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Design, synthesis and evaluation of anti-CD123 antibody drug conjugates.

Abstract：

:Leukemia stem cells (LSCs) account for the development of drug resistance and increased recurrence rate in acute myeloid leukemia (AML) patients. Targeted drug delivery to leukemia stem cells remains a major challenge in AML chemotherapy. Overexpressed interleukin-3 receptor alpha chain, CD123, on the surface of leukemia stem cells was reported to be a potential target in AML treatment. Here, we designed and developed an antibody drug conjugate (CD123-CPT) by integrating anti-CD123 antibody with a chemotherapeutic agent, Camptothecin (CPT), via a disulfide linker. The linker is biodegradable in the presence of Glutathione (GSH, an endogenous component in cells), which leads to release of CPT. Anti-CD123 antibody conjugates showed significant higher cellular uptake in CD123-overexpressed tumor cells. More importantly, CD123-CPT demonstrated potent inhibitory effects on CD123-overexpressed tumor cells. Consequently, these results provide a promising targeted chemotherapeutical strategy for AML treatment.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Li B,Zhao W,Zhang X,Wang J,Luo X,Baker SD,Jordan CT,Dong Y

doi

10.1016/j.bmc.2016.09.043

subject

Has Abstract

pub_date

2016-11-15 00:00:00

pages

5855-5860

issue

22

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30744-1

journal_volume

24

pub_type

杂志文章

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