Rational design, optimization, and biological evaluation of novel α-Phosphonopropionic acids as covalent inhibitors of Rab geranylgeranyl transferase

Joanna Małolepsza, Aleksandra Marchwicka, Remigiusz A. Serwa, Sanna P. Niinivehmas, Olli T. Pentikäinen, Edyta Gendaszewska-Darmach & Katarzyna M. Błażewska
Rab geranylgeranyltransferase (GGTase-II, RGGT) catalyses the post-translational modification of eukaryotic Rab GTPases, proteins implicated in several pathologies, including cancer, diabetes, neurodegenerative, and infectious diseases. Thus, RGGT inhibitors are believed to be a potential platform for the development of drugs and tools for studying processes related to the abnormal activity of Rab GTPases. Here, a series of new α-phosphonocarboxylates have been prepared in the first attempt of rational design of covalent inhibitors of RGGT derived from...
1 citation reported since publication in 2022.
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