Article
An Improved PDE6D Inhibitor Combines with Sildenafil To Inhibit KRAS Mutant Cancer Cell Growth.
Journal of medicinal chemistry - 13 Jun 2024
Kaya Pelin, Schaffner-Reckinger Elisabeth, Manoharan Ganesh Babu, Vukic Vladimir, Kiriazis Alexandros, Ledda Mirko, Burgos Renedo Maria, Pavic Karolina, Gaigneaux Anthoula, Glaab Enrico, Abankwa Daniel Kwaku
Abstract excerpt
The trafficking chaperone PDE6D (or PDEδ) was proposed as a surrogate target for K-Ras, leading to the development of a series of inhibitors that block its prenyl binding pocket. These inhibitors suffered from low solubility and suspected off-target effects, preventing their clinical development. Here, we developed a highly soluble, low nanomolar PDE6D inhibitor (PDE6Di), Deltaflexin3, which has the lowest...
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