Marine-derived anthranilamides turn out to be selective HDAC6 inhibitors for colitis
- A marine natural product was optimized at multiple positions into anthranilamide analogues for inflammatory bowel disease.
- The lead compound curbed IL-6 and IL-1β in cells and proved a selective HDAC inhibitor, favoring HDAC6 over HDAC1.
- Docking proposed its HDAC6 binding mode, and it eased colonic damage in a DSS colitis mouse model.
💡 Points Based on the abstract
A preference for HDAC6 over HDAC1 is notable, but docking alone shouldn't settle it. A full isoform panel and a cellular readout comparing tubulin and histone acetylation would test it. Whether the anti-inflammatory effect is on-target is a separate question, answerable with an HDAC6 knockout or tool-inhibitor control; binding kinetics of the zinc-binding group may also shape isoform selectivity.