J
Johannes Roesel
Researcher at Novartis
Publications - 42
Citations - 3158
Johannes Roesel is an academic researcher from Novartis. The author has contributed to research in topics: Tyrosine kinase & HIV-1 protease. The author has an hindex of 22, co-authored 42 publications receiving 2913 citations.
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Journal ArticleDOI
Tyrosine Phosphorylation Inhibits PKM2 to Promote the Warburg Effect and Tumor Growth
Taro Hitosugi,Sumin Kang,Matthew G. Vander Heiden,Tae-Wook Chung,Shannon Elf,Katherine Lythgoe,Shaozhong Dong,Sagar Lonial,Xu Wang,Georgia Z. Chen,Jianxin Xie,Ting-Lei Gu,Roberto D. Polakiewicz,Johannes Roesel,Titus J. Boggon,Fadlo R. Khuri,D. Gary Gilliland,Lewis C. Cantley,Jonathan L. Kaufman,Jing Chen +19 more
TL;DR: The findings suggest that tyrosine phosphorylation regulates PKM2 to provide a metabolic advantage to tumor cells, thereby promoting tumor growth.
Journal ArticleDOI
Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants
Maria Debiec-Rychter,Jan Cools,Herlinde Dumez,Raf Sciot,Michel Stul,Nicole Mentens,Hilde Vranckx,Bartosz Wasag,Bartosz Wasag,Hans Prenen,Johannes Roesel,Anne Hagemeijer,Allan T. van Oosterom,Peter Marynen +13 more
TL;DR: This study shows the high frequency of KIT/PDGFRA kinase domain mutations in patients with secondary resistance and defines genomic amplification of Kit / PDGFRA as an alternative cause of resistance to the drug.
Journal ArticleDOI
Tyrosine Phosphorylation of Mitochondrial Pyruvate Dehydrogenase Kinase 1 Is Important for Cancer Metabolism
Taro Hitosugi,Jun Fan,Tae-Wook Chung,Katherine Lythgoe,Xu Wang,Jianxin Xie,Qingyuan Ge,Ting-Lei Gu,Roberto D. Polakiewicz,Johannes Roesel,Georgia Z. Chen,Titus J. Boggon,Sagar Lonial,Haian Fu,Fadlo R. Khuri,Sumin Kang,Jing Chen +16 more
TL;DR: It is reported that tyrosine phosphorylation enhancesPDHK1 kinase activity by promoting ATP and PDC binding and activates PDHK1 to promote the Warburg effect and tumor growth.
Journal ArticleDOI
Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domain
Florian H. Heidel,Fian K. Solem,Frank Breitenbuecher,Daniel B. Lipka,Stefan Kasper,M. H. Thiede,Christian Brandts,Hubert Serve,Johannes Roesel,Francis J. Giles,Eric J. Feldman,Gerhard Ehninger,Gary J. Schiller,Stephen D. Nimer,Richard Stone,Yanfeng Wang,Thomas Kindler,Pamela S. Cohen,Christoph Huber,Thomas Fischer +19 more
TL;DR: In vivo and in vitro investigation of primary blasts at relapse revealed persistent TK phosphorylation of FLT3 despite sufficient PKC412 serum levels, pointing out that a genetically complex malignancy such as AML may retain dependence on a single oncogenic signal.
Journal ArticleDOI
Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors
Mark J. Levis,Patrick O. Brown,B. Douglas Smith,Adam Stine,Rosalyn Pham,Richard Stone,Daniel J. DeAngelo,Ilene Galinsky,Frank Giles,Elihu H. Estey,Hagop M. Kantarjian,Pamela S. Cohen,Yanfeng Wang,Johannes Roesel,Judith E. Karp,Donald Small +15 more
TL;DR: The application of this assay has revealed that the metabolite CGP52421 may contribute a significant portion of the antileukemia activity observed in patients receiving oral PKC412, and suggest that nonselectivity may constitute an important component of the cytotoxic effect of FLT3 inhibitors inFLT3-mutant AML.