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Molecular docking simulations were carried out for ligands i
2023-08-10
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic Di
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The first rationally designed dual mPGES LO inhibitor was re
2023-08-10
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic Z DEVD FMK - 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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Steroidal CYP inhibitors can further be
2023-08-10
Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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In the last decade the zebrafish has emerged as a
2023-08-09
In the last decade, the zebrafish has emerged as a valuable vertebrate model to systematically dissect the genetic underpinnings of both vertebrate heart development and function [8,9], as well as distinct cardiac diseases such as congenital heart disease [10], cardiomyopathies [11,12] and cardiac a
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The picture br Acknowledgment This study was supported by Ja
2023-08-09
Acknowledgment This study was supported by Japan Society for the Promotion of Science Grants-in-Aid for Scientific Research (KAKENHI) [grant number 15K15031]. Introduction Glioma is the leading malignancy of astrocyte origin in the brain. The most aggressive, invasive, and destructive glioma
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Over the years measures of total antioxidant status TAS
2023-08-09
Over the years, measures of total antioxidant status (TAS) have been developed to capture the collective effect of antioxidant defense capacity, including enzymatic and nonenzymatic systems (Fraga et al., 2014, Franco et al., 2007). Multiple antioxidant enzymes, as well as antioxidant vitamins and
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br Concluding remarks br Definition Prion diseases
2023-08-09
Concluding remarks Definition Prion diseases are fatal neurodegenerative disorders that are caused by an unconventional agent that is neither bacterial nor viral, but is in essence an infectious misfolded amyloidogenic protein, termed a prion (Prusiner, 1982). Once considered highly controvers
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Sorafenib was the first small RTK inhibitor
2023-08-09
Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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The specific functions of ERs and
2023-08-09
The specific functions of ERs and AR underline their crucial roles during different phases of spermatogenesis. Their deregulation could affect numerous downstream targets, thereby, disrupting spermatogenesis and male fertility. Various studies have shown that estrogen-like chemicals in the environme
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br Acknowledgements This work was supported by Programme Gra
2023-08-09
Acknowledgements This work was supported by Programme Grants from the MRC and the Wellcome Trust (SGC-C and MF). CB was in receipt of a Marie Curie Intra-European Fellowship during part of this work. We thank past and present members of our group for numerous valuable discussions throughout these
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Neural activity resulting from sensory experience is require
2023-08-09
Neural activity resulting from sensory experience is required for the refinement and maturation of neural circuits during cortical critical periods. This refinement is thought to be important for functional optimization of primary sensory cortices, enabling critical functions such as feature detecti
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br Materials and methods br Results br
2023-08-09
Materials and methods Results Discussion The novel and central finding of the current study is that endothelial 12/15-LO rather than the monocytic/macrophagic 12/15-LO has a critical role in hyperglycemia-induced leukocyte adhesion and retinal endothelial barrier dysfunction. The following
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With regard to the correlation between
2023-08-09
With regard to the correlation between -rearrangements and thromboembolic events, Zer et al. reported a VTE rate of 36% in a cohort of 98 patients with ALK-positive NSCLC. Of note, VTE was also associated with shorter overall survival (HR: 5.71, =0.01) . Only few others have investigated NSCLC driv
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95 9 br Dysregulated aromatase expression the link between
2023-08-08
Dysregulated aromatase expression: the link between obesity and breast cancer Obesity has been associated with abnormally high expression of the enzyme aromatase in the breast, influencing the local production and bioavailability of estrogens (Morris et al, 2011, Subbaramaiah et al, 2012). Bowers
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Based on the results of studies done
2023-08-08
Based on the results of studies done to-date, there are three characteristics that make a letrozole-based protocol attractive for use in cattle: 1) it is steroid-free, 2) it is cost-effective and requires a shorter time and fewer animal handlings than conventional methods (Table 1), and 3) it may ha
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