関連する実験動画
Updated: Jan 13, 2026

Detection of Histone Modifications in Plant Leaves
Published on: September 23, 2011
植物ホルモン受容体調節における反応性拮抗薬戦略:システイン指向型共有結合分子グルー
Minoru Ueda1,2, Kotaro Matsumoto1, Takao Nomura3
1Department of Chemistry, Graduate School of Science, Tohoku University, Sendai, Japan.
Abstract:
Controlling protein-protein interactions (PPIs) remains a challenge in modern chemistry. In plants, jasmonoyl-L-isoleucine (JA-Ile) acts as a molecular glue that facilitates PPIs between the F-box protein COI1 and JAZ repressors, leading to transcriptional reprogramming. However, the functional redundancy of JAZ proteins complicates biological studies. To overcome this, we introduce a reactive antagonist (RA) strategy that selectively induces COI1-JAZ interactions for a Cys-mutated JAZ mutant while inhibiting interactions with wild-type JAZs. We designed and synthesized COR-oxime derivatives, identifying O-bromo-ethyl COR-oxime as an optimal RA, functioning as a Cys-directed covalent molecular glue. Mass spectrometry and fluorescence anisotropy assays confirmed its selective covalent binding to Cys-mutated JAZ1, leading to targeted degradation in Arabidopsis. This strategy enables precise functional dissection of JAZ subtypes without affecting endogenous pathways. Given the genetic redundancy in many biological systems, the RA strategy provides a powerful chemical biology tool for dissecting complex signaling networks beyond plant hormone research.
関連する概念動画
Cell Signaling in Plants
The Two-State Receptor Model
The binding affinity of a drug determines its interaction with...
Ligand-Gated Ion Channel Receptor: Gating Mechanism
Drug-Receptor Interaction: Antagonist
Antagonists can be classified as competitive or noncompetitive based on their...
Plant Hormones
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...

