Related Experiment Video
Updated: May 27, 2026

Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells
Published on: January 18, 2017
Synthesis and activity of folate conjugated didemnin B for potential treatment of inflammatory diseases
Walter A Henne1, Sumith A Kularatne, Wilfredo Ayala-López
1Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, IN 47907, USA. whenne@govst.edu
Abstract:
A folate receptor targeted didemnin B conjugate was synthesized using a hydrophilic peptide spacer linked to folate via a releasable disulfide carbonate linker. Cell cytotoxicity and TNF-α inhibition in RAW264.7 macrophage-like cells exhibited IC(50)s of 13 and 5 nM, respectively. Folate didemnin B was found to be ∼50-100 fold more potent than didemnin B itself. More importantly, activity of the prodrug was blocked by excess folic acid, demonstrating receptor-mediated cellular uptake of the conjugate.
Related Concept Videos
Drugs for Treatment of Crohn's Disease in IBD Using Immunomodulatory Agents
Drugs for Treatment of Ulcerative Colitis in IBD
Drugs for Treatment of Crohn's Disease in IBD Using Biologic Agents: Anti-TNF
Combined Effects of Drugs: Synergism
Such synergistic combinations...
Drugs for Treatment of Crohn's Disease in IBD Using Glucocorticoids
Inflammatory Bowel Disease IV: Pharmacological Management
Pharmacologic...
