Structure-Activity Relationship Studies of Retro-1 Analogues Against Shiga Toxin

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

doi:10.26434/chemrxiv.11860707.v1

Biological and Medicinal Chemistry

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Structure-Activity Relationship Studies of Retro-1 Analogues Against Shiga Toxin

20 February 2020, Version 1

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Abstract

The Retro-1 molecule was identified in a high-throughput screening as an inhibitor of ricin and Shiga toxins by diminishing their intracellular trafficking via the retrograde route, from early endosomes to the Golgi apparatus. In order to improve the activity of Retro-1, a SAR study was undertaken yielding an analog that possesses roughly 70-fold better EC₅₀ against Shiga toxin cytotoxicity measured in a cell protein synthesis assay.

Keywords

Retro-1

Shiga Toxin

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

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

Journal of Medicinal Chemistry , Volume 63, Issue 15

Online publication date: Jul 10, 2020

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Feb 20, 2020 Version 1

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The content is available under CC BY NC ND 4.0

DOI

10.26434/chemrxiv.11860707.v1

Funding

Agence Nationale de la Recherche

ANR-11-BSV2-0018

Chemical genetics of the retrograde transport route – RETROscreen

https://app.dimensions.ai/details/grant/grant.4524072

Author’s competing interest statement

no conflict of interest

Structure-Activity Relationship Studies of Retro-1 Analogues Against Shiga Toxin

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Abstract

Keywords

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Author’s competing interest statement

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