Zobrazeno 1 - 10
of 97
pro vyhledávání: '"Felix Rohdich"'
Publikováno v:
CPT: Pharmacometrics & Systems Pharmacology, Vol 11, Iss 5, Pp 594-603 (2022)
Abstract Pan‐proteasome inhibitors (pPIs) significantly improve outcomes in patients with multiple myeloma; however, their indiscriminate inhibition of multiple proteasome and immunoproteasome subunits causes diverse toxicities, including thrombocy
Externí odkaz:
https://doaj.org/article/037f8e2d220e446cbde8d82c7134ae1e
Autor:
Paul A Clarke, Maria-Jesus Ortiz-Ruiz, Robert TePoele, Olajumoke Adeniji-Popoola, Gary Box, Will Court, Stephanie Czasch, Samer El Bawab, Christina Esdar, Ken Ewan, Sharon Gowan, Alexis De Haven Brandon, Phillip Hewitt, Stephen M Hobbs, Wolfgang Kaufmann, Aurélie Mallinger, Florence Raynaud, Toby Roe, Felix Rohdich, Kai Schiemann, Stephanie Simon, Richard Schneider, Melanie Valenti, Stefan Weigt, Julian Blagg, Andree Blaukat, Trevor C Dale, Suzanne A Eccles, Stefan Hecht, Klaus Urbahns, Paul Workman, Dirk Wienke
Publikováno v:
eLife, Vol 5 (2016)
Mediator-associated kinases CDK8/19 are context-dependent drivers or suppressors of tumorigenesis. Their inhibition is predicted to have pleiotropic effects, but it is unclear whether this will impact on the clinical utility of CDK8/19 inhibitors. We
Externí odkaz:
https://doaj.org/article/a201fbf6b4ca430996a70dd003f4f498
Publikováno v:
CPT: Pharmacometrics & Systems Pharmacology. 11:594-603
Pan-proteasome inhibitors (pPIs) significantly improve outcomes in patients with multiple myeloma; however, their indiscriminate inhibition of multiple proteasome and immunoproteasome subunits causes diverse toxicities, including thrombocytopenia. We
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::737e69991fcbb7976f128d0ceb596c71
https://doi.org/10.1002/psp4.12743
https://doi.org/10.1002/psp4.12743
Autor:
Brian H. Heasley, Jing Lin, Thomas F. N. Haxell, Igor Mochalkin, Constantin Neagu, Felix Rohdich, Ruoxi Lan, Amanda E. Sutton, Jennifer Jackson, Potnick Justin, Bayard R. Huck, Andreas Machl, Katrin Georgi, Xiaoling Chen, Sherer Brian A, Erik Wilker, Thomas E. Richardson, Anderson Clark, Reinaldo Jones, Johnson Theresa L, Lizbeth Celeste Deselm, Andreas Goutopoulos, Hui Tian, Yufang Xiao, Joseph A. Moore, Lindsey Crowley
Publikováno v:
Journal of Medicinal Chemistry. 64:14603-14619
Herein, we report the discovery of a novel class of quinazoline carboxamides as dual p70S6k/Akt inhibitors for the treatment of tumors driven by alterations to the PI3K/Akt/mTOR (PAM) pathway. Through the screening of in-house proprietary kinase libr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f0f668e1b7d0d3fdf120a40211a6894
https://doi.org/10.1021/acs.jmedchem.1c01087
https://doi.org/10.1021/acs.jmedchem.1c01087
Autor:
Floriane Lignet, Christina Esdar, Gina Walter-Bausch, Manja Friese-Hamim, Sofia Stinchi, Elise Drouin, Samer El Bawab, Andreas D. Becker, Claude Gimmi, Michael P. Sanderson, Felix Rohdich
Publikováno v:
The Journal of pharmacology and experimental therapeutics.
