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Identification of a Covalent Importin-5 Inhibitor, Goyazensolide, from a Collective Synthesis of Furanoheliangolides

Cover illustration created for Prof. Nicolas Winssinger from the Department of Organic Chemistry at the University of Geneva (2021)

The synthesized small molecule Goyazensolide selectively and covalently binds the oncoprotein importin-5 (IPO5), inhibiting the translocation of its cargo RASAL-2. This is traditionally difficult with small molecules because they interact with such a small portion of the binding site relative to the protein-protein interaction. This illustration was thus inspired by the image of David vs Goliath.
Liu W, Patouret R, Barluenga S, Plank M, Loewith R, Winssinger N. Identification of a Covalent Importin-5 Inhibitor, Goyazensolide, from a Collective Synthesis of Furanoheliangolides. ACS Cent Sci. 2021 Jun 23;7(6):954-962. doi: 10.1021/acscentsci.1c00056.

Audience: Expert scientists


Media: UCSF Chimera, Autodesk Maya, Adobe Photoshop