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br Disclaimer br Conflicts of interest br
2024-03-07
Disclaimer Conflicts of interest Role of the Sponsor Acknowledgements Funding/support: This project was supported by a grant from the Department of Surgery (R5129), Western University and by the Institute for Clinical Evaluative Sciences (ICES) Western site. ICES is funded by an annual g
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Steroidal CYP inhibitors can further
2024-03-07
Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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ASK has been identified as an
2024-03-06
ASK2 has been identified as an ASK1 binding protein (Wang et al., 1998). ASK1 supports the stability and active configuration of ASK2 in the heteromeric complex, while ASK2 has been found to activate ASK1 by direct phosphorylation (Takeda et al., 2007). Unlike ASK1, which is ubiquitously expressed i
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Available data thus indicate that there
2024-03-06
Available data thus indicate that there are at least two ways that HMGA proteins can induce localized changes in the chromatin structure of inducible gene promoters, both of which involve positioned nucleosomes that must be “remodeled” before gene transcription can occur. The first mechanism is exem
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Although many factors influence the effects of medications d
2024-03-06
Although many factors influence the effects of medications, during recent years it has become evident that genetic factors could explain the differences between individuals in drug response. These differences are due to variants in genes encoding drug targets [8]. The challenge for pharmacogenetics
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Aberrant or a sustained activation of AhR signaling
2024-03-06
Aberrant or a sustained activation of AhR signaling pathway, triggered by exogenous toxic ligands such as dioxins, PAHs or polychlorinated biphenyls (PCBs), is a well-described biological process engaged during tumor initiation and/or promotion in various tissues (e.g. liver, lung, skin)(reviewed in
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With one exception all receptors for dopamine DA
2024-03-06
With one exception, all receptors for dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT), and norepinephrine are metabotropic receptors. The five metabotropic DA receptors (D1–D5) in the CNS are involved in motivation, pleasure, cognition, learning, memory, fine motor control, and modulate neuroen
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To this the evidence of opposite effects of noradrenaline
2024-03-06
To this, the evidence of opposite effects of noradrenaline and adrenaline on the striatal firing initiation (Fig. 6, Fig. 7) should not be ignored, because the striatum is related to controlling action timing by regulating the firing increase rate (Tanaka and Kunimatsu, 2011). Although the ligand su
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In order to investigate their effects in vitro
2024-03-06
In order to investigate their effects in vitro, therefore, we first used TE671 cells, which have provided a useful source of human AChR for in vitro and radioimmunoassay studies. We found no marked effect of either MuSK-MG or SNMG sera on AChR numbers or on AChR subunit expression. This appears to c
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Indanone and its analogues are useful intermediates for the
2024-03-05
1-Indanone and its analogues are useful intermediates for the synthesis of compounds some of which have applications as pharmaceuticals, especially as analgesic and antihypertensive as well as tobacco flavoring agents. Indanones are commonly used as starting agent for the synthesis of ninhydrin whi
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Inhibitors of mPGES are considered as safe alternative to NS
2024-03-05
Inhibitors of mPGES-1 are considered as safe alternative to NSAIDs in the treatment of chronic inflammatory diseases that are characterized by excessive PGE2 production (Bahia et al., 2014; Khurana and Jachak, 2016; Koeberle et al., 2016; Korotkova and Jakobsson, 2014; Norberg et al., 2013; Psarra e
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AG-120 A key function of the reference
2024-02-23
A key function of the reference AFST would be to detect fungal resistance, i.e. to determine which antifungal agents are likely to be clinically inactive [2]. To this end, the epidemiological cut-off value, defined as ‘the upper end of the wild-type (WT) or beginning of the non-wild-type (NWT) MIC d
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In this study we have generated new FRET reporters
2024-02-23
In this study, we have generated new FRET reporters to screen all submembrane domains of AT1R for interactions with CaM. We identified a new CaM-binding domain on the receptor’s SMD2 (a.a. 125 – 141), confirmed interactions at SMD4JM (a.a. 309 – 327) and characterized the full interacting domain in
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A phase I trial has recently evaluated enzalutamide an anti
2024-02-23
A phase I trial has recently evaluated enzalutamide, an anti-androgen agent, in patients with ER- and AR-positive advanced BC to estimate safety and tolerability of enzalutamide therapy alone or in association to anastrozole, exemestane or fulvestrant [65]. The results of major clinical trials with
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br AR signaling and urothelial cancer progression
2024-02-23
AR signaling and urothelial cancer progression As shown in other types of malignancies, such as prostate cancer cells, it has been documented that androgens induce AR expression and its nuclear translocation as well as ARE promoter activity in urothelial cancer cells (Chen et al., 2003, Izumi et
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