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Gratifyingly compound also demonstrated improved physicochem
2023-04-25
Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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br Experimental procedure br Introduction Migraine is a debi
2023-04-25
Experimental procedure Introduction Migraine is a debilitating neurovascular disorder characterized by recurring unilateral pulsating headaches of moderate to severe intensity, associated with nausea, photophobia and/or phonophobia, lasting from 4 to 72 h (Headache Classification Committee of
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Having established the structural requirements for potency i
2023-04-25
Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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br Acknowledgements br Introduction Double stranded
2023-04-25
Acknowledgements Introduction Double-stranded DNA breaks (DSBs) are among the most deleterious DNA lesions that threaten genomic integrity. DSBs are generated not only by exogenous DNA-damaging agents but also by normal cellular processes such as V(D)J recombination, meiosis, and DNA replicati
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Similar to the importance of MeJA in postharvest
2023-04-24
Similar to the importance of MeJA in postharvest A. bisporus quality maintenance at 10°C storage (Meng et al., 2012a), MeJA was also observed to play a pivotal role in this event at 4°C storage. Cap opening is an important mushroom quality indicator (Braaksma et al., 1999). During postharvest storag
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br Acknowledgements This study was funded the Irish Departme
2023-04-21
Acknowledgements This study was funded the Irish Department of Agriculture, Food and the Marine through the research program FIRM/RSF/CoFoRD (Reference: 13 F 462). The authors declare no conflict of interest. Introduction Radiotherapy (RT) is one of the major treatment methods among patients
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2825 Thalidomide is now a well known antiangiogenic agent Th
2023-04-21
Thalidomide is now a well known antiangiogenic agent. This property of thalidomide is being extensively researched upon, for its significant utility in the treatment of various malignant tumors. Studies show that thalidomide efficaciously inhibits various pro-angiogenic factors such as tumor necrosi
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Although sex hormones activational effects are
2023-04-21
Although sex hormones (activational effects) are known to directly interact with RAS (Baiardi et al., 2005, Miller et al., 1999, Silbiger and Neugarten, 1995), the potential contribution of organizational hormonal and SCC effects on physiological sex-based difference in the regulation of the RAS rem
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Evidence from basic science studies
2023-04-21
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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The first and the best characterized mechanism of receptor d
2023-04-21
The first and the best-characterized mechanism of receptor-dependent internalization of Aβ is mediated via the α7-nicotinic PCI-34051 receptor [82]. Lipoprotein receptor protein represents the second best-studied route that facilitates the uptake of Aβ by neurons, involving additional molecules suc
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The reduced IFN production seen with BPAL primed
2023-04-21
The reduced IFNγ production seen with BPAL10-primed splenocytes could potentially be attributed to the impaired intracellular survival of B. pertussis, thereby leading to a weakened induction of cell-mediated immunity. Earlier studies have suggested an antimicrobial role of IFNγ in mediating the eli
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direct renin inhibitors br The role of AMPK beyond energy ho
2023-04-20
The role of AMPK beyond direct renin inhibitors homeostasis: regulating metabolism AMPK plays a major role in glucose homeostasis by modulating glucose transport in peripheral tissues [20]. Skeletal muscle, one of the main peripheral tissues involved in glucose uptake and disposal, expresses gluc
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MHC class II antigen (45-57) [Homo sapiens] br Conflicts of
2023-04-20
Conflicts of interest Acknowledgments Significance Introduction Androgen receptor (AR) plays a paramount role in the onset and progression of prostate cancer (PC) (Burnstein, 2005, Lonergan and Tindall, 2011, Watson et al., 2015). This very facet underlies androgen deprivation therapy (A
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Conclusion Twenty compounds with dinitrobenzoate scaffold we
2023-04-20
Conclusion Twenty compounds with 3,5-dinitrobenzoate scaffold were synthesized and evaluated using cell-free and HWB assays for their 5-LOX inhibition activities. Compared to the parent compound, six compounds show significantly increased enzyme inhibition activities. The best compound, 3-tolyl 3,
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br LOX in esophageal cancer Various studies
2023-04-20
5-LOX in esophageal cancer Various studies suggest that abnormal levels of AA metabolites play an essential role in human esophageal adenocarcinogenesis (EAC). The key AA derivatives of 5-LOX signaling molecules namely include, 5-HETE, LTB4, and cysteinyl LTs, which are well-known to initiate inf
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