Abstract
TIR1/AFB auxin receptors play a central role in the perception of auxin and regulate the many aspects of auxin-regulated developmental processes in plant. Therefore, specific auxin antagonists on TIR1/AFB receptors are promising chemical tools for auxin biology. We have found that α-alkyl-IAA function as specific auxin antagonists to block TIR1/AFB function. Our efforts for the development of new potent auxin antagonists using virtual screening and structure-based drug design lead to the identification of potent lead compounds, PEO-IAA that showed a high affinity to TIR1 and anti-auxin activities in planta. We then optimized the structure of PEO-IAA to show higher auxin antagonistic activity. As the results of derivatization, mXO-IAA, new antagonistic probe exhibited potent and specific inhibitory activity on SCF (TIR1) signaling.
