Abstract
A folate receptor targeted camptothecin prodrug was synthesized using a hydrophilic peptide spacer linked to folate via a releasable disulfide carbonate linker. The conjugate was found to possess high affinity for folate receptor-expressing cells and inhibited cell proliferation in human KB cells with an IC50 of 10 nM. Activity of the prodrug was completely blocked by excess folic acid, demonstrating receptor-mediated uptake.
Original language | English (US) |
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Pages (from-to) | 5350-5355 |
Number of pages | 6 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 16 |
Issue number | 20 |
DOIs | |
State | Published - Oct 15 2006 |
Keywords
- Camptothecin
- Carbonate
- Disulfide
- Endocytosis
- Folate
- Folic acid
- Peptide
- Prodrug
- Releasable linker
- Targeted drug delivery
ASJC Scopus subject areas
- Biochemistry
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science