RRC ID 63920
著者 Matsuoka S, Sato K, Maruki-Imamura R, Noutoshi Y, Okabe T, Kojima H, Umezawa T.
タイトル Identification of novel compounds that inhibit SnRK2 kinase activity by high-throughput screening.
ジャーナル Biochem Biophys Res Commun
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 character ization of these compounds by in vitro phosphorylation assays confirmed that three of the ten com pounds 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.
巻・号 537
ページ 57-63
公開日 2020-12-29
DOI 10.1016/j.bbrc.2020.12.046
PII S0006-291X(20)32223-3
PMID 33385806
MeSH Abscisic Acid / pharmacology Arabidopsis / drug effects Arabidopsis / enzymology* Arabidopsis / genetics Arabidopsis Proteins / antagonists & inhibitors* Arabidopsis Proteins / metabolism Gene Expression Regulation, Plant / drug effects Genes, Plant High-Throughput Screening Assays* Phosphorylation / drug effects Protein Kinase Inhibitors / analysis* Protein Kinase Inhibitors / chemistry Protein Kinase Inhibitors / pharmacology* Protein Serine-Threonine Kinases / antagonists & inhibitors* Protein Serine-Threonine Kinases / metabolism Recombinant Proteins / metabolism
IF 2.985
リソース情報
シロイヌナズナ / 植物培養細胞・遺伝子 rpc00008