81.新規オーキシン受容体阻害剤の分子設計と合成(口頭発表)

概要

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TIR1 is F-Box protein, a component of an SCF-class E3 ubiquitin-ligase and was identified as auxin receptor. Arabdidopsis plants have five redundant auxin receptors, AFBs homologous to TIR1. Therefore, the redundant function of receptors prevents the detailed analysis of physiological role of auxin via TIR1/AFBs signaling. We recently reported alpha-alkyl-auxin as a novel antiauxin probe to specifically modulate TIR1/AFB function. To find more potent auxin probe on TIR1/AFBs, we rationally designed the probes according to crystal structural information of TIR1. On the basis of TIR1 structures, we designed various new auxin probes with high affinity to TIR1 utilizing molecular docking calculation between ligands and target proteins. As the results of biological evaluation, some new probes exhibited high activity on modulating SCF-TIR1 signaling. We also searched TIR1 binding ligands against compound structural databases by in silico screening method. As the results of virtual screening, we identified some candidates of TIR1-specific probes.
植物化学調節学会の論文
2008-10-06