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Since the cloning of ARs in the beginning of the
2024-06-19
Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav
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Pifithrin-α That disassembling actin filaments transport
2024-06-19
That disassembling Pifithrin-α filaments transport chromosomes towards the spindle in oocytes may be surprising at first sight. On the other hand, it is well established that chromosome movement during anaphase is driven by the depolymerization of microtubules [20]. It will be interesting to invest
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Tacrine an aminoacridine derivative Fig A was
2024-06-19
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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Caffeic acid dihydroxycinnamic acid is
2024-06-19
Caffeic Lovastatin (3,4-dihydroxycinnamic acid) is a natural compound that inhibits 5-LO and exerts potent anti-inflammatory and antioxidant properties. Recently, Takeda et al. reported that caffeic acid provided neuroprotective and anti-depressive activities [23]. Sertraline, a selective serotonin
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For both the hydroxylation and
2024-06-18
For both, the 17α-hydroxylation and 17, 20-lyase reactions, the heme iron center of P450 17A1 receives electron reducing equivalents from CPR. Both reactions require one pair of electrons and molecular oxygen for the conversion of the substrate into product in each catalytic cycle. However, the 17,2
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However cancer and fibrotic diseases are
2024-06-18
However, cancer and fibrotic diseases are the most extensively studied disease states. ATX is connected to various cancers because it can stimulate chemokinesis and chemotaxis in melanoma cells. Upregulated ATX aa2414 has been reported in breast cancer,, prostate cancer, thyroid cancer, non-small-
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br Disclosure statement br Acknowledgements The work was sup
2024-06-18
Disclosure statement Acknowledgements The work was supported by the National Science Foundation of China (Nos. 81273526, 81473268) and Natural Science Foundation of Colleges and Universities (Nos. KJ2017A197). What is already known What this article adds Introduction Sevoflurane is o
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Why do glutamate and glycine bind to the receptor in
2024-06-18
Why do glutamate and glycine bind to the 242 4 in such different ways? Given the overall structural similarity between the GluN2A and GluN1 LBDs, one might conclude that the LBDs also bind ligands via similar processes. NMDA receptors with engineered disulfide linkages that lock the GluN1 lobes shut
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l Arginine supplementation was reported
2024-06-18
l-Arginine supplementation was reported to be efficient, inefficient or toxic in aged patients. The present study does not support our hypothesis that increased tissue arginase activity may account for the ineffectiveness and even the toxicity of l-arginine supplementation in ageing. Indeed, except
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Since artemisinin shows low solubility and poor oral bioavai
2024-06-18
Since artemisinin shows low solubility and poor oral bioavailability [8], [9], derivatizations of artemisinin were carried out and yielded different semisynthetic antimalarial drugs such as artemether and sodium artesunate. Artemether (decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano [4.3-
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Secondly as pointed out by Sulentic and Kaminski in their
2024-06-18
Secondly, as pointed out by Sulentic and Kaminski in their recent paper [90], most of the AhR literature to date has focused on mouse AhR. Although both mouse and human AhR are interchangeable in many in vitro systems, the in vivo ligand binding affinity is drastically different between the two AhRs
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br Introduction Nausea and vomiting are
2024-06-17
Introduction Nausea and vomiting are among the most distressing side effects associated with chemotherapy in cancer patients (Billio et al., 2010). Severe emesis can negatively affect a patient's nutritional state, ability to work and motivation, which can, in turn, interfere with the clinical co
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Macrophage polarization is linked to activation of the ligan
2024-06-17
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 ecop
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Of note core autophagy factors also play an important role
2024-06-17
Of note, core autophagy factors also play an important role during the infection of host cells by another type of picornavirus, namely, echovirus 7. ATG16L1 was found necessary for entry/internalization into Caco-2 polarized epithelial cells because the virus accumulated on the surface of ATG16L1-de
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Based on currently available knowledge autophagy supports ad
2024-06-17
Based on currently available knowledge, autophagy supports adipocytes development and differentiation. In animals with specific skeletal muscle Disulfiram of Atg7, reduced adipogenesis was shown. In rodents, autophagy was decreased in adipose tissue of animals fed with high-fat diet (HFD). In contr
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