diverse xenobiotics as well as endogenous steroids and bile acids (Bertilsson et al., 1998, Kliewer et al., 1998, Lehmann et al., 1998). PXR regulates the metaboli
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br Acknowledgment br Introduction The yeast Cdc
2025-01-06
Acknowledgment Introduction The yeast Cdc48 ATPase and its metazoan ortholog p97 (or VCP) are critical components of many ubiquitin-dependent cellular pathways that require the segregation of individual proteins from binding partners or membranes (for review, see Buchberger, 2013, Meyer and We
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In the nineties we knew that
2025-01-06
In the nineties we knew that (-)baclofen was the stereo-selective ligand for the GABAB receptor which had been recognised by Norman Bowery as a receptor for GABA, which was different from the GABAA receptor (Hill and Bowery, 1981). GABAB receptor antagonists were also synthesised and made available
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The approach of enzymatically converting an analyte and
2025-01-06
The approach of enzymatically converting an analyte and detecting it by the resulting small pH changes near the reduced graphene oxide (rGO) surface has successfully been pursued in case of urea (Piccinini et al., 2017). Furthermore, this work reported that electrostatic layer-by-layer (LbL) assembl
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Currently NSAIDs which achieve antineoplastic actions mainly
2025-01-06
Currently, NSAIDs which achieve antineoplastic actions mainly through apoptosis are emerging choice in chemotherapy. Their antineoplastic effects were demonstrated before in tumor-bearing models [5], [6], [7]. Through in vitro cell models, we identified an indomethacin-activation of ceramide/PP2A/Ak
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As with most G protein coupled receptors GPCRs
2025-01-06
As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et a
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L-817,818 br Materials and methods br Results br Discussion
2025-01-06
Materials and methods Results Discussion Diabetic kidney disease (DKD) is the most common cause of end-stage renal disease [15], [16]. The pathogenesis of DKD is not fully understood, and there is no effective treatment. Although previous studies suggested that early lesions of DKD are foun
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No starting dose adjustment is needed
2025-01-06
No starting dose adjustment is needed for mild or moderate renal impairment and mild hepatic impairment (Child-Pugh A classification) though use in patients with severe hepatic impairment (Child-Pugh classification Class C, 10–15 points score) is not recommended.8, 9, 10, 13 Drug interaction & ad
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Evidence from basic science studies suggests
2025-01-06
Evidence from basic science studies suggests that Cd may play a role in prostate cancer through disruption of the androgen receptor (AR). AR, a hormone-activated transcription factor, is the key driver of prostate cancer progression [6]. Ironically, the AR is also required for normal prostate growth
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Intriguingly androgens may also have an indirect
2025-01-06
Intriguingly androgens may also have an indirect effect on AR gene expression through inhibition of the GATA2 transcription factor gene (He et al., 2014) (Table 1). Using ChIP-seq, GATA2 was found to bind to a regulatory element 5.5 kb upstream of the TSS of the AR gene and enhanced transcription, w
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2 deoxyglucose This development notwithstanding the chemothe
2025-01-06
This development notwithstanding, the chemotherapeutic treatment for leukemia has stagnated over the last 40 years [35]. Main treatment options necessitate aggressive chemotherapy to target leukemic cells [36], [37], [38], [39]. Several limitations of current treatment options include the use of ant
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ddhC The lack of specific PARP
2025-01-06
The lack of specific PARP inhibitors prevents our understanding of how TIPARP or perhaps other PARPs affect AHR signaling. Current inhibitors are based on NAM and were designed to inhibit PARP1 [59]. Many of them do not effectively inhibit mono-ADP-ribosyltransferases and their ability to inhibit TI
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Although AMPK is a negative
2025-01-03
Although AMPK is a negative regulator of bioenergetic reprogramming in cancer cells, little is known about the role of AMPK in immunometabolism in sepsis. Our current study indicates that AMPKα dysfunction enhances PKM2-dependent aerobic glycolysis, which results in HMGB1 release in macrophages and
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Isoxsuprine hydrochloride mg br Experimental section br Resu
2025-01-03
Experimental section Results and discussion Conclusion Acknowledgement This work was supported by the National Natural Science Foundation of China (Grant Nos. 81401489), the Shanghai Pujiang Program (17PJ1402800) and the Shanghai Sailing Program (Grant No. 14YF1409000). Introduction
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br Applications of ATN in
2025-01-03
Applications of ATN in clinical trials In pivotal trials, the use of biomarkers will also have to be considered in the context of regulatory risk and scrutiny. Although an important intended application of the framework is in research studies, its use will undoubtedly impact clinical development
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