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The first natural product described as LO inhibitor was the
2023-02-06
The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic INF39 mg 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 mPGES-1 wa
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AGI-6780 Matthew et al synthesized and carried out SAR studi
2023-02-06
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that AGI-6780 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3), EC
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The GRAVY value for a protein
2023-02-06
The GRAVY value for a protein is calculated as the sum of hydropathy values of all the amino acids, divided by the number of residues in the sequence (Kyte and Doolittle, 1982). According to Kyte and Doolittle (1982) integral membrane proteins typically have higher GRAVY scores than do globular prot
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Introduction The MMR system keeps
2023-02-06
Introduction The MMR system keeps the fidelity of replication by repairing replication errors such as base-base mispairs and insertions/deletions. It plays a substantial role in restoring the fidelity of DNA and contributing to genome integrity [1]. The components of MMR are conserved in a broad ra
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For the TSH receptor signaling at the
2023-02-06
For the TSH receptor, signaling at the Golgi/trans-Golgi network appears required for both rapid effects of TSH − such as ACET sale depolymerization, which is implicated in thyroglobulin reuptake and, thus, thyroid hormone release − and late ones, such as those on gene transcription. Continued sign
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br Experimental section br Acknowledgements br Introduction
2023-02-06
Experimental section Acknowledgements Introduction DJ-1 is a highly conserved, homodimeric protein that was originally cloned as an oncogene capable of transforming leukotriene receptor antagonists in cooperation with activated ras[1]. DJ-1 is over-expressed in multiple tumor types and is
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multidrug resistance transporter Second the choice of the PA
2023-02-06
Second, the choice of the PAABD is critical for an efficient and sensitive biosensor. The sequence of the PAABD should present high affinity and efficient recognition of the phosphorylated substrate, as opposed to poor affinity for the unphosphorylated substrate, and should display a fully reversibl
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Maynard et al demonstrated that serum levels of sFlt
2023-02-06
Maynard et al. [54] demonstrated that serum levels of sFlt-1 were five times higher in pregnant women with PE than in normotensive women; as a consequence, VEGF and PlGF levels were found to be proportionally reduced in these women [54]. The literature confirms that there is a sharp increase in sFlt
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br Introduction Increased renin angiotensin system RAS
2023-02-06
Introduction Increased renin-angiotensin system (RAS) activity and inflammation in cardiovascular-related regions of the central nervous system contribute to the overactivity of neurohumoral systems that promote volume retention, cardiac remodeling and serious cardiac arrhythmias in systolic hear
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Breast Cancer Although androgens have been considered to be
2023-02-06
Breast Cancer: Although androgens have been considered to be a risk factor in prostate cancer they have been recommended to treat breast cancers. Even before the discovery of SERMs and aromatase inhibitors, steroidal androgens such as medroxyprogesterone and fluoxymesterone were used to treat breast
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Based on their different sources
2023-02-06
Based on their different sources, the APN inhibitors (APNIs) can be divided into the natural products and synthetic compounds. Bestatin (1, Fig. 1), isolated from the Streptomyces oliuoreticuli by Umezawa et al., is the first reported and only marketed natural dipeptidomimetic inhibitor of APN. Afte
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As one of emerging high throughout methods metabolomics dete
2023-02-06
As one of emerging high-throughout methods, metabolomics detects metabolites which are ultimate response of biological systems to environmental changes [14]. Metabolomics uncovers metabolic alteration at the systems level. Comparison of global metabolic profiling reflects some unidentified biologica
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br Introduction Cell motility is fundamentally important in
2023-02-03
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 SH-
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This study was funded and supported by Tehran University of
2023-02-03
This study was funded and supported by Tehran University of Medical Sciences and Health Services; and Iran National Science Foundation. Introduction The enzyme acetylcholinesterase (AChE) plays a central role in the signal transduction in the nervous system, hydrolyzing the neurotransmitter acet
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The reductase activity in patients with OHD as assessed
2023-02-01
The 5α-reductase activity in patients with 21-OHD, as assessed by the 5α-THF to 5β-THF (ratio 3) and by the 5α-17HP to 17HP (ratio 4) ratios, showed a similar pattern of activities (Fig. 2A–C) and significant correlations (ratio 1 vs. ratio 3; rs=0.67; pPicroside II to the 5α-reducase activity, the
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