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The first natural product described
2023-11-30
The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic motilin receptor 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 time before mPG
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In humans the major LOs are
2023-11-30
In humans, the major LOs are subdivided by their positional specificity into 5-(ALOX5), 12-(ALOX12) and 15-LO (ALOX15) (Kuhn et al., 2015). 5-LO is the key enzyme for LT biosynthesis and mainly found in mature cells from myeloid origin, including neutrophil, eosinophil and basophil granulocytes, mon
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Fencilli et al reported derivatives of PHA
2023-11-30
Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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br Conclusion In summary screening a small
2023-11-30
Conclusion In summary, screening a small compound library based on the 3-aminopyridin-2-one motif in a target-blind manner against a 26-kinase panel, representative of the kinome, identified hits that possess good activity and excellent ligand efficiency against MPS1, Aurora A and Aurora B. The b
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These results must also be addressed in light of
2023-11-30
These results must also be addressed in light of porcine AMPKγ3R200Q (RN−) mutation. Pigs harboring this mutation produce meat with an abnormally low ultimate pH (pHas hydrazide meat (Copenhafer et al., 2006, Lundström et al., 1998, Milan et al., 2000). This extremely low pH is very close to the is
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Preliminary results of studies sponsored by the manufacturer
2023-11-30
Preliminary results of studies sponsored by the manufacturer of ETC-1002 have also shown positive results for monotherapy in statin-intolerant patients and for the combined use of the ACL inhibitor plus other cholesterol-reducing agents. In patients with a documented history of intolerance to statin
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Apelin is involved in various physiological functions includ
2023-11-30
Apelin is involved in various physiological functions, including SB 216763 receptor contraction (Ashley et al., 2005), vasodilatation (Jia et al., 2007), feeding control (Valle et al., 2008), and metabolic homeostasis (Higuchi et al., 2007, Dray et al., 2008, Attane et al., 2010). Its plasma level i
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Previous studies demonstrate that chiral biointerface has gr
2023-11-30
Previous studies demonstrate that chiral biointerface has great influence on cells adhesion and proteins adsorption [39], [40], [41], [42], [43], which inspired us to further develop antimicrobial materials or surfaces by taking advantage of the “chiral taste” of microbes. L-borneol is a hydrophobic
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Most clinically approved antiangiogenic drugs are aimed at b
2023-11-29
Most clinically approved antiangiogenic drugs are aimed at blocking the action of vascular endothelial growth factor, or VEGF, which is accepted to be the most important tumor-derived angiogenic factor, stimulating proliferation and migration of endothelial cells, as well as branching of vessels (Fe
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As patients with type diabetes are known
2023-11-29
As patients with type 2 diabetes are known to be hyperinsulinemic per se, this relationship between insulin/IGF1 receptor and AR may point towards a causal role of insulin in AR upregulation. Indeed, this is supported by several previous observations. Beyond the already mentioned AR activation by in
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In conclusion we demonstrated that
2023-11-29
In conclusion, we demonstrated that, in the skeletal muscle of rats with T1DM, CRBN levels increased and AMPK, Akt, GLUT4, PGC-1α, and FNDC5 levels decreased, resulting in increased fasting glucose levels. Aerobic exercise training decreased levels of CRBN, which was possibly mediated by AMPK, Akt,
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While high fat diet models of insulin resistance are
2023-11-29
While high-fat diet models of insulin resistance are acceptable approaches for the study of pre-diabetes in humans, they are not suitable for modeling progression towards established type2 diabetes. The pattern of activation of the lipoxygenase pathway in pre-clinical models of type2 diabetes has no
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br ABCA and cancer drug response
2023-11-29
ABCA2 and cancer drug response Overall, the expression of ABC transporters has been linked with multidrug resistance phenotypes through the efflux of drugs via ATP-dependent transport. For example, 13 distinct transporters (ABCA2, ABCB1, ABCB4, ABCB11, ABCC1–6 ABCC10, ABCC11 and ABCG2) have been
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The relatively high concentration of HT used in this study
2023-11-29
The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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Introduction Myasthenia gravis MG is
2023-11-29
Introduction Myasthenia gravis (MG) is an autoimmune disorder characterized by muscle weakness, which is mainly due to autoantibodies reducing the number or function of postsynaptic CZC-25146 receptors (AChRs) [1], [2]. Animal models have been developed to uncover the immunopathogenesis of MG. Exp
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