5GJA

Crystal structure of Arabidopsis thaliana ACO2 in complex with 2-PA

Summary for 5GJA

• Entry DOI: 10.2210/pdb5gja/pdb
• Related: 5GJ9
• Descriptor: 1-aminocyclopropane-1-carboxylate oxidase 2, ZINC ION, PYRIDINE-2-CARBOXYLIC ACID, ... (4 entities in total)
• Functional Keywords: ethylene oxidase inhibitor, oxidoreductase
• Biological source: Arabidopsis thaliana (Mouse-ear cress)
• Total number of polymer chains: 8
• Total formula weight: 277589.18

Authors

Sun, X.Z.,Li, Y.X.,He, W.R.,Ji, C.G.,Xia, P.X.,Wang, Y.C.,Du, S.,Li, H.J.,Raikhel, N.,Xiao, J.Y.,Guo, H.W. (deposition date: 2016-06-28, release date: 2017-05-10, Last modification date: 2024-03-20)

Primary citation

Sun, X.,Li, Y.,He, W.,Ji, C.,Xia, P.,Wang, Y.,Du, S.,Li, H.,Raikhel, N.,Xiao, J.,Guo, H.
Pyrazinamide and derivatives block ethylene biosynthesis by inhibiting ACC oxidase.
Nat Commun, 8:15758-15758, 2017

PubMed Abstract: Ethylene is an important phytohormone that promotes the ripening of fruits and senescence of 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 to treat tuberculosis, as an inhibitor of ethylene biosynthesis in Arabidopsis thaliana, using a chemical genetics approach. PZA is converted to pyrazinecarboxylic acid (POA) in plant cells, suppressing the activity of 1-aminocyclopropane-1-carboxylic acid oxidase (ACO), the enzyme catalysing the final step of ethylene formation. The crystal structures of Arabidopsis ACO2 in complex with POA or 2-Picolinic Acid (2-PA), a POA-related compound, reveal that POA/2-PA bind at the active site of ACO, preventing the enzyme from interacting with its natural substrates. Our work suggests that PZA and its derivatives may be promising regulators of plant metabolism, in particular ethylene biosynthesis.

PubMed: 28604689
DOI: 10.1038/ncomms15758

Experimental method

X-RAY DIFFRACTION (2.1 Å)