A PDE6δ‐KRas Inhibitor Chemotype with up to Seven H‐Bonds and Picomolar Affinity that Prevents Efficient Inhibitor Release by Arl2

A PDE6δ‐KRas Inhibitor Chemotype with up to Seven H‐Bonds and Picomolar Affinity that Prevents Efficient Inhibitor Release by Arl2

Small‐molecule inhibition of the interaction between the KRas oncoprotein and the chaperone PDE6δ impairs KRas spatial organization and signaling in cells. However, despite potent binding in vitro (KD

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Bibliographische Detailangaben
Veröffentlicht in:Angewandte Chemie 2017-02, Vol.129 (9), p.2463-2468
Hauptverfasser: Martín‐Gago, Pablo, Fansa, Eyad K., Klein, Christian H., Murarka, Sandip, Janning, Petra, Schürmann, Marc, Metz  , Malte, Ismail, Shehab, Schultz‐Fademrecht, Carsten, Baumann, Matthias, Bastiaens, Philippe I. H., Wittinghofer, Alfred, Waldmann, Herbert
Format: Artikel
Sprache:eng
Schlagworte:
Affinity
Binding
Hydrogen bonds
Inhibition
Inhibitors
Interference
Medizinische Chemie
Organizations
PDEδ
Ras-Protein
Struktur-Aktivitäts-Beziehungen
Tumors
Wirkstoffentwicklung
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Beschreibung
Zusammenfassung:Small‐molecule inhibition of the interaction between the KRas oncoprotein and the chaperone PDE6δ impairs KRas spatial organization and signaling in cells. However, despite potent binding in vitro (KD
ISSN:0044-8249
1521-3757
DOI:10.1002/ange.201610957