44.タンパク質二量体誘導化合物(CID)を利用した新規植物化学調節剤の創出(口頭発表)

概要

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A dimer of a ligand for a target protein functions in some cases as a chemical inducer of dimerization (CID) that induces dimerization of the target protein. The CID can bind strongly to the target protein because of protein-protein interactions to function as a stronger ligand (an enzyme inhibitor or an antagonist) than the corresponding monomer. However, there have been a few reports (especially no reports for plant enzymes) of CID, probably because chemical modifications for dimerization have a negatively affect on the affinity to the target. Abscinazole-E1 (Abz-E1), which is a uniconazole (UNI) derivative, inhibits CYP707A, a key P450 enzyme of ABA catabolism, as strongly as UNI, in spite of possessing a long diethylene glycol chain. Therefore, a UNI dimer linked by oligoethylene glycol chain may function as a CID for CYP707A. Base on this expectation, we designed and synthesized five UNI dimmers, UTD1-En, and examined their inhibitory activity against CYP707A3 and plant growth. Although UTD1-En inhibited CYP707A as strongly as UNI, we cannot have confirmed in our present assay system whether or not UTD1-En functioned as CID. UTD1-En promoted and inhibited the root elongation of rice seedlings at 30 and 100μM, respectively. This effect depended on the number of ethylene glycol unit, n. Because UNI and Abz-E1 had no effect on the root elongation, this activity may be caused by that two UNI units is linked with an appropriate distance.
2010-10-01