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dhfr inhibitor The first rationally designed dual mPGES LO i
2024-07-19
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic dhfr inhibitor - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been syn
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Nevertheless though the LO pathway dictates the
2024-07-19
Nevertheless, though the 5-LO pathway dictates the production of lipid mediators with opposite roles in the immune reactions, like LTs and LXA4 [32], our results seemed to corroborate others that pointed to LTB4 as an outstanding mediator involved in persistent and chronic inflammatory skin diseases
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The observation that vortioxetine blocks HT induced currents
2024-07-19
The observation that vortioxetine blocks 5-HT-induced currents in 5-HT3 receptor-expressing oocytes suggests that vortioxetine acts to functionally antagonize these receptors, and is in line with previously published data (Bang-Andersen et al., 2011). For example, Mørk et al. (2012) demonstrated tha
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Acknowledgments br P c is expressed in several steroidogenic
2024-07-19
Acknowledgments P450c17 is expressed in several steroidogenic tissues, including the adrenal cortex, the ovary, and the testes (). Thus, 17α-hydroxylase/17,20-lyase is a key enzyme required for the production of both cortisol and sex steroids. This enzyme defect blocks the synthesis of cortisol,
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Although we have achieved a great deal of
2024-07-19
Although we have achieved a great deal of success in the development of tools to understand autophagy in health and disease, highly specific reagents for autophagy manipulation and deep knowledge of autophagy is required to advance the research in therapeutic treatment. Better disease (ischemia) ani
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Phagosomes acquire some hydrolases early during their journe
2024-07-19
Phagosomes acquire some hydrolases early during their journey from the cell surface to lysosomes. An example for such hydrolase is cathepsin H which is most concentrated in the early phagosome at a pH of approximately 6.3 (Claus et al., 1998), the pH optimum of enzyme activity (Schwartz and Barrett,
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It is increasingly evident that many
2024-07-19
It is increasingly evident that many metabolic genes are associated with cancer progression of various tumor cells, including NSCLC. In particular, GLUT1 overexpression has been reported in NSCLC, and correlations between GLUT1 expression and a number of clinical parameters such as gender, smoking s
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We used the lead compound C
2024-07-19
We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system.
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In this paper we described synthesis biological evaluation a
2024-07-19
In this paper, we described synthesis, biological evaluation and docking study of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives 4a–o as 15-lipoxygenase inhibitors. Results and discussion Conclusion We designed and synthesized a novel of thiourea derivatives containing phenylsulfonamide mo
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Somatostatin analogs also bind to somatostatin receptors It
2024-07-19
Somatostatin analogs also bind to somatostatin receptors. It has been reported that octreotide has a high affinity for hSSTR2, moderate affinity for hSSTR3 and hSSTR5, and does not bind to hSSTR1 or hSSTR4 (Ben-Shlomo and Melmed 2008). Compared to octreotide, pasireotide displays 40-, 30-, and 5-fol
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However from our meta analysis emerge
2024-07-18
However, from our meta-analysis emerge some strategic considerations for the continued use of antiangiogenic drugs for glioblastoma patients: Conflict of interest Funding Introduction Angiogenesis is a physiological process involving the formation of new blood vessels from pre-existing blo
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Introduction Cardiovascular disease is the
2024-07-18
Introduction Cardiovascular disease is the principal cause of morbidity and mortality in patients with lobeline australia (1). Comprehensive management of these patients includes not only adequate glycemic control but also attention to additional recognized risk factors. Hypertension is a cardiovas
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The specific mechanism and neurotoxic
2024-07-18
The specific mechanism and neurotoxic Aβ Hydroxysafflor yellow A are yet to be elucidated, however recent studies have provided significant evidence for the amyloid channel hypothesis. These reports have established that relatively small oligomers ( Conflict of interest Acknowledgements This wo
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With regard to participation of the S
2024-07-18
With regard to participation of the 12S-lipoxygenase in diabetes mellitus, inconsistent results have been obtained. Earlier studies demonstrated that the leukocyte-type 12S-lipoxygenase is specifically expressed in pancreatic b-cells and is involved in regulating glucose-stimulated insulin secretion
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Altogether the situations described above clearly impede the
2024-07-17
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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