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用于抗体药物偶联物的过氧化物裂解连接物。

Peroxide-cleavable linkers for antibody-drug conjugates.

机构信息

Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK.

Cancer Research UK Cambridge Institute, Robinson Way, Cambridge, CB2 ORE, UK.

出版信息

Chem Commun (Camb). 2023 Feb 9;59(13):1841-1844. doi: 10.1039/d2cc06677g.

DOI:10.1039/d2cc06677g
PMID:36722863
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9910056/
Abstract

Antibody-drug conjugates containing peroxide-cleavable arylboronic acid linkers are described, which target the high levels of reactive oxygen species (ROS) in cancer. The arylboronic acid linkers rapidly release a payload in the presence of hydrogen peroxide, but remain stable in plasma. Anti-HER2 and PD-L1 peroxide-cleavable ADCs exhibited potent cytotoxicity .

摘要

本文介绍了含有过氧键可裂解芳基硼酸连接物的抗体药物偶联物，该连接物靶向癌细胞中高水平的活性氧（ROS）。在过氧化氢存在下，芳基硼酸连接物迅速释放有效载荷，但在血浆中保持稳定。抗 HER2 和 PD-L1 过氧键可裂解 ADC 表现出强大的细胞毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e37a/9910056/982cd683e595/d2cc06677g-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e37a/9910056/577bbc81c779/d2cc06677g-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e37a/9910056/b89684a50e15/d2cc06677g-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e37a/9910056/c3fefe99cdab/d2cc06677g-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e37a/9910056/1a4ff2c2eebc/d2cc06677g-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e37a/9910056/982cd683e595/d2cc06677g-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e37a/9910056/577bbc81c779/d2cc06677g-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e37a/9910056/b89684a50e15/d2cc06677g-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e37a/9910056/c3fefe99cdab/d2cc06677g-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e37a/9910056/1a4ff2c2eebc/d2cc06677g-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e37a/9910056/982cd683e595/d2cc06677g-f5.jpg

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