ENZYME INHIBITORS SY · Combinatorial synthesis of enzyme inhibitors as new generation anticancer agents

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Накратко на български

Цел на проекта

In recent years, the search for new lead molecules in pharmaceutical research has been radically altered by the introduction of combinatorial technologies. Our goal is to apply these techniques to the discovery of novel anticancer agents designed to act on a specific enzyme in the cell. This enzyme, termed Protein Farnesyl Transferase (PFTase), is implicated in the post-translational modification of proteins such as Ras, found mutated in approximately 30% of all human cancers. Compared to classical cytotoxic agents, PFTase inhibitors represent one of the few classes of anticancer agents that could constitute a real improvement in the cancer therapy. Indeed, these drugs are able to selectively target cancer cells while normal cells remain unaffected. Ras proteins required prenylation for activity and this transfer of a farnesyl group from farnesyl pyrophosphate (FPP) to a cysteine residue of Ras protein is catalyzed by PFTase. Two approaches are possible to inhibit this farnesylation. The first is to design compounds that mimic the terminal residue of the Ras protein (CAAX box) and the second is to design compounds that will compete with FPP. The efforts of our chemistry team have been mainly focused on the discovery of original PFTase inhibitors that mimic the CAAX box. The project of the Fellow will be to design compounds that will compete with FPP. This new approach will create a stimulating environment in that it will require numerous exchanges with other researchers.

Оригинален текст от CORDIS (на английски).

Участници

• INSTITUT DE RECHERCHE PIERRE FABRE, S.A.S. · CASTRESКоординаторФранция

Връзки

• Виж в CORDIS