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br Conclusion Leukocytes adhesion to endothelial cells is
2022-03-18

Conclusion Leukocytes adhesion to endothelial cells is one of the most critical event in the inflammatory response. In presented paper using a relevant model of adhesion we have demonstrated that histamine influence eosinophils adhesion to endothelium. This effect appears to be mediated by H4 his
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br HO and cerebral malaria In a post
2022-03-18

HO-1 and cerebral malaria In a post-mortem evaluation of human cerebral (falciparum) malaria, strong HO-1 immunostaining was consistently noted in microglia/macrophages within and surrounding the pathognomonic Durck’s granulomas (Schluesener et al., 2001). As witnessed in cerebral trauma specimen
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br Acknowledgments br Introduction Histone deacetylases
2022-03-18

Acknowledgments Introduction Histone deacetylases (HDACs) related to tumor suppressor genes have become promising targets for the treatment of cancer [1,2]. Under the normal physiological conditions, Histone acetyltransferases (HATs) and histone deacetylases (HDACs) together regulate the acety
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Ras small GTPases are critical molecular switches that conne
2022-03-18

Ras small GTPases are critical molecular switches that connect extracellular signals to intracellular signaling pathways initiated by membrane receptors, such as growth factor receptors and G protein-coupled receptors (Simanshu et al., 2017). When shifting between active GTP-bound and inactive GDP-b
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br Discussion Regulation of redox homeostasis is
2022-03-18

Discussion Regulation of redox homeostasis is critical in the maintenance of normal cell functions, and both glutathione S-transferase and peroxiredoxin enzymes are important contributors to this process. There are numerous reports of aberrant expression patterns of GSTP linked with cancer and wi
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All experiments in this study were performed
2022-03-18

All experiments in this study were performed at pD 6.1 for reasons described above. This leaves a question about the implications of stereochemistry in vivo. At physiological pH the GSTP1-1 catalyzed rate of EASG formation is only 1.1-fold higher than the non-enzymatic rate [26]. However, when human
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br Conclusions br Introduction G
2022-03-18

Conclusions Introduction G protein-coupled receptors (GPRs) share common structural motifs, including seven transmembrane helices, and the ability to activate heterotrimeric G proteins such as Gs, Gi, Gq and G12/13. A variety of GPR cellular functions are mediated by second messengers such as
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In summary through medicinal chemistry design and
2022-03-18

In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on
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GPR A a G protein coupled receptor located mainly
2022-03-18

GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic AP 24534 [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-mediated
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br AUTHOR CONTRIBUTIONS br ACKNOWLEDGMENTS br Introduction C
2022-03-18

AUTHOR CONTRIBUTIONS ACKNOWLEDGMENTS Introduction Chronic neuropathic pain is a common symptom in patients with human immunodeficiency virus (HIV)-1 infection. Glycoprotein 120 (gp120) is an HIV-1 protein that can cause pain behaviors in animal models (Hao, 2013, Nasirinezhad et al., 2015,
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The two competitive bivalent GlxI
2022-03-18

The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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The monomer composition and the variation
2022-03-17

The monomer composition and the variation in the cryogelation process can result in cryogels with slightly different properties. The adequate characterization of these matrices is advisable in the studies aiming a better understanding of flow inside its structure and also the interactions between th
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The effects of GHS R a blockade on
2022-03-17

The effects of GHS-R1a blockade on alcohol-related outcomes have been examined in numerous preclinical experiments, utilizing various GHS-R1a antagonists (JMV 2959, [D-Lys3]-GHRP-6, BIM 28163) and rodent species (prairie vole, mouse, rat). In spite of methodological differences, the results consiste
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Receptor tyrosine kinases RTKs consist of subfamilies
2022-03-17

Receptor tyrosine kinases (RTKs) consist of 20 subfamilies in humans, all of which share a common structure consisting of extracellular ligand-binding region, a single-pass transmembrane domain and an intracellular tyrosine kinase domain [2]. Binding of a growth factor to the ligand-binding domain r
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br Significance Metabolites present in the
2022-03-17

Significance Metabolites present in the extracellular environment can potently modulate cellular phenotypes and potentially serve as therapeutics for various diseases. Ferroptosis is a non-apoptotic cell death process characterized by the generation of toxic lipid reactive oxygen species (ROS). I
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