Structure-based development of PDEδ inhibitors

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Abstract: The prenyl binding protein PDEδ enhances the diffusion of farnesylated Ras proteins in the cytosol, ultimately affecting their correct localization and signaling. This has turned PDEδ into a promising target to prevent oncogenic KRas signaling. In this review we summarize and describe the structure-guided-development of the three different PDEδ inhibitor chemotypes that have been documented so far. We also compare both their potency for binding to the PDEδ pocket and their in vivo efficiency in suppressing oncogenic KRas signaling, as a result of the inhibition of the PDEδ/KRas interaction.

Location: Deutsche Nationalbibliothek Frankfurt am Main

Extent: Online-Ressource

Language: Englisch

Bibliographic citation: Structure-based development of PDEδ inhibitors ; volume:398 ; number:5-6 ; year:2017 ; pages:535-545 ; extent:11
Biological chemistry ; 398, Heft 5-6 (2017), 535-545 (gesamt 11)

Creator: Martín-Gago, Pablo
Fansa, Eyad Kalawy
Wittinghofer, Alfred
Waldmann, Herbert

DOI: 10.1515/hsz-2016-0272

URN: urn:nbn:de:101:1-2408051816433.818360231998

Rights: Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.

Last update: 14.08.2025, 11:02 AM CEST

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Martín-Gago, Pablo
Fansa, Eyad Kalawy
Wittinghofer, Alfred
Waldmann, Herbert

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Structure-based development of PDEδ inhibitors

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