Issue 5, 2018
From the journal:

MedChemComm

Reduction–rebridging strategy for the preparation of ADPN-based antibody–drug conjugates†‡

Oleksandr Koniev,a   Igor Dovgan,b   Brigitte Renoux,c   Anthony Ehkirch,de   Jitka Eberova,b   Sarah Cianférani,de   Sergii Kolodych, ORCID logo *a   Sébastien Papot ORCID logo *c  and  Alain Wagner ORCID logo b  

* Corresponding authors

a Syndivia SAS, 650 Bd Gonthier d'Andernach, 67400 Illkirch, France
E-mail: sk@syndivia.com

b Laboratory of Functional ChemoSystems (UMR 7199), Labex Medalis, University of Strasbourg, 74 route du Rhin, 67401 Illkirch-Graffenstaden, France

c Institut de Chimie des Milieux et des Matériaux de Poitiers, IC2MP, Université de Poitiers, UMR-CNRS 7285, 4 Rue Michel Brunet, 86022 Poitiers, France

d BioOrganic Mass Spectrometry Laboratory (LSMBO), IPHC, Université de Strasbourg, 25 rue Becquerel, 67087 Strasbourg, France

e IPHC, CNRS, UMR7178, 67087 Strasbourg, France

Abstract

The reduction–rebridging strategy is a powerful method for the preparation of stable and homogeneous antibody–drug conjugates (ADCs). In this communication, we describe the development of the arylene-dipropiolonitrile (ADPN) functional group for the rebridging of reduced disulphide bonds and its application in the preparation of potent and selective ADCs.

Graphical abstract: Reduction–rebridging strategy for the preparation of ADPN-based antibody–drug conjugates

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Article information

DOI
https://doi.org/10.1039/C8MD00141C
Article type
Research Article
Submitted
14 Mar 2018
Accepted
07 Apr 2018
First published
20 Apr 2018

Med. Chem. Commun., 2018,9, 827-830

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Reduction–rebridging strategy for the preparation of ADPN-based antibody–drug conjugates

O. Koniev, I. Dovgan, B. Renoux, A. Ehkirch, J. Eberova, S. Cianférani, S. Kolodych, S. Papot and A. Wagner, Med. Chem. Commun., 2018, 9, 827 DOI: 10.1039/C8MD00141C

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