Novel Abscisic Acid Antagonists Identified with Chemical Array Screening.
Abscisic acid (ABA) signaling is involved in multiple processes in plants, such as water stress control and seed dormancy. Major regulators of ABA signaling are the PYR/PYL/RCAR family receptor proteins, group A protein phosphatases 2C (PP2Cs), and subclass III of SNF1-related protein kinase 2 (SnRK2). Novel ABA agonists and antagonists to modulate the functions of these proteins would not only contribute to clarification of the signaling mechanisms but might also be used to improve crop yields. To obtain small molecules that interact with Arabidopsis ABA receptor PYR1, we screened 24 275 compounds from a chemical library at the RIKEN Natural Products Depository by using a chemical array platform. Subsequent SnRK2 and PP2C assays narrowed down the candidates to two molecules. One antagonized ABA in a competitive manner and inhibited the formation of the PYR1-ABA-PP2C ternary complex. These compounds might have potential as bioprobes to analyze ABA signaling.
Chemical Biology Research Group, RIKEN Center for Sustainable Resource Science, Wako, Saitama, 351-0198, Japan.|Gene Discovery Research Group, RIKEN Center for Sustainable Resource Science, Yokohama, Kanagawa, 230-0045, Japan.
Takuya
T
Ito
Chemical Biology Research Group, RIKEN Center for Sustainable Resource Science, Wako, Saitama, 351-0198, Japan.
Yasumitsu
Y
Kondoh
Chemical Biology Research Group, RIKEN Center for Sustainable Resource Science, Wako, Saitama, 351-0198, Japan.
Kazuko
K
Yoshida
Graduate School of Bio-Applications and Systems Engineering, Tokyo University of Agriculture and Technology, Yokohama, Koganei, Tokyo, 184-8588, Japan.
Taishi
T
Umezawa
Chemical Biology Research Group, RIKEN Center for Sustainable Resource Science, Wako, Saitama, 351-0198, Japan.
Takeshi
T
Shimizu
Gene Discovery Research Group, RIKEN Center for Sustainable Resource Science, Yokohama, Kanagawa, 230-0045, Japan.
Kazuo
K
Shinozaki
Chemical Biology Research Group, RIKEN Center for Sustainable Resource Science, Wako, Saitama, 351-0198, Japan. hisyo@riken.jp.
Hiroyuki
H
Osada
D000040:Abscisic Acid / Q000737:chemistry / Q000494:pharmacology; D017360:Arabidopsis / Q000254:growth & development / Q000378:metabolism; D029681:Arabidopsis Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D018525:Germination / Q000187:drug effects; D057166:High-Throughput Screening Assays; D007700:Kinetics; D026901:Membrane Transport Proteins / Q000378:metabolism; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors / Q000378:metabolism; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism; D011714:Pyrans / Q000737:chemistry; D012639:Seeds / Q000254:growth & development / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology
D029681:Arabidopsis Proteins; D026901:Membrane Transport Proteins; C540976:AT4G17870 protein, Arabidopsis; D011714:Pyrans; D054852:Small Molecule Libraries; D000040:Abscisic Acid; C071570:SNF1-related protein kinases; D017346:Protein Serine-Threonine Kinases; D010749:Phosphoprotein Phosphatases
abscisic acid; antagonist; chemical array; chemical biology; inhibitors; signal transduction