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A rational approach for the design of new steroid compounds
2023-08-12
A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a
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Thymoquinone TQ is the major active compound
2023-08-12
Thymoquinone (TQ) is the major active an American idol derived from Nigella sativa (Woo et al., 2012). Recent animal studies support the potential of TQ for the treatment of a variety of inflammatory disorders like inflammatory bowel disease (IBD), RA, and osteoarthritis (OA) (Salem, 2005, Badr et a
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The Limitations of our data include the absence
2023-08-12
The Limitations of our data include the absence of functional/behavioral assessments and lack of direct comparison with females which would require additional studies and conceivably support sex-specific interventions for stroke [50]. Competing interests Acknowledgements This study was suppor
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br Implementation of sacubitril valsartan into clinical prac
2023-08-12
Implementation of sacubitril/valsartan into clinical practice Following on from the results of PARADIGM-HF, sacubitril/valsartan was given regulatory approval for use in patients who conform to the main inclusion criteria of the trial; NYHA functional class II–IV, reduced left ventricular ejectio
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br Introduction Cell motility is fundamentally important in
2023-08-12
Introduction Cell motility is fundamentally important in morphogenesis, wound healing, and the immune response. One of the best-studied basic types of cell movement is lamellipodial motility [1, 2], characterized by a thin (∼0.1–0.2 μm), broad (∼10–40 μm) motile appendage containing a dynamic sb
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The first rationally designed dual
2023-08-11
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic Rufinamide - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synthes
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In brief serotonin can interact with classes of
2023-08-11
In brief, serotonin can interact with 7 classes of receptors are differentiated into 14 subtypes (Barnes and Sharp, 1999). Specifically, 5-HT1A and 5-HT2C receptors have been the most widely studied in the modulation of anxiety responses (Deakin et al., 1992; Millan, 2003). However, the studies that
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Herein we disclose novel dihydropyrano c pyrazoles that
2023-08-11
Herein, we disclose novel 2,4-dihydropyrano[2,3-c]pyrazoles that inhibit human ATX (hATX). Our results demonstrate and further support previous findings showing that a desired biological action can be achieved without targeting the catalytic site of the enzyme. Moreover, this study validated hen egg
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Along with the improvement of the cadmium transport from roo
2023-08-11
Along with the improvement of the cadmium transport from roots to aerial tissues, as is required for phytoremediation, over-expression of PtoHMA5 also led to the excessive accumulation of cadmium in leaves that was harmful to plant growth and physiological performance. Thus, detoxification of the he
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Furthermore low affinity sites that share no structural
2023-08-11
Furthermore, low-affinity sites that share no structural homology with the aforementioned sites have been described in the transmembrane domain. It has been discovered that, in α1βγ2 receptors, potentiation of GABA-activated currents by high concentrations of diazepam is biphasic, with a high- and a
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There is a delicate balance between ROS generation and scave
2023-08-11
There is a delicate balance between ROS generation and scavenging by the protective antioxidant defenses in the cell. Antioxidant systems present in the spleen tyrosine kinase include enzymes like superoxide dismutase (SOD), catalases, glutathione peroxidases (GPxs) and peroxiredoxins (PRxs) (Fig.
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AP activity is increased by
2023-08-11
AP-1 activity is increased by MAP kinase stimulation in different cell types (Whitmarsh and Davis, 1996), while MKP-1, the enzyme that catalyzes the dephosphorylation and inactivation of MAP kinases in the nucleus, inhibits AP-1 (Rössler et al., 2008, Rössler and Thiel, 2009, Mayer et al., 2011, Thi
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That increased longevity was not the exclusive result
2023-08-11
That increased longevity was not the exclusive result of blood pressure reduction. This was demonstrated by analysis of life-long, whole body deletion of AT1A receptors in normotensive mice. These animals exhibited a very significant increase in lifespan when compared to wild- type mice [159], [160]
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The association of male gender with increased atherosclerosi
2023-08-11
The association of male gender with increased atherosclerosis has stimulated interest in the role of androgen signalling in this condition. Androgens act (Fig. 2) by direct activation of androgen receptor (AR), a nuclear receptor that acts as a ligand-regulated transcription factor (Gao et al., 2005
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br Introduction The traditional Chinese
2023-08-11
Introduction The traditional Chinese medicine (TCM), Ganoderma (G.) lucidum Karst is a well-known mushroom which has been used clinically in some Asian countries. It is termed “Lingzhi” in China, “Reishi” in Japan and “Yeongji” in Korea. It has long been used in TCM for the promotion of longevity
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