Drug intelligence / Profile preview

aplyronine a

Development stage
Preclinical
Modality
RNA-Targeting Small Molecules → Nucleic Acid-Directed Small Molecules → Small Molecules, Peptides
Administration
Intravenous
01

Overview

Aplyronine A is a highly potent antitumor macrolide compound originally isolated from the sea hare Aplysia kurodai. It exhibits strong cytotoxic activity, primarily through its unique mechanism of disrupting cytoskeletal dynamics by dual targeting of both actin and tubulin. Aplyronine A induces protein-protein interactions between actin and tubulin, inhibits the polymerization of G-actin to F-actin, and depolymerizes F-actin to G-actin. This results in disruption of cell division and potent antimitotic effects. Its picomolar-level cytotoxicity and novel mode of action make it an attractive candidate for development as an anticancer agent, including as a payload for antibody–drug conjugates in cancer chemotherapy[2][3][4][5][6][7].

02

Targets

Actin filament proteinsActin–tubulin protein–protein interfaceTUBB (Tubulin (alpha and beta subunits))

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