largazole

Largazole is a potent, marine-derived cyclic depsipeptide originally isolated from the cyanobacterium *Symploca* sp. It is primarily characterized as a highly selective Class I histone deacetylase (HDAC) inhibitor. Structurally, largazole functions as a prodrug; its thioester linkage is cleaved in vivo to release a free thiol group, which then coordinates with the zinc ion in the active site of HDAC enzymes. Beyond its well-documented epigenetic effects, recent research has identified largazole as a potential inhibitor of the RNA-binding protein Musashi-2 (MSI2), which is often upregulated in various malignancies. By inhibiting MSI2, largazole suppresses downstream oncogenic pathways such as the mammalian target of rapamycin (mTOR) signaling. It has demonstrated significant antiproliferative and pro-apoptotic activity in preclinical models of non-small cell lung cancer (NSCLC), chronic myeloid leukemia (CML), and colorectal cancer, making it a promising candidate for further oncological development.

Other names

largazole