Identification of pyrazolopyridazinones as PDEδ inhibitors

The prenyl-binding protein PDEδ is crucial for the plasma membrane localization of prenylated Ras. Recently, we have reported that the small-molecule Deltarasin binds to the prenyl-binding pocket of PDEδ, and impairs Ras enrichment at the plasma membrane, thereby affecting the proliferation of KRas-...

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Bibliographic Details
Published in:Nature communications 2016-04, Vol.7 (1), p.11360-9, Article 11360
Main Authors: Papke, Björn, Murarka, Sandip, Vogel, Holger A, Martín-Gago, Pablo, Kovacevic, Marija, Truxius, Dina C, Fansa, Eyad K, Ismail, Shehab, Zimmermann, Gunther, Heinelt, Kaatje, Schultz-Fademrecht, Carsten, Al Saabi, Alaa, Baumann, Matthias, Nussbaumer, Peter, Wittinghofer, Alfred, Waldmann, Herbert, Bastiaens, Philippe I.H.
Format: Article
Language:English
Subjects:
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631/67/1504/1713
631/80/86
631/92/436/108
82/1
82/29
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Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Binding Sites
Cell Line, Tumor
Crystallography, X-Ray
Cyclic Nucleotide Phosphodiesterases, Type 6 - antagonists & inhibitors
Cyclic Nucleotide Phosphodiesterases, Type 6 - chemistry
Cyclic Nucleotide Phosphodiesterases, Type 6 - genetics
Cyclic Nucleotide Phosphodiesterases, Type 6 - metabolism
Epithelial Cells - drug effects
Epithelial Cells - metabolism
Epithelial Cells - pathology
Gene Expression
Gene Expression Regulation, Neoplastic
Humanities and Social Sciences
Humans
Molecular Docking Simulation
multidisciplinary
Pancreatic Ducts - drug effects
Pancreatic Ducts - metabolism
Pancreatic Ducts - pathology
Phosphodiesterase Inhibitors - chemical synthesis
Phosphodiesterase Inhibitors - chemistry
Phosphodiesterase Inhibitors - pharmacology
Protein Binding
Protein Interaction Domains and Motifs
Protein Structure, Secondary
Proto-Oncogene Proteins p21(ras) - antagonists & inhibitors
Proto-Oncogene Proteins p21(ras) - chemistry
Proto-Oncogene Proteins p21(ras) - genetics
Proto-Oncogene Proteins p21(ras) - metabolism
Pyrazines - chemical synthesis
Pyrazines - chemistry
Pyrazines - pharmacology
Pyrazoles - chemical synthesis
Pyrazoles - chemistry
Pyrazoles - pharmacology
Recombinant Proteins - chemistry
Recombinant Proteins - genetics
Recombinant Proteins - metabolism
Science
Signal Transduction
Small Molecule Libraries - chemical synthesis
Small Molecule Libraries - chemistry
Small Molecule Libraries - pharmacology
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