Deltarasin binds PDE6D

Stable Identifier
R-HSA-9656781
Type
Reaction [binding]
Species
Homo sapiens
Compartment
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Deltarasin is a small molecule inhibitor of PDE6D that binds in the farnesyl-binding pocket of the enzyme and prevents interaction with KRAS4B and other farnesylated proteins (Zimmerman et al, 2013). PDE6D inhibition results in RAS protein mislocalization and reduces cellular proliferation and increase cell death in KRAS-dependent pancreatic cell lines (Zimmerman et al, 2013; reviewed in Shimansu et al, 2017). Other farnesyl-pocket binding small molecule inhibitors are also under development (Papke et al, 2016).

Literature References
PubMed ID Title Journal Year
27094677 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

Nat Commun 2016
23698361 Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling

Zimmermann, G, Papke, B, Ismail, S, Vartak, N, Chandra, A, Hoffmann, M, Hahn, SA, Triola, G, Wittinghofer, A, Bastiaens, PI, Waldmann, H

Nature 2013
28666118 RAS Proteins and Their Regulators in Human Disease

Simanshu, DK, Nissley, DV, McCormick, F

Cell 2017
Participants
Participant Of
hasEvent
Disease
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
Authored
Reviewed
Created
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