M3258 is an orally bioavailable, potent, selective, reversible inhibitor of the large multifunctional peptidase 7 (LMP7, β5i, PSMB8) proteolytic subunit of the immunoproteasome; a component of the cellular protein degradation machinery, highly expre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb0b32417eb18d77d30e0666a98cc907
https://pubmed.ncbi.nlm.nih.gov/36273822
https://pubmed.ncbi.nlm.nih.gov/36273822
Autor:
Felix Rohdich, Stefano Crosignani, Michael Busch, Christina Esdar, Manja Friese-Hamim, Markus Klein, Thomas Fuchss, Oliver Schadt, Djordje Musil, Ugo Zanelli, Michael P. Sanderson, Gina Walter-Bausch, Philip Hewitt, Jeyaprakashnarayanan Seenisamy
Publikováno v:
Journal of Medicinal Chemistry. 64:10230-10245
Proteasomes are broadly expressed key components of the ubiquitin-dependent protein degradation pathway containing catalytically active subunits (β1, β2, and β5). LMP7 (β5i) is a subunit of the immunoproteasome, an inducible isoform that is predo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1a3d051fc60306aef1b64a7ba1b3e7b
https://doi.org/10.1021/acs.jmedchem.1c00604
https://doi.org/10.1021/acs.jmedchem.1c00604
Autor:
Jeyaprakashnarayanan Seenisamy, Frank Becker, Djordje Musil, Jörg Bomke, Jakub Gunera, Uwe Eckert, Timo Heinrich, Felix Rohdich, Kerrin Hansen, Beatrix Blume, Christian Siegl, Frank Zenke, Jens Pfalzgraf, Dieter Spuck, Ansgar Wegener, Birgitta Leuthner, Melanie Dietz, Manja Friese-Hamim
Publikováno v:
Journal of Medicinal Chemistry. 62:11119-11134
The recently disclosed next generation of reversible, selective, and potent MetAP-2 inhibitors introduced a cyclic tartronic diamide scaffold. However, the lead compound 1a suffered from enterohepatic circulation, preventing further development. Neve
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::539fb7d602f3d1bbfe1d4a86e7331eb7
https://doi.org/10.1021/acs.jmedchem.9b01070
https://doi.org/10.1021/acs.jmedchem.9b01070
Autor:
Martin Lehmann, Djordje Musil, Daniel Kuhn, Richard Schneider, Daniela Radtki, Uwe Anlauf, Claudio Ritzert, Hans-Peter Buchstaller, Felix Rohdich, Christina Esdar, Dieter Dorsch, Birgitta Leuthner
Publikováno v:
Journal of Medicinal Chemistry. 62:7897-7909
Tankyrases 1 and 2 (TNKS1/2) are promising pharmacological targets that recently gained interest for anticancer therapy in Wnt pathway dependent tumors. 2-Aryl-quinazolinones were identified and optimized into potent tankyrase inhibitors through SAR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7371fae3b66367497e11c106cc91c92d
https://doi.org/10.1021/acs.jmedchem.9b00656
https://doi.org/10.1021/acs.jmedchem.9b00656
Autor:
Stefanie Gaus, Djordje Musil, Ugo Zanelli, Felix Rohdich, Markus Klein, Oliver Schadt, Michael Busch, Gina Walter-Bausch, Manja Friese-Hamim, Sondra L. Downey-Kopyscinski, Michael P. Sanderson, Christina Esdar, Constantine S. Mitsiades
Publikováno v:
Molecular cancer therapeutics. 20(8)
Large multifunctional peptidase 7 (LMP7/β5i/PSMB8) is a proteolytic subunit of the immunoproteasome, which is predominantly expressed in normal and malignant hematolymphoid cells, including multiple myeloma, and contributes to the degradation of ubi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8236bec98870a33c669340e4befd62d
https://pubmed.ncbi.nlm.nih.gov/34045234
https://pubmed.ncbi.nlm.nih.gov/34045234
Autor:
Felix Rohdich, Thorsten Knöchel, Hans-Peter Buchstaller, Mireille Krier, Birgitta Leuthner, Frank Zenke, Jörg Bomke, Timo Heinrich, Djordje Musil, Manja Friese-Hamim, Bertram Cezanne
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:551-556
The natural product fumagillin 1 and derivatives like TNP-470 2 or beloranib 3 bind to methionine aminopeptidase 2 (MetAP-2) irreversibly. This enzyme is critical for protein maturation and plays a key role in angiogenesis. In this paper we describe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e4009266f86ec7bd4e6ec260e57185a
https://doi.org/10.1016/j.bmcl.2016.12.019
https://doi.org/10.1016/j.bmcl.2016.12.019