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Retro‐1 Analogues Differentially Affect Oligonucleotide Delivery and Toxin Trafficking |
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| Authors: | Bing Yang Dr Xin Ming Hajer Abdelkafi Valerie Pons Aurelien Michau Dr Daniel Gillet Dr Jean‐Christophe Cintrat Dr Julien Barbier Dr Rudy Juliano |
| Affiliation: | 1. Division of Molecular Pharmaceutics, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, USA;2. Service de Chimie Bio-organique et Marquage (SCBM), IBITECS, CEA, LabEx LERMIT, Université Paris-Saclay, Gif-sur-Yvette, France;3. Service d'Ingénierie Moléculaire des Protéines (SIMOPRO), IBITECS, CEA, LabEx LERMIT, Université Paris-Saclay, Gif-sur-Yvette, France |
| Abstract: | Retro‐1 is a small molecule that displays two important biological activities: First, it blocks the actions of certain toxins by altering their intracellular trafficking. Second, it enhances the activity of oligonucleotides by releasing them from entrapment in endosomes. This raises the question of whether the two actions involve the same cellular target. Herein we report the effects of several Retro‐1 analogues on both toxins and oligonucleotides. We found analogues that affect toxins but not oligonucleotides and vice‐versa, while Retro‐1 is the only compound that affects both. This indicates that the molecular target(s) involved in the two processes are distinct. |
| Keywords: | endocytosis oligonucleotides Retro-1 toxins trafficking |