Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Eddy Damen"'
Autor:
Erik H. Heijne, Christopher D. Hupp, John W. Cuozzo, Anthony D. Keefe, Rob Winkel, L. Babiss, Wendy van Bruggen, Louis Renzetti, Mark J. Mulvihill, Birgit Zech, Andrew J. McRiner, Johan J. N. Veerman, Eddy Damen, Yorik B. Bruseker, Heather A. Thomson, Julie Liu, Gerhard Müller, Koen F. W. Hekking, Ying Zhang, Peter van Rijnsbergen
Publikováno v:
ACS Medicinal Chemistry Letters. 12:555-562
Herein we report the discovery of 2,4-1H-imidazole carboxamides as novel, biochemically potent, and kinome selective inhibitors of transforming growth factor β-activated kinase 1 (TAK1). The target was subjected to a DNA-encoded chemical library (DE
Autor:
Eddy Damen, Albert Galera-Prat, Piotr Nieczypor, Jo Waaler, Sudarshan Murthy, Sven T. Sowa, Sjoerd Aertssen, Ruben Gerardus George Leenders, Max Lycke, Marc Nazaré, Shoshy Alam Brinch, Stefan Krauss, Lari Lehtiö, Anita Wegert
Publikováno v:
Journal of Medicinal Chemistry
Tankyrases 1 and 2 are central biotargets in the WNT/β-catenin signaling and Hippo signaling pathways. We have previously developed tankyrase inhibitors bearing a 1,2,4-triazole moiety and binding predominantly to the adenosine binding site of the t
Autor:
Christoph Schächtele, Jan E. Ehlert, Ruben Gerardus George Leenders, Daniel Müller, Daniel Feger, Danny C. Lenstra, Jasmin Mecinović, Federica Trivarelli, Remco Zijlmans, Gerhard Müller, Bart van Bree, Anita Wegert, Marc van de Sande, Eddy Damen, Carolin Heidemann-Dinger, Michael H.G. Kubbutat
Publikováno v:
Bioorganic & Medicinal Chemistry Letters, 29, 2516-2524
Bioorganic & Medicinal Chemistry Letters, 29, 17, pp. 2516-2524
Bioorganic & Medicinal Chemistry Letters, 29, 17, pp. 2516-2524
Detailed structure activity relationship of two series of quinazoline EHMT1/EHMT2 inhibitors (UNC0224 and UNC0638) have been elaborated. New and active alternatives are presented for the ubiquitous substitution patterns found in literature for the li
Autor:
Ruben G. G. Leenders, Shoshy Alam Brinch, Sven T. Sowa, Enya Amundsen-Isaksen, Albert Galera-Prat, Sudarshan Murthy, Sjoerd Aertssen, Johannes N. Smits, Piotr Nieczypor, Eddy Damen, Anita Wegert, Marc Nazaré, Lari Lehtiö, Jo Waaler, Stefan Krauss
Publikováno v:
Journal of Medicinal Chemistry
Tankyrase 1 and 2 (TNKS1/2) catalyze post-translational modification by poly-ADP-ribosylation of a plethora of target proteins. In this function, TNKS1/2 also impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8427ede283b6e2e612e0c012c6a2929
http://hdl.handle.net/10852/92113
http://hdl.handle.net/10852/92113
Autor:
Johan J N, Veerman, Yorik B, Bruseker, Eddy, Damen, Erik H, Heijne, Wendy, van Bruggen, Koen F W, Hekking, Rob, Winkel, Christopher D, Hupp, Anthony D, Keefe, Julie, Liu, Heather A, Thomson, Ying, Zhang, John W, Cuozzo, Andrew J, McRiner, Mark J, Mulvihill, Peter, van Rijnsbergen, Birgit, Zech, Louis M, Renzetti, Lee, Babiss, Gerhard, Müller
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein we report the discovery of 2,4-1H-imidazole carboxamides as novel, biochemically potent, and kinome selective inhibitors of transforming growth factor β-activated kinase 1 (TAK1). The target was subjected to a DNA-encoded ch
Autor:
Danny C. Lenstra, Ruben Gerardus George Leenders, Jasmin Mecinović, Richard H. Blaauw, Anita Wegert, Eddy Damen, Floris P. J. T. Rutjes
Publikováno v:
Chemmedchem, 13, 14, pp. 1405-1413
Chemmedchem, 13, 1405-1413
Chemmedchem, 13, 1405-1413
SETD7 is a histone H3K4 lysine methyltransferase involved in human gene regulation. Aberrant expression of SETD7 has been associated with various diseases, including cancer. Therefore, SETD7 is considered a good target for the development of new epig
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ad6207eb960f60220fdb327ae3daa2c
https://doi.org/10.1002/cmdc.201800242
https://doi.org/10.1002/cmdc.201800242