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A new series of pyrimidones
2022-02-03
A new series of pyrimidones (14) with C-7 and C-9 modifications were furnished consisting of a hydroxypyridinone and a thiazole ring and checked against raltegravir resistant HIV mutant strains to determine their in vitro anti-HIV IN potency. Compounds 14a–14a, 14b–14b and 14c–14c appeared with 6.4
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Sometime ago we have described diamino triazines as histamin
2022-02-01
Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by SGX-523 and zymosan. In this work we describe new derivati
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GSK 1120212 br Discussion br Conflict of interest
2022-02-01
Discussion Conflict of interest Acknowledgements We thank Rosetta Barkley for expert technical assistance. We thank Robin Maser, James Calvet, Darren Wallace, and Jovanka Koo for many helpful discussions and expert technical advice. This work was supported by National Institutes of Health,
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Human GPR hGPR was originally isolated in as
2022-02-01
Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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br Acknowledgements This work was supported by
2022-02-01
Acknowledgements This work was supported by the grants from National key Basic Research Program of China (2012CB124702), 948 Program (2015-Z33), National Natural Science Foundation of China (31172093, 31301947), the National Science Foundation for Fostering Talents in Basic Research (J1103510), S
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br Glucose metabolism and diet
2022-01-31
Glucose metabolism and diet Glucokinase is essential for sensing blood glucose levels, thus controls metabolism (Iynedjian, 1993, Iynedjian, 2009, Postic et al., 2001, Agius, 2008). Loss of glucokinase activity in humans and mice leads to diabetes (Printz et al., 1993b, Postic et al., 2001, Agius
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br Voltage dependent anion channel VDAC is a ubiquitous
2022-01-31
Voltage-dependent anion channel VDAC is a ubiquitous protein showing well conserved structural and functional properties in spite of major variations in its sequence (for review see [50]). Most of what we know about VDAC electrophysiological properties (for reviews, see [51], [52]) was initially
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br Experimental br Results and
2022-01-31
Experimental Results and discussion Conclusion In conclusion, four bisnaphthalimides have been investigated for their potential G-quadruplex binding. The compounds 3a, 3b and 5b display high affinity for telomeric and oncogenic G-quadruplexes. On the other hand, 5a only show high affinity f
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Glucose metabolic pathways are well defined but the
2022-01-31
Glucose metabolic pathways are well defined but the subcellular organization of these pathways is poorly understood in liver and kidney. Several factors affect the net flux of gluconeogenesis and allow the orphan receptor to respond to physiological changes [1]. Ovadi and Srere have suggested that
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br Factor Xa an enzyme in the
2022-01-31
Factor Xa, an enzyme in the coagulation cascade, has recently been identified as having a role in inflammation, generating interest in factor Xa inhibitors as anti-inflammatory agents beyond their established use as anticoagulants [, , , ]. We report sustained clinical and electrophysiologic impro
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Septic shock a condition where endothelium
2022-01-31
Septic shock, a condition where endothelium-derived substances most likely play an important role, is often accompanied by cardiac dysfunction, pulmonary hypertension, systemic hypotension and impaired oxygen utilisation with systemic acidosis (Vincent, 1998). Experimental endotoxaemia shows a simil
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In order to establish proper folding and enzymatic activity
2022-01-31
In order to establish proper folding and enzymatic activity, G9a and GLP methyltransferases each contain four structural zinc ions. Both Tie2 kinase inhibitor synthesis contain two distinguishable types of zinc fingers; three Zn(II) ions are chelated in a triangular cluster by 9 cysteines (b, top l
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br Notch Similar to the Wnt
2022-01-30
Notch Similar to the Wnt and Hedgehog pathways as discussed earlier, Notch is an evolutionarily conserved primordial developmental pathway which affects patterning, and has an important role to play in cancer biology ranging from angiogenesis to cancer stem LXR-623 to tumor immunity [88]. Notch
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br GC C and cGMP
2022-01-30
GC-C and cGMP: of mice and men As is usually the case for many genes, most of the studies that relate to GC-C have to date been carried out in mouse models, or in cell lines derived from human colorectal cancer tissue. What appeared to be a lacuna was any report of a human disorder that resulted
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Conflict of Interest The authors have no conflicts of
2022-01-30
Conflict of Interest: The authors have no conflicts of interest to declare. Acknowledgments Understanding Pulmonary Remodeling The effects of serotonin (5-hydroxytryptamine, 5-HT) class 2 receptors (5-HT2) on airway function and remodeling in respiratory disorders are unclear. Using murine p
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