アブシジン酸の代謝不活性化とシグナル伝達を制御する化合物の創出研究

書誌事項

タイトル別名
  • Studies on creation of specific regulators for abscisic acid catabolism and signal transduction
  • 学会賞 アブシジン酸の代謝不活性化とシグナル伝達を制御する化合物の創出研究
  • ガッカイショウ アブシジンサン ノ タイシャ フカッセイカ ト シグナル デンタツ オ セイギョ スル カゴウブツ ノ ソウシュツ ケンキュウ

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説明

<p>Abscisic acid (ABA) has critical roles in many physiological processes including seed dormancy, stomatal closure and adaptive responses to abiotic stress. Synthetic positive or negative regulators of ABA function are expected to use as not only chemical tools for research in plant biology but also plant growth regulators for agriculture application. We developed inhibitors of ABA-inactivating enzymes as the positive regulators and antagonists of ABA receptors as the negative regulators. (1) Specific inhibitors of ABA-inactivating enzymes: Key enzymes for ABA inactivation are ABA 8′-hydroxylases, cytochrome P450 enzymes classified into the CYP707A subfamily. Because the tertiary structure of CYP707A has never been clarified, we developed the CYP707A inhibitors as ABA analogs (AHI) or azoles (abscinazoles) by lead optimization based on structure-activity relationship. These inhibitors conferred drought tolerance in plants. (2) Antagonists of ABA receptors: ABA signaling is repressed by PP2Cs, but stress-induced ABA binds PYL, which then bind and inhibit PP2Cs. X-ray structures of several receptor-ABA complexes revealed a tunnel above ABA’s 3′-CH and 4′-CO that opens at the PP2C binding interface. Because ABA analogs with sufficiently long 3′ or 4′ chains were predicted to traverse this tunnel and block PYL-PP2C interactions, we designed and synthesized AS6 and PAN. These compounds functioned as a potent ABA antagonist to block multiple stress-induced ABA responses in vivo.</p>

収録刊行物

  • 植物の生長調節

    植物の生長調節 51 (1), 1-7, 2016

    一般社団法人 植物化学調節学会

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