- 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.
Angewandte Chemie (International ed. in English) (2017-01-21)
Pablo Martín-Gago, Eyad K Fansa, Christian H Klein, Sandip Murarka, Petra Janning, Marc Schürmann, Malte Metz, Shehab Ismail, Carsten Schultz-Fademrecht, Matthias Baumann, Philippe I H Bastiaens, Alfred Wittinghofer, Herbert Waldmann
PMID28106325
要旨
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 (K
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