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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. Among authors: wittinghofer a. 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
Small-Molecule Inhibition of the UNC119-Cargo Interaction.
Mejuch T, Garivet G, Hofer W, Kaiser N, Fansa EK, Ehrt C, Koch O, Baumann M, Ziegler S, Wittinghofer A, Waldmann H. Mejuch T, et al. Among authors: wittinghofer a. Angew Chem Int Ed Engl. 2017 May 22;56(22):6181-6186. doi: 10.1002/anie.201701905. Epub 2017 May 4. Angew Chem Int Ed Engl. 2017. PMID: 28471079
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. Among authors: wittinghofer a. 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. Among authors: wittinghofer a. Nat Commun. 2016 Apr 20;7:11360. doi: 10.1038/ncomms11360. Nat Commun. 2016. PMID: 27094677 Free PMC article.
Novel Biochemical and Structural Insights into the Interaction of Myristoylated Cargo with Unc119 Protein and Their Release by Arl2/3.
Jaiswal M, Fansa EK, Kösling SK, Mejuch T, Waldmann H, Wittinghofer A. Jaiswal M, et al. Among authors: wittinghofer a. J Biol Chem. 2016 Sep 23;291(39):20766-78. doi: 10.1074/jbc.M116.741827. Epub 2016 Aug 1. J Biol Chem. 2016. PMID: 27481943 Free PMC article.
Recently, we have shown that prenylated proteins are sorted according to their affinity to the carrier protein PDE6delta and the ability of Arl3 but not Arl2 to release high affinity cargo inside the cilia (Fansa, E. K., Kosling, S. K., Zent, E., Wittinghofer, A., a …
Recently, we have shown that prenylated proteins are sorted according to their affinity to the carrier protein PDE6delta and the ability of …
316 results