Pyrrolobenzodiazepine Antibody-Drug Conjugates Designed for Stable Thiol Conjugation

Pyrrolobenzodiazepine Antibody-Drug Conjugates Designed for Stable Thiol Conjugation

Thiosuccinimide-linked antibody-drug conjugates (ADCs) are susceptible to drug loss over time due to a retro-Michael reaction, which can be prevented by selecting stable conjugation positions or hydrolysis of the thiosuccinimide. Here, we investigate pyrrolobenzodiazepine (PBD) ADC drug-linkers equi...

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Bibliographic Details
Main Authors: R. James Christie, Arnaud C. Tiberghien, Qun Du, Binyam Bezabeh, Ryan Fleming, Amanda Shannon, Shenlan Mao, Shannon Breen, Jing Zhang, Haihong Zhong, Jay Harper, Herren Wu, Philip W. Howard, Changshou Gao
Format: Article
Language:English
Published: MDPI AG 2017-11-01
Series:Antibodies
Subjects:
PBD dimer
thiosuccinimide hydrolysis
N-phenyl maleimide
retro-Michael reaction
serum stability
ADC
site-specific conjugation
Online Access:https://www.mdpi.com/2073-4468/6/4/20

Internet

https://www.mdpi.com/2073-4468/6/4/20

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