Details

Autor(en) / Beteiligte

• Abdelkafi, Hajer
• Michau, Aurélien
• Pons, Valérie
• Ngadjeua, Flora
• Clerget, Alexandra
• Ait Ouarab, Lilia
• Buisson, David-Alexandre
• Montoir, David
• Caramelle, Lucie
• Gillet, Daniel
• Barbier, Julien
• Cintrat, Jean-Christophe

Titel

Structure–Activity Relationship Studies of Retro‑1 Analogues against Shiga Toxin

Ist Teil von

• Journal of medicinal chemistry, 2020-08, Vol.63 (15), p.8114-8133

Ort / Verlag

American Chemical Society

Erscheinungsjahr

2020

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• High-throughput screening has shown that Retro-1 inhibits ricin and Shiga toxins by diminishing their intracellular trafficking via the retrograde route, from early endosomes to the Golgi apparatus. To improve the activity of Retro-1, a structure–activity relationship (SAR) study was undertaken and yielded an analogue with a roughly 70-fold better half-maximal effective concentration (EC50) against Shiga toxin cytotoxicity measured in a cell protein synthesis assay.