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TitleChemical inhibition of Arabidopsis PIN-FORMED auxin transporters by the anti-inflammatory drug naproxen.
Journal, issue, pagesPlant Commun, Vol. 4, Issue 6, Page 100632, Year 2023
Publish dateNov 13, 2023
AuthorsJing Xia / Mengjuan Kong / Zhisen Yang / Lianghanxiao Sun / Yakun Peng / Yanbo Mao / Hong Wei / Wei Ying / Yongxiang Gao / Jiří Friml / Jianping Weng / Xin Liu / Linfeng Sun / Shutang Tan /
PubMed AbstractThe phytohormone auxin plays central roles in many growth and developmental processes in plants. Development of chemical tools targeting the auxin pathway is useful for both plant biology and ...The phytohormone auxin plays central roles in many growth and developmental processes in plants. Development of chemical tools targeting the auxin pathway is useful for both plant biology and agriculture. Here we reveal that naproxen, a synthetic compound with anti-inflammatory activity in humans, acts as an auxin transport inhibitor targeting PIN-FORMED (PIN) transporters in plants. Physiological experiments indicate that exogenous naproxen treatment affects pleiotropic auxin-regulated developmental processes. Additional cellular and biochemical evidence indicates that naproxen suppresses auxin transport, specifically PIN-mediated auxin efflux. Moreover, biochemical and structural analyses confirm that naproxen binds directly to PIN1 protein via the same binding cavity as the indole-3-acetic acid substrate. Thus, by combining cellular, biochemical, and structural approaches, this study clearly establishes that naproxen is a PIN inhibitor and elucidates the underlying mechanisms. Further use of this compound may advance our understanding of the molecular mechanisms of PIN-mediated auxin transport and expand our toolkit in auxin biology and agriculture.
External linksPlant Commun / PubMed:37254481 / PubMed Central
MethodsEM (single particle)
Resolution3.7 Å
Structure data

36254

8jh5

EMDB-36254, PDB-8jh5:
Structure of the auxin exporter PIN1 in Arabidopsis thaliana in the Naproxen-bound state
Method: EM (single particle) / Resolution: 3.7 Å

Chemicals

ChemComp-NPS:
(2S)-2-(6-methoxynaphthalen-2-yl)propanoic acid / antiinflammatory*YM

Source
  • arabidopsis thaliana (thale cress)
  • escherichia coli (E. coli)
KeywordsPLANT PROTEIN / membrane transporter

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