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Disulfide-based multifunctional conjugates for targeted theranostic drug delivery
Min Hee Lee1, Jonathan L Sessler2, Jong Seung Kim3
1Department of Chemistry, Sookmyung Women's University , Seoul 140-742, Korea.
Accounts of Chemical Research
|October 30, 2015
Summary
Disulfide-based theranostic conjugates offer targeted cancer therapy and imaging. These systems release drugs and signal changes in fluorescence upon cleavage by tumor-specific thiols.
Area of Science:
- Bioconjugate Chemistry
- Molecular Imaging
- Cancer Therapeutics
Background:
- Theranostics integrate therapeutic and diagnostic functions for personalized medicine.
- Cancer-targeted drug delivery requires selective agents and monitoring capabilities.
- Disulfide bonds are promising linkers due to their cleavage by elevated tumor thiols (GSH, Trx).
Purpose of the Study:
- To summarize recent studies on disulfide-based fluorescent drug delivery conjugates.
- To evaluate the biological utility of these theranostic systems in vitro and in vivo.
- To explore cancer-targeting ligands for enhanced selectivity.
Main Methods:
- Synthesis of multicomponent theranostic conjugates (drug-disulfide-fluorophore-ligand).
- Utilizing various chemotherapeutics (doxorubicin, gemcitabine, camptothecin) and fluorophores (naphthalimide, coumarin, BODIPY, rhodol, Cy7).
- Incorporating cancer-targeting ligands (galactose, folate, biotin, RGD peptide).
Main Results:
- Disulfide conjugates demonstrated efficient drug release and fluorescence changes upon thiol cleavage.
- Targeting ligands improved selectivity for cancer cells.
- Preliminary in vitro and in vivo studies showed promising biological activity.
Conclusions:
- Disulfide-based theranostics enable targeted drug delivery and real-time monitoring.
- These systems can advance cancer drug discovery and understanding of drug release.
- Further development holds potential for improved cancer patient treatment.
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