H
Hans-Peter Buchstaller
Researcher at Merck & Co.
Publications - 8
Citations - 69
Hans-Peter Buchstaller is an academic researcher from Merck & Co.. The author has contributed to research in topics: Wnt signaling pathway & Colorectal cancer. The author has an hindex of 4, co-authored 8 publications receiving 42 citations.
Papers
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Journal ArticleDOI
Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity.
Hans-Peter Buchstaller,Uwe Anlauf,Dieter Dorsch,Daniel Kuhn,Martin Lehmann,Birgitta Leuthner,Djordje Musil,Daniela Radtki,Claudio Ritzert,Felix Rohdich,Richard Schneider,Christina Esdar +11 more
TL;DR: The X-ray structure of 5k in complex with TNKS1 was solved and confirmed the design hypothesis and Modulation of Wnt pathway activity was demonstrated with this compound in a colorectal xenograft model in vivo.
Journal ArticleDOI
3D imaging of colorectal cancer organoids identifies responses to Tankyrase inhibitors.
Luned Badder,Andrew John Hollins,Bram Herpers,Kuan Yan,Kenneth Burnside Ramsay Ewan,Mairian Thomas,Jennifer R. Shone,Delyth A. Badder,Marc Naven,Kevin E. Ashelford,Rachel Hargest,Rachel Hargest,Alan Richard Clarke,Christina Esdar,Hans-Peter Buchstaller,J. Mark Treherne,Sylvia F. Boj,Bahar Ramezanpour,Dirk Wienke,Leo S. Price,Paul Shaw,Trevor Clive Dale +21 more
TL;DR: It is demonstrated that morphometric analyses can capture subtle alterations in organoid responses to Wnt inhibitors that are consistent with activity against a cancer stem cell subpopulation, highlighting the value of phenotypic readouts as a quantitative method to asses drug-induced effects in a relevant preclinical model.
Patent
Heterocyclic substituted bisarylurea derivatives as kinase inhibitors
Frank Stieber,Alfred Jonczyk,Guenter Hoelzemann,Hans-Peter Buchstaller,Lars Thore Burgdorf,Wilfried Rautenberg,Hartmut Greiner +6 more
TL;DR: In this article, the use of the compounds of formula I as inhibitors of one or more kinases, and the use for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
Posted ContentDOI
3D imaging of colorectal cancer organoids identifies responses to Tankyrase inhibitors
Luned Badder,Andrew John Hollins,Bram Herpers,Kuan Yan,Kenneth Burnside Ramsay Ewan,Jennifer R. Shone,Delyth A. Badder,Marc Naven,Kevin E. Ashelford,Rachel Hargest,Rachel Hargest,Alan Richard Clarke,Christina Esdar,Hans-Peter Buchstaller,Dirk Wienke,Leo S. Price,Paul Shaw,Trevor Clive Dale +17 more
TL;DR: It is demonstrated that morphometric analyses can capture subtle alterations in organoid responses to Wnt inhibitors that are consistent with activity against a cancer stem cell subpopulation, highlighting the value of phenotypic readouts as a quantitative method to asses drug-induced effects in a relevant preclinical model.
Patent
N1-(3,3,3-trifluoro-2-hydroxy-2-methylpropionyl)-piperidine derivatives as inhibitors of pyruvate dehydrogenase kinase
TL;DR: In this paper, the meaning of compounds of the formula (I) in which X, Q, R 1 and R 2 have the meanings indicated in Claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK).