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When studying the potential of HATi for the treatment
2022-05-24
When studying the potential of HATi for the treatment of inflammatory lung diseases, investigating lung tissue specific effects may be particularly relevant since local administration of small molecule inhibitors in lung tissue is possible and is already applied for inhaled glucocorticoids in the tr
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GSK dimethylpiperidin yl butoxy phenyl piperidine carbonyl n
2022-05-24
GSK-835726 (3-[4-[4-[4-[4-(3,3-dimethylpiperidin-1-yl)butoxy]phenyl]piperidine-1-carbonyl]naphthalen-1-yl]propanoic acid) is a dual H1/H3 receptor antagonist with the potential to be used in allergic rhinitis. Likewise GSK-1004723, the drug-likeness criteria have not been passed by this drug candida
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In cancer cells HIF upregulates HK
2022-05-24
In cancer cells, HIF-1α upregulates HK-II expression by binding to the hypoxia-responsive element in the HK-II promoter region to adapt to hypoxic conditions [20]. In the present study, we observed that mangiferin transiently increased HIF-1α expression in endothelial cells, suggesting another possi
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Second although HO expression in the
2022-05-24
Second, although HO-1 expression in the stromal macrophages has been seen in the other cancer tissues [21], the impact of HO-1 expression on EAOC progression has not been explored. We have found that the CD163+ M2-like Ticlopidine HCl were HO-1+ in OE, but malignant transformation may be associated
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br Introduction Soluble guanylyl cyclase GC maintains vascul
2022-05-24
Introduction Soluble guanylyl cyclase (GC-1) maintains vascular function through the NO/GC-1/cGMP pathway [1,2] by catalyzing the conversion of GTP into cGMP (Fig. 1). The GC-1 heme prosthetic group binds NO with picomolar affinity, resulting in a 100- to 200-fold increase in catalytic activity.
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Human GPR hGPR was originally isolated in
2022-05-24
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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Compounds and were tested for pharmacodynamic
2022-05-24
Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a
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Our last area of exploration was the piperidine
2022-05-24
Our last area of exploration was the piperidine core as shown in . We rationalised that the basicity of the nitrogen (measured p=7.0) may be responsible for the affinity for the hERG receptor and we therefore sought to moderate this by incorporation of electronegative groups at the 3-position. To th
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To determine the functional consequences of HIV gp
2022-05-24
To determine the functional consequences of HIV gp120 binding to vaginal epithelial cells, an annotation clustering of the differentially expressed genes was performed. The top enriched biological processes included an inflammatory immune response, defense response and the pathways included the SODD
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Through the analysis of various synthetic GPR
2022-05-23
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic cAMPS-Rp, triethylammonium salt motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early per
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br Conclusions br Acknowledgements br Introduction Glucose m
2022-05-23
Conclusions Acknowledgements Introduction Glucose metabolism is vital to prepare uterine epithelium and stroma for embryo implantation and for the differentiation of the functionalis layer to support the developing conceptus [[1], [2], [3], [4]]. Due to its polar nature and hydrophilic cond
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br Conclusion In conclusion we discovered
2022-05-23
Conclusion In conclusion, we discovered a pair of novel epimers CBC and CBD from plant C. bungei. These two natural compounds inhibit Hh pathway by blocking signaling at the level of Gli. They are effective in suppressing Hh pathway-dependent medulloblastoma growth in vitro and in vivo. Furthermo
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In addition to inactivation of Notch we found that the
2022-05-23
In addition to inactivation of Notch, we found that the combination of BTZ and GSI-I downregulated ERK phosphorylation in ALK+ ALCL cells, and we speculate this may occur through the inhibition of upstream regulators of the ERK pathway. These findings emphasize the functional complementation of the
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Single cell reverse transcriptase PCR on A mellifera antenna
2022-05-23
Single-cell reverse transcriptase-PCR on A. mellifera antennal lobe (AL) cells showed the expression of RDL as well as another GABA receptor like subunit, LCCH3 (Dupuis et al., 2010). Based on whole cell patch-clamp electrophysiology it was concluded that the predominant GABA receptors in AL cells a
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br Introduction As a fundamental metal
2022-05-23
Introduction As a fundamental metal-dependent hydrolytic enzyme, inorganic pyrophosphatase (PPase) exhibits a specific catalytic ability, in which one molecule of inorganic pyrophosphate (PPi) can be transformed into two orthophosphate (Pi) ions [1,2]. The process of transformation is extremely e
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