ArticleDrug delivery2021
Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates.
Article in Drug delivery, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 15 citations in OpenAlex.
- Synthesis and Characterization of Transferrin Receptor-Targeted Peptide Combination SN-38 and Rucaparib Conjugate for the Treatment of Glioblastoma.Pharmaceutics · 2025Article
- Design, Synthesis, and Evaluation of Camptothecin-Based Antibody-Drug Conjugates with High Hydrophilicity and Structural Stability.Molecules (Basel, Switzerland) · 2025Article
- The multifaceted anticancer potential of luteolin: involvement of NF-κB, AMPK/mTOR, PI3K/Akt, MAPK, and Wnt/β-catenin pathways.Inflammopharmacology · 2025Review
- Quantum Dots Functionalized Polymeric Nanoparticles as Cancer Theranostics: An Advanced Nanomedicine Strategy.Current cancer drug targets · 2025Review
- Article
- Research Progress of SN38 Drug Delivery System in Cancer Treatment.International journal of nanomedicine · 2024Review
- Synthesis and Antitumor Evaluation of Biotin-SN38-Valproic Acid Conjugates.Molecules (Basel, Switzerland) · 2023Article
- Synthesis and biological evaluation of novel quaternary ammonium antibody drug conjugates based on camptothecin derivatives.PloS one · 2023Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Camptothecins, traditional chemotherapy drugs, have been clinically used in antibody-drug conjugates (ADCs), which refreshes the recognition that ADCs preferably incorporate highly potent payloads. However, SN-38, active metabolite of irinotecan from camptothecins, tended to be incorporated into ADCs with an unstable acid sensitive bond, not with the widely used Cathepsin B (CTSB) sensitive bond, which may pose the risk of off-target. Herein, we reported a novel strategy to construct highly releasable and structurally stable SN-38-conjugates, in which CTSB linkers directly connected to the 10-OH group through ether bond, not to the common 20-OH group of lactones of SN-38. In this paper, rapid release of SN-38 was skillfully demonstrated by utilizing the fluorescence properties of SN-38. The SN-38-ether-ADC displayed highly stable serum stability with the half-life over 10 days. Moreover, the drug-antibody-ratio (DAR) of ADC could be elevated to 7.1 through the introduction of polyethylene glycol (PEG) moieties without aggregation. The optimized ADC exhibited potent
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.