Zobrazeno 1 - 10
of 74
pro vyhledávání: '"Yafeng Xue"'
Autor:
Iain A. Cumming, Sébastien L. Degorce, Anna Aagaard, Erin L. Braybrooke, Nichola L. Davies, Coura R. Diène, Andrew J. Eatherton, Hannah R. Felstead, Sam D. Groombridge, Eva M. Lenz, Yunxia Li, Youfeng Nai, Stuart Pearson, Graeme R. Robb, James S. Scott, Oliver R. Steward, Chengyan Wu, Yafeng Xue, Lanping Zhang, Yanxiu Zhang
Publikováno v:
Bioorganicmedicinal chemistry. 63
In this article, we report the discovery of a series of pyrimidopyridones as inhibitors of IRAK4 kinase. From a previously disclosed 5-azaquinazoline series, we found that switching the pyridine ring for an N-substituted pyridone gave a novel hinge b
Autor:
Jennifer H. Pink, James S. Scott, Nicola Lindsay, Alan Rosen, Andrew Bloecher, Yafeng Xue, Lisa Drew, Sébastien L. Degorce, Graeme R. Robb, Christopher Thomas Halsall, Rana Anjum, Eva M. Lenz, Rodrigo J. Carbajo, Keith Dillman, Michele Mayo
Publikováno v:
Journal of Medicinal Chemistry. 62:9918-9930
In this article, we report the discovery of a series of 5-azaquinazolines as selective IRAK4 inhibitors. From modestly potent quinazoline 4, we introduced a 5-aza substitution to mask the 4-NH hydrogen bond donor (HBD). This allowed us to substitute
Autor:
Roine I. Olsson, Rikard Pehrson, Rongfeng Chen, Jesper Malmberg, Anna Malmberg, Nafizal Hossain, Hanna Grindebacke, Mia Collins, Matti Lepistö, Yao Xiong, Nina Krutrök, Antonio Llinas, Thomas Hansson, Eva L. Hansson, Elisabeth Bäck, Anna Aagaard, Jane McPheat, Linda Thunberg, Sarah Lever, Agnes Leffler, Yafeng Xue, Stefan von Berg, Petter Svanberg, Frank Narjes, Marie Ramnegård, Glyn Hughes, Johan Jirholt
Publikováno v:
Journal of medicinal chemistry. 64(18)
Inverse agonists of the nuclear receptor RORC2 have been widely pursued as a potential treatment for a variety of autoimmune diseases. We have discovered a novel series of isoindoline-based inverse agonists of the nuclear receptor RORC2, derived from
Autor:
James M. Smith, Rana Anjum, Sébastien L. Degorce, Ina Terstiege, Turner Paul, Stuart E. Pearson, Michael J. Tucker, Alexandra L. Orton, Charlene Fallan, Graeme Scarfe, Anna Aagaard, James S. Scott, Oliver R. Steward, Yafeng Xue, Iain A. Cumming, Tony Johnson, Gail L. Wrigley, Karl-Johan Leuchowius, Stephen D. Wilkinson, Graeme R. Robb, Coura R. Diène, Alan Rosen
Publikováno v:
Bioorganicmedicinal chemistry. 28(23)
In this article, we report our efforts towards improving in vitro human clearance in a series of 5-azaquinazolines through a series of C4 truncations and C2 expansions. Extensive DMPK studies enabled us to tackle high Aldehyde Oxidase (AO) metabolism
Autor:
Hanna Grindebacke, Frank Narjes, Eva L. Hansson, Yao Xiong, Antonio Llinas, Linda Thunberg, Jesper Malmberg, Stefan Tångefjord, Roine I. Olsson, Ge Hongbin, Rongfeng Chen, Yafeng Xue, Agnes Leffler, Hanna Leek, Thomas Hansson, Elisabeth Bäck, Jane McPheat, Nafizal Hossain, Matti Lepistö, Stefan von Berg, Johan Jirholt, Anna Aagaard
Publikováno v:
Journal of Medicinal Chemistry. 61:7796-7813
Retinoic acid receptor related orphan receptor γt (RORγt), has been identified as the master regulator of TH17-cell function and development, making it an attractive target for the treatment of autoimmune diseases by a small-molecule approach. Here
Autor:
Hanna Tegel, Jerry Eriksson, Mei Ding, Teodor Aastrup, Åsa Sivertsson, Mathias Uhlén, Douglas Ross-Thriepland, Lovisa Holmberg Schiavone, Sophia Hober, Lisa U. Magnusson, Rick Davies, Yafeng Xue, Fredrik Wågberg, Diluka Peiris, Marjorie Chimienti, Jenny Bernström, Piero Ricchiuto, Per-Erik Strömstedt, Ulla Karlsson, Karin Jennbacken
Publikováno v:
International Journal of Molecular Sciences
Volume 20
Issue 23
Volume 20
Issue 23
Paracrine factors can induce cardiac regeneration and repair post myocardial infarction by stimulating proliferation of cardiac cells and inducing the anti-fibrotic, antiapoptotic, and immunomodulatory effects of angiogenesis. Here, we screened a hum
Autor:
Sébastien L, Degorce, Rana, Anjum, Andrew, Bloecher, Rodrigo J, Carbajo, Keith S, Dillman, Lisa, Drew, Christopher T, Halsall, Eva M, Lenz, Nicola A, Lindsay, Michele F, Mayo, Jennifer H, Pink, Graeme R, Robb, Alan, Rosen, James S, Scott, Yafeng, Xue
Publikováno v:
Journal of medicinal chemistry. 62(21)
In this article, we report the discovery of a series of 5-azaquinazolines as selective IRAK4 inhibitors. From modestly potent quinazoline
Autor:
Stefan von Berg, Yafeng Xue, Mia Collins, Antonio Llinas, Roine I. Olsson, Torbjörn Halvarsson, Maria Lindskog, Jesper Malmberg, Johan Jirholt, Nina Krutrök, Marie Ramnegård, Marie Brännström, Anders Lundqvist, Matti Lepistö, Anna Aagaard, Jane McPheat, Eva L. Hansson, Rongfeng Chen, Yao Xiong, Thomas G. Hansson, Frank Narjes
Publikováno v:
ACS Med Chem Lett
[Image: see text] The further optimization of a recently disclosed series of inverse agonists of the nuclear receptor RORC2 is described. Investigations into the left-hand side of compound 1, guided by X-ray crystal structures, led to the substitutio
Autor:
David Karis, Hans-Georg Beisel, Carina A Johansson, Stefan Bäckström, Tommy Olsson, Mattias Rohman, Linda Öster, Yafeng Xue
Publikováno v:
ChemMedChem. 11:497-508
Soluble epoxide hydrolase (sEH) is involved in the regulation of many biological processes by metabolizing the key bioactive lipid mediator, epoxyeicosatrienoic acids. For the development of sEH inhibitors with improved physicochemical properties, we
Autor:
Rongfeng Chen, Hanna Grindebacke, Pia Hansson, Agnes Leffler, Yafeng Xue, Stefan von Berg, Roine I. Olsson, Hongbin Ge, Eva L. Hansson, Thomas Hansson, Jane McPheat, Johan Jirholt, Yao Xiong, Jenny Bernström, Frank Narjes, Anna Aagaard
Publikováno v:
ChemMedChem. 11:207-216
RORγt, an isoform of the retinoic acid-related orphan receptor gamma (RORc, RORγ), has been identified as the master regulator of T-helper 17 (TH 17) cell function and development, making it an attractive target for the treatment of autoimmune dise