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A PDE6δ-KRas Inhibitor Chemotype with up to Seven H-Bonds and Picomolar Affinity that Prevents Efficient Inhibitor Release by Arl2.
Martín-Gago P, Fansa EK, Klein CH, Murarka S, Janning P, Schürmann M, Metz M, Ismail S, Schultz-Fademrecht C, Baumann M, Bastiaens PI, Wittinghofer A, Waldmann H. Martín-Gago P, et al. Angew Chem Int Ed Engl. 2017 Feb 20;56(9):2423-2428. doi: 10.1002/anie.201610957. Epub 2017 Jan 20. Angew Chem Int Ed Engl. 2017. PMID: 28106325
The N- and C-terminal ends of RPGR can bind to PDE6δ.
Fansa EK, O'Reilly NJ, Ismail S, Wittinghofer A. Fansa EK, et al. EMBO Rep. 2015 Dec;16(12):1583-5. doi: 10.15252/embr.201541404. Epub 2015 Nov 9. EMBO Rep. 2015. PMID: 26553937 Free PMC article.
Identification of pyrazolopyridazinones as PDEδ inhibitors.
Papke B, Murarka S, Vogel HA, Martín-Gago P, Kovacevic M, Truxius DC, Fansa EK, Ismail S, Zimmermann G, Heinelt K, Schultz-Fademrecht C, Al Saabi A, Baumann M, Nussbaumer P, Wittinghofer A, Waldmann H, Bastiaens PI. Papke B, et al. Nat Commun. 2016 Apr 20;7:11360. doi: 10.1038/ncomms11360. Nat Commun. 2016. PMID: 27094677 Free PMC article.
180 results