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Altogether the situations described above clearly impede the
2023-12-14
Altogether, the situations described above clearly impede the critical steps of drug discovery and development and the scientific process in general [14]. In conclusion, it is the opinion of these authors that many exciting lines of drug discovery (which includes those devoted to nAChR ligands) have
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Compounds were profiled for their inhibitory activity
2023-12-14
Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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The discovery of acetylsalicylic acid aspirin
2023-12-14
The discovery of acetylsalicylic Nicotine Difartrate (aspirin) in 1897 paved the way for the development of classical NSAIDs as first-line therapeutics for anti-inflammatory, anti-pyretic and analgesic therapy. Large efforts have been made in the following decades to improve the efficacy and in par
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LO is a soluble kDa enzyme composed of an
2023-12-14
5-LO is a soluble 78 kDa enzyme, composed of an α-helix-rich catalytic domain and a regulatory β-sheet-rich C2-like domain. Depending on the cell type, 5-LO may be located in the cytosol, in the nucleoplasm, or in both compartments (Werz, 2002). Upon cell stimulation by agents that elevate intracell
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br Conclusion In this brief Letter we
2023-12-14
Conclusion In this brief Letter, we report an easy method for the preparation of the antileukemic natural product 1. Using a biomimetic strategy,1, 8 in which the aromatic residues are attached to a lysine moiety prior to the reduction of the central carboxylate group, a step-economical synthesis
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The inhibition of the exacerbated inflammatory response that
2023-12-14
The inhibition of the exacerbated inflammatory response that follows injury may be an alternative approach to induce a more efficient repair [17,83]. In line with that, 5-LO is one of the most consolidated targets for dampening inflammation, mainly through the therapeutic effects of 5-LO inhibitors
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LO is a soluble kDa enzyme composed of an
2023-12-14
5-LO is a soluble 78 kDa enzyme, composed of an α-helix-rich catalytic domain and a regulatory β-sheet-rich C2-like domain. Depending on the cell type, 5-LO may be located in the cytosol, in the nucleoplasm, or in both compartments (Werz, 2002). Upon cell stimulation by agents that elevate intracell
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The present work has implications for our thinking about the
2023-12-14
The present work has implications for our thinking about the effects of antidepressant (e.g. SSRIs) use on maternal care in depressed mothers which consist of approximately 10–20% of all mothers (Gjerdingen and Yawn, 2007, Susser et al., 2016), and more than 40% of depressed mothers are prescribed w
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Whereas more research is needed to
2023-12-14
Whereas more research is needed to identify the precise mechanism by which FIN exerts its antidyskinetic effect, the DMP 777 that it can negatively modulate dopaminergic transmission is also supported by our previous findings. Indeed, we have previously shown that FIN completely reversed the behavio
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The original Aurora kinase was identified during a phenotypi
2023-12-13
The original Aurora kinase was identified during a phenotypic screen for defects in mitotic spindles in Drosophila mutants. Aurora mutants were so named because of the morphological defects at the mitotic spindle resembling the Aurora borealis, or the Northern light [4]. The structure of the Auroras
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glutathione s-transferase br Acknowledgments br Introduction
2023-12-13
Acknowledgments Introduction Human innate immune system provides first line of defense against multiple viral or bacterial attacks, and provides critical surveillance against oncogenic development. Evidences show that individuals with primary immunodeficiency or induced immunosuppression durin
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Molecular docking quantitative structure activity relationsh
2023-12-13
Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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Thus a majority of known chemical and physico chemical metho
2023-12-13
Thus, a majority of known chemical and physico-chemical methods of metallic ions assay has a number of disadvantages, such as a low sensitivity and selectivity, high costs and complexity of the equipment. Therefore, the development of simple cost-effective sensitive methods of quantitative analysis
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Natural compounds present in medicinal and or nutritional pl
2023-12-13
Natural compounds, present in medicinal and/or nutritional plants as well as in macrofungi sources, have stimulated a great interest from the pharmaceutical industry. Different natural compounds such as phenolic compounds, alkaloids, terpenoids among others, have shown strong antiangiogenic effects
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br Available treatment modalities for
2023-12-13
Available treatment modalities for individuals with NAFLD There are several treatment modalities currently used or in clinical trials for individuals with NAFLD. The most widely recommended treatment is a lifestyle modification plan. As little as 5% weight loss has been shown to improve NASH hist
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