アクチン脱重合分子の合成と活性

DOI Web Site 被引用文献6件 参考文献30件

書誌事項

タイトル別名
  • Synthesis and Biological Activity of Actin-depolymerizing Substances
  • アクチン ダツジュウゴウ ブンシ ノ ゴウセイ ト カッセイ

この論文をさがす

説明

Aplyronine A 1 is a potent antitumor macrolide isolated from the sea hare Aplysia kurodai. Aplyronine A interacts with actin, one of the major proteins in cytoskeleton. We achieved total synthesis of aplyronine A and its 18 analogs and investigated structure-activity relationships. Analysis of the interaction of aplyronine analogs with actin by a photoaffinity labeling method and X-ray crystal structure analysis of actin complex with aplyronine A have been carried out. These results revealed that aplyronine A binds to actin at the hydrophobic cleft between subdomains 1 and 3 of actin. The binding mode of the macrolactone part of aplyronine A was different from previously reported macrolides. In addition, the trimethylserine moiety of aplyronine A, the essential functional group for cytotoxicity against HeLa S3 cells, was sticking out from a surface of actin-aplyro-nine A complex.

収録刊行物

被引用文献 (6)*注記

もっと見る

参考文献 (30)*注記

もっと見る

関連プロジェクト

もっと見る

キーワード

詳細情報 詳細情報について

問題の指摘

ページトップへ