Title of article :
Synthesis and activity of a folate peptide camptothecin prodrug
Author/Authors :
Walter A. Henne، نويسنده , , Derek D. Doorneweerd، نويسنده , , Andrew R. Hilgenbrink، نويسنده , , Sumith A. Kularatne، نويسنده , , Philip S. Low، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2006
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.
Keywords :
camptothecin , Targeted drug delivery , Endocytosis , peptide , prodrug , Carbonate , Disulfide , Folate , folic acid , Releasable linker
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
