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We have previously disclosed the discovery
2019-11-01
We have previously disclosed the discovery of a 7-azaindole-3-acetic Methyllycaconitine citrate CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosur
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Liproxstatin-1 In the course of carbohydrate metabolism
2019-11-01
In the course of carbohydrate metabolism, pyruvate, the end product of glycolysis, is converted to acetyl-CoA, which fuels the citrate cycle for further generation of energy. In the case of elevated levels of acetyl-CoA, acetyl-CoA is converted into malonyl-CoA by the action of acetyl-CoA carboxylas
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glycosylase inhibitor br The estrogen receptors History and
2019-11-01
The estrogen receptors: History and discovery In 1958, Elwood Jensen discovered the estrogen receptor, the first receptor ever encountered for any hormone, by showing that reproductive female tissues were able to uptake estrogen from the circulation by binding to proteins. He later demonstrated t
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CYP contributes to the metabolism of
2019-11-01
CYP450 contributes to the metabolism of more than 90% of currently available drugs (Shapiro and Shear, 2002). Currently, CYP1A is the most studied xenobiotic-metabolizing isoform in fish and is often used as a biomarker for early effects of pollutants in aquatic organisms (Havelkova et al., 2007). T
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Interestingly several ES cell lines are null for
2019-10-31
Interestingly, several ES cell lines are null for p53, possibly because the EWS-FLI1 chimeric protein can directly and indirectly interfere with p53 activity [38], [39]. The inhibition, loss and/or mutation of p53, one of the most common events in tumorigenesis, results in a decreased oxygen consump
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Initial investigations in the heart uncovered Epac as a posi
2019-10-31
Initial investigations in the heart uncovered Epac as a positive regulator of myocyte hypertrophy [8], [9]. Concomitantly, Epac has been shown to regulate cardiac Ca homeostasis [8], [10], [11], [12], [13]. Ca is an essential second messenger in the cardiac physiology because its rhythmic variations
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Grapiprant is a selective antagonist
2019-10-31
Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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br Disclosures br Acknowledgements This work was
2019-10-31
Disclosures Acknowledgements This work was supported by the Natural Science Foundation of China (No. 81560587); the Fok Ying-Tong Education Foundation of China (No. 151107), the basic ability promotion project for young and middle-aged teachers in Universities in Guangxi (No. 2018KY1146) and t
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br Orthotopic liver transplantation OLT is the
2019-10-31
Orthotopic liver transplantation (OLT) is the only curative therapy available for patients with end-stage liver disease. The surgical procedure of liver transplantation inherently involves cold ischemia during graft preservation , followed by reperfusion of the transplanted graft which results in
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br Author contribution br Acknowledgements We want
2019-10-31
Author contribution Acknowledgements We want to thank Dr. Manuel Rodriguez, Dr. Ch. Blattner, Dr. Jorge Moscat, Dr. Erwin Knecht and Dr. Peter Tontonoz for materials. This work has been supported by grants from the Spanish Ministry of Education and ScienceSAF2011-27442 and a grant from General
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HCV has evolved mechanisms to evade humoral immune responses
2019-10-31
HCV has evolved mechanisms to evade humoral immune responses including high functional flexibility and variability of immunogenic portions of its envelope proteins. The highest sequence variability occurs in the first 27 Octreotide acetate of the N-terminus of E2, which is referred to as the hyperva
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Mulan protein level is regulated with conditions that stimul
2019-10-31
Mulan protein level is regulated with conditions that stimulate mitophagy such as treatment of SAR405838 with CCCP [12]. We found that exogenously expressed GFP-GABARAP and RFP-Mulan could co-precipitate and co-localize in mammalian cells and the degree of co-localization increased when the cells w
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AT-406 br Experimental Procedures br Author Contributions br
2019-10-31
Experimental Procedures Author Contributions Acknowledgments Research in the Davis laboratory was supported by grants 4R37NS019904, 5R01NS052351, and 1R35NS097224 from NINDS. Research in the Martemyanov laboratory was supported by grants DA036596 and DA026405 from NIDA, and MH105482 from NI
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br Material and methods br Results and discussion br
2019-10-31
Material and methods Results and discussion Conclusions Acknowledgements S. De thanks DST, New Delhi for generous grant of the SERC Fast Track Scheme No. SR/FT/CS-057/2008. R. Kundu thanks the University of Kalyani for financial assistance. We are grateful to Prof. K. Bhattacharyya of IA
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Common enzyme quantitative methods include enzyme linked imm
2019-10-31
Common enzyme quantitative methods include enzyme-linked immunosorbent assay [,] (ELISA), chemiluminescence (CLIA) [, , ] and immunochromatography []. The advantages of ELISA are cost reduction and automation, but non-specific reaction caused by HOOK effect, false positive caused by cross-contamina
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