Pyrazinamide and derivatives block ethylene biosynthesis by inhibiting ACC oxidase.

摘要: Ethylene is an important phytohormone that promotes the ripening of fruits and senescence flowers thereby reducing their shelf lives. Specific ethylene biosynthesis inhibitors would help to decrease postharvest loss. Here, we identify pyrazinamide (PZA), a clinical drug used treat tuberculosis, as inhibitor in Arabidopsis thaliana, using chemical genetics approach. PZA converted pyrazinecarboxylic acid (POA) plant cells, suppressing activity 1-aminocyclopropane-1-carboxylic oxidase (ACO), enzyme catalysing final step formation. The crystal structures ACO2 complex with POA or 2-Picolinic Acid (2-PA), POA-related compound, reveal POA/2-PA bind at active site ACO, preventing from interacting its natural substrates. Our work suggests derivatives may be promising regulators metabolism, particular biosynthesis.