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 |