Identification of novel compounds that inhibit SnRK2 kinase activity by high-throughput screening

Shoko Matsuoka, Karin Sato, Riyo Maruki-Imamura, Yoshiteru Noutoshi, Takayoshi Okabe, Hirotatsu Kojima, Taishi Umezawa

Research output: Contribution to journalArticlepeer-review

Abstract

Abscisic acid (ABA) is a major phytohormone that regulates abiotic stress responses and development. SNF1-rerated protein kinase 2 (SnRK2) is a key regulator of ABA signaling. To isolate compounds which directly affect SnRK2 activity, we optimized a fluorescence-based system for high-throughput screening (HTS) of SnRK2 kinase regulators. Using this system, we screened a chemical library consisting of 16,000 compounds and identified ten compounds (INH1-10) as potential SnRK2 inhibitors. Further characterization of these compounds by in vitro phosphorylation assays confirmed that three of the ten compounds were SnRK2-specific kinase inhibitors. In contrast, seven of ten compounds inhibited ABA-responsive gene expression in Arabidopsis cells. From these results, INH1 was identified as a SnRK2-specific inhibitor in vitro and in vivo. We propose that INH1 could be a lead compound of chemical tools for studying ABA responses in various plant species.

Original languageEnglish
Pages (from-to)57-63
Number of pages7
JournalBiochemical and Biophysical Research Communications
Volume537
DOIs
Publication statusPublished - Jan 22 2021

Keywords

  • ABA signaling
  • Drought stress
  • High-throughput screening
  • Kinase inhibitor
  • SNF1-Related protein kinase 2

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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