radicicol

Radicicol is a macrocyclic antifungal antibiotic (macrolactone) originally isolated from fungi such as Monosporium bonorden and Diheterospora chlamydosporia. It acts primarily as a potent inhibitor of heat shock protein 90 (Hsp90), binding to its N-terminal ATP/ADP-binding site with high affinity and inhibiting its ATPase activity. This inhibition leads to the degradation of Hsp90 client proteins and disrupts multiple signaling pathways including v-Src, Ras-Raf-MAPK, and estrogen receptor signaling. Radicicol also exhibits tyrosine kinase inhibitory activity and has demonstrated antifungal, antimalarial, anti-cancer (in vitro), antiangiogenic effects by inhibiting VEGF secretion in tumor models. However, due to rapid metabolic inactivation in vivo resulting from its chemical instability (notably the presence of an epoxide group), radicicol itself was not advanced into clinical development; instead, more stable derivatives have been explored for therapeutic use[1][5][6].

Other names

Monorden