5. Molecular design of auxin antagonists specific to TIR1/AFB auxin receptors

DOI

Bibliographic Information

Other Title
  • 5.TIR1/AFBオーキシン受容体特異的拮抗剤の分子設計(口頭発表)

Search this article

Description

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.

Journal

Details 詳細情報について

  • CRID
    1390282679399174144
  • NII Article ID
    110007767105
  • DOI
    10.18978/jscrpanb.45.0_22
  • ISSN
    21896313
    09191887
  • Text Lang
    ja
  • Data Source
    • JaLC
    • CiNii Articles
  • Abstract License Flag
    Disallowed

Report a problem

Back to top