Synthetic agonist of HTL/KAI2 shows potent stimulating activity for Arabidopsis seed germination
| Autor: | Tadao Asami, Hiroyuki Kasahara, Kazushi Arai, Ken-ichiro Hayashi, Kosuke Fukui |
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| Rok vydání: | 2019 |
| Předmět: |
Agonist
Hydrolases medicine.drug_class Clinical Biochemistry Mutant Arabidopsis Pharmaceutical Science Strigolactone Germination Ligands 01 natural sciences Biochemistry Structure-Activity Relationship Drug Discovery Hydrolase medicine Furans Molecular Biology biology Arabidopsis Proteins 010405 organic chemistry Chemistry Organic Chemistry Temperature Ligand (biochemistry) biology.organism_classification 0104 chemical sciences Karrikin 010404 medicinal & biomolecular chemistry Seeds Molecular Medicine Plant hormone Signal Transduction |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 29:2487-2492 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2019.07.018 |
| Popis: | HTL/KAI2, a member of the α/β-fold hydrolase superfamily, is known to be a receptor-like protein of lactone compounds and that triggers seed germination of Arabidopsis. However, the endogenous ligand and physiological roles of HTL/KAI2 have remained unclear. To understand the mechanism underlying seed germination involved in HTL/KAI2 signaling, it is necessary to identify the endogenous ligand of HTL/KAI2. To date, even a biosynthetic mutant of the ligand has not yet been isolated. Because exogenous agonistic chemicals can only be purchased in small amounts at high prices, the limited supply of those chemicals has hampered any large-scale experiments, such as mutant screening. Therefore, easily synthesized and scalable artificial agonist would remove the limitation of the chemical supply and contribute to the identification of the endogenous ligand of HTL/KAI2 and/or the biosynthetic mutants. In this study, we demonstrated that designed chemicals with a phenoxyfuranone scaffold potently stimulated seed germination via HTL/KAI2 in Arabidopsis. As a result of screening of these chemicals, we selected a representative compound with convincing selectivity. Here in, we provide a new promising synthetic agonist of HTL/KAI2. |
| Databáze: | OpenAIRE |
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