Synthetic agonist of HTL/KAI2 shows potent stimulating activity for Arabidopsis seed germination

Bioorg Med Chem Lett. 2019 Sep 1;29(17):2487-2492. doi: 10.1016/j.bmcl.2019.07.018. Epub 2019 Jul 9.

Abstract

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.

Keywords: HTL/KAI2; Karrikin; Plant hormone; Seed germination; Strigolactone.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arabidopsis / growth & development*
  • Arabidopsis / metabolism
  • Arabidopsis Proteins / agonists*
  • Arabidopsis Proteins / metabolism
  • Furans / chemical synthesis
  • Furans / chemistry
  • Furans / pharmacology
  • Germination* / drug effects
  • Hydrolases / metabolism
  • Ligands
  • Seeds / growth & development
  • Seeds / metabolism
  • Signal Transduction / drug effects
  • Structure-Activity Relationship
  • Temperature

Substances

  • Arabidopsis Proteins
  • Furans
  • Ligands
  • HTL protein, Arabidopsis
  • Hydrolases