76.オーキシン不活性化を阻害する安定な化学的ツール : IAA-アミノ酸複合体合成酵素(GH3)阻害剤の阻害活性(口頭発表)

概要

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The formation and degradation of IAA-amino acid conjugates (IAA-aa) play an important role in auxin homeostasis. GH3s encode IAA-aa synthetases, but their functional redundancy has hampered the genetic approach to study auxin homeostasis. GH3s belong to the acyl-activating enzyme superfamily that activates IAA by adenylation. According to this catalytic mechanism, we previously designed and synthesized N-sulfamoyladenosine (SA) derivatives of auxins (IAA-SA, PAA-SA, NAA-SA and 2,4-D-SA) as intermediate analog inhibitors of GH3s. Previous studies indicated that the SA derivatives served as potent in vitro inhibitors of GH3s and exhibited in vivo activities. To improve the in vivo activity, we designed and synthesized a series of N-acylsulfamide derivatives that are chemically stable and more hydrophobic than SA derivatives. The sulfamide derivatives showed the inhibitory activities for GH3s as comparable to the SA derivatives.
植物化学調節学会の論文
2008-10-06