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

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

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 f...

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Bibliographic Details
Main Authors: Joanna Małolepsza, Aleksandra Marchwicka, Remigiusz A. Serwa, Sanna P. Niinivehmas, Olli T. Pentikäinen, Edyta Gendaszewska-Darmach, Katarzyna M. Błażewska
Format: Article
Language:English
Published: Taylor & Francis Group 2022-12-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
Phosphonocarboxylate
Rab geranylgeranyltransferase
prenylation
imidazo[1
2-a]pyridine
covalent inhibitors
Online Access:https://www.tandfonline.com/doi/10.1080/14756366.2022.2053525
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https://www.tandfonline.com/doi/10.1080/14756366.2022.2053525

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