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(+)-MK 801 Maleate br Experimental procedures Adk tg Adktm t
2024-06-26

Experimental procedures Adk-tg (Adktm1−/−:tg(UbiAdk) mice were created by breeding a loxP-flanked Adk transgene under the control of a human ubiquitin promoter into ADK knockout mice (Fedele et al., 2005,). Fb-Adk-def (Adktm1−/−:tg(UbiAdk):Emx1-Cre-tg3) mice were generated by pairing Emx1-Cre-tg3
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Curcumin is the principal natural polyphenol
2024-06-26

Curcumin is the principal natural polyphenol curcuminoid of turmeric (Curcuma longa) rhizome, a member of the ginger family (Zingiberaceae) [13]. Curcumin has a wide spectrum of therapeutic properties, and it has been shown to possess antioxidant, anti-inflammatory, anticancer, antiangiogenesis, che
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br Introduction In myasthenia gravis MG
2024-06-26

Introduction In myasthenia gravis (MG), autoantibodies against the native AChR conformation cause loss of AChR at the neuromuscular junction and fatigable muscle weakness (Newsom-Davis et al., 1993). The AChR is a pentameric transmembrane protein, with two splice forms of the α-subunit, P3A− and
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Beclomethasone dipropionate Macrophage polarization is linke
2024-06-26

Macrophage polarization is linked to activation of the ligand-dependent transcription factor PPARγ. Recently, Odegaard et al. demonstrated with a macrophage-specific deletion of PPARγ in mice that alternative macrophage activation is impaired [14]. We provided evidence that contact to apoptotic Becl
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The first rationally designed dual mPGES LO
2024-06-26

The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic Tirapazamine - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synth
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The first natural product described as LO inhibitor was the
2024-06-26

The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic death associated protein kinase from the Mexican dessert plant Larrea divaricata in 1981 (Bokoch and Reed, 1981), short after the initial identification of 5-LO in 1979 (Borgeat and Samuelsson, 1979). Long
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Subsequently Palvimaki et al corroborated Ni and Miledi s st
2024-06-26

Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a
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Several tertiary prevention studies are currently underway e
2024-06-26

Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Du
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br Concluding remarks Autophagy ensures cell homeostasis and
2024-06-26

Concluding remarks Autophagy ensures cell homeostasis and survival through the continuous degradation/recycling of intracellular components. It can also represent a conserved, cell-intrinsic, defense mechanism against invading pathogens, including viruses. The autophagy process can be activated r
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Ryoichi et al modified potent clinical candidate VX with
2024-06-26

Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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V ATPase is a complex enzyme that is
2024-06-26

V-ATPase is a complex enzyme that is composed of several subunits, which are assembled into two domains: trans-membrane (V0) and cytosolic (V1) domains [3,5]. Epididymal epithelial AK-7 of rats has been reported to contain V-ATPase which is distributed at the apical pole of the narrow and clear cell
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Recent studies have supported the existence
2024-06-26

Recent studies have supported the existence of an inward RAS regulatory mechanism in which AT1 receptors downregulate angiotensin-converting enzyme 2 (ACE2) and subsequently impair angiotensin-(1-7) generation and MAS functionality (Jessup et al., 2006, Gallagher et al., 2008, Xia et al., 2009, Pern
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Evidence from basic science studies suggests that Cd
2024-06-26

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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In light of several reports of defects in memory related
2024-06-26

In light of several reports of defects in memory-related tasks for the dysbindin-deficient mice (Cox et al., 2009, Takao et al., 2008), it was rather unexpected that an enhancement of CA3–CA1 LTP was observed in our investigation as well as in another independent study (T.T. Tang et al., 2009). The
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Accumulating evidence suggest that patients
2024-06-25

Accumulating evidence suggest that patients with advanced -positive NSCLC are at increased risk of VTE or coagulation disorders during the course of their disease, indicating that cancer genotype might play a role in the occurrence of cancer-related thromboembolism . Here we report the case of a pat
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