verticillin A

Verticillin A is a **natural fungal metabolite** classified as an epipolythiodioxopiperazine (ETP) alkaloid, originally isolated from fungi such as *Amanita flavorubescens* with parasitic fungi *Hypomyces hyalines*. It exhibits **potent antitumor activity** in preclinical models against several cancers, including **colon cancer**, **pancreatic cancer**, and **ovarian cancer**. Verticillin A acts primarily as a **selective inhibitor of histone methyltransferases**, targeting enzymes such as SUV39H1, SUV39H2, G9a, MLL1, and GLP, resulting in the **altered methylation of histone marks** (notably H3K9 and H3K4 methylation), induction of apoptosis, and disruption of cancer cell migration and invasion[1][3][5][7]. Additional mechanisms include suppression of the c-Met pathway and its downstream effectors (Ras/Raf/MEK/ERK, AKT), and regulation of immune checkpoint molecules such as PD-L1, potentially **sensitizing tumors to immune checkpoint blockade therapy**[1][3][7]. Verticillin A is not an approved drug and is under preclinical or early-stage development as an investigational anticancer therapeutic.

Other names

verrupectin