Design, Synthesis, and Evaluation of Camptothecin-Based Antibody–Drug Conjugates with High Hydrophilicity and Structural Stability

In this study, we constructed a linear antibody–drug conjugate (ADC), 7300-LP1003, by coupling the camptothecin derivative 095 to a linker through an ether bond. In vitro enzyme experiments indicated that LP1003 releases 095 through the action of tissue cathepsin B. Therefore, we introduced lysine p...

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Bibliographic Details
Published in:	Molecules (Basel, Switzerland) Vol. 30; no. 7; p. 1398
Main Authors:	Xiong, Tingyu, Jin, Jiyu, Liu, Dongliang, Jin, Chen
Format:	Journal Article
Language:	English
Published:	Switzerland MDPI AG 21.03.2025
Subjects:	Analog to digital converters Animals Antibodies antibody–drug conjugates Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biopharmaceutics Breast cancer Camptothecin Camptothecin - analogs & derivatives Camptothecin - chemistry Camptothecin - pharmacology Cathepsins Cell Line, Tumor Chromatography Cytotoxicity Drug Design Drug Stability Enzymes Ethylenediaminetetraacetic acid Humans Hydrophobic and Hydrophilic Interactions Immunoconjugates - chemistry Immunoconjugates - pharmacology Mice Phosphates Polyethylene glycol Polyols polysarcosine topoisomerase I inhibitor Viral antibodies Xenograft Model Antitumor Assays Japan China polyethylene glycol polysarcosine topoisomerase I inhibitor antibody–drug conjugates
ISSN:	1420-3049, 1420-3049
Online Access:	Get full text
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