Nature Communications (Apr 2016)
Identification of pyrazolopyridazinones as PDEδ inhibitors
- Björn Papke,
- Sandip Murarka,
- Holger A Vogel,
- Pablo Martín-Gago,
- Marija Kovacevic,
- Dina C Truxius,
- Eyad K Fansa,
- Shehab Ismail,
- Gunther Zimmermann,
- Kaatje Heinelt,
- Carsten Schultz-Fademrecht,
- Alaa Al Saabi,
- Matthias Baumann,
- Peter Nussbaumer,
- Alfred Wittinghofer,
- Herbert Waldmann,
- Philippe I.H. Bastiaens
Affiliations
- Björn Papke
- Department of Systemic Cell Biology, Max Planck Institute of Molecular Physiology
- Sandip Murarka
- Department of Chemical Biology, Max Planck Institute of Molecular Physiology
- Holger A Vogel
- Department of Systemic Cell Biology, Max Planck Institute of Molecular Physiology
- Pablo Martín-Gago
- Department of Chemical Biology, Max Planck Institute of Molecular Physiology
- Marija Kovacevic
- Department of Systemic Cell Biology, Max Planck Institute of Molecular Physiology
- Dina C Truxius
- Department of Systemic Cell Biology, Max Planck Institute of Molecular Physiology
- Eyad K Fansa
- Structural Biology Group, Max Planck Institute for Molecular Physiology
- Shehab Ismail
- Structural Biology Group, Max Planck Institute for Molecular Physiology
- Gunther Zimmermann
- Department of Chemical Biology, Max Planck Institute of Molecular Physiology
- Kaatje Heinelt
- Department of Systemic Cell Biology, Max Planck Institute of Molecular Physiology
- Carsten Schultz-Fademrecht
- Lead Discovery Center GmbH
- Alaa Al Saabi
- Lead Discovery Center GmbH
- Matthias Baumann
- Lead Discovery Center GmbH
- Peter Nussbaumer
- Lead Discovery Center GmbH
- Alfred Wittinghofer
- Structural Biology Group, Max Planck Institute for Molecular Physiology
- Herbert Waldmann
- Department of Chemical Biology, Max Planck Institute of Molecular Physiology
- Philippe I.H. Bastiaens
- Department of Systemic Cell Biology, Max Planck Institute of Molecular Physiology
- DOI
- https://doi.org/10.1038/ncomms11360
- Journal volume & issue
-
Vol. 7,
no. 1
pp. 1 – 9
Abstract
PDEδ is a widely expressed factor that sustains the spatial organization and signalling of Ras family proteins. Here the authors describe the activity of Deltazinone 1, a new highly selective PDEδ inhibitor of KRAS-dependent cancer cell growth with low cytotoxic side effects.
