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

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Reduction–rebridging strategy for the preparation of ADPN-based antibody–drug conjugates†‡
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-04-20 00:00:00 , DOI: 10.1039/c8md00141c
Oleksandr Koniev _{1,

2,

3} , Igor Dovgan _{3,

4,

5,

6,

7} , Brigitte Renoux _{3,

8,

9,

10,

11} , Anthony Ehkirch _{3,

12,

13,

14,

15} , Jitka Eberova _{3,

4,

5,

6,

7} , Sarah Cianférani _{3,

12,

13,

14,

15} , Sergii Kolodych _{1,

2,

3} , Sébastien Papot _{3,

8,

9,

10,

11} , Alain Wagner _{3,

4,

5,

6,

7}

Affiliation

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.

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