書誌事項
- タイトル別名
-
- Target Identification and Mode of Action Studies of an Antitumor Compound Aplyronine A by Using Photoaffinity Derivatives
- ヒカリ シンワセイ プローブ オ モチイタ コウシュヨウセイ テンネンブツ アプリロニン A ノ ヒョウテキ ブンシ ト サヨウ キジョ ノ ケンキュウ
この論文をさがす
抄録
Actin is an essential cytoskeletal protein for the regulation of various cellular functions. A number of actin-stabilizing and depolymerizing agents have been discovered in marine invertebrates, and they show potent cytotoxicity. Among them, a polyketide macrolide aplyronine A has antitumor effects against xenograft in mice. However, the potent cytotoxicity and apoptogenic effect of aplyronine A was not entirely accounted for by its actin filament-severing properties, and its molecular targets and mechanisms of action remained unclear. We developed aplyronine A acetylene or biotin derivatives that bear an aryldiazirine group at the C34 terminus, which formed a covalent bond with actin. By using these chemical probes, we have showed that aplyronine A synergistically binds to tubulin in association with actin, and prevents spindle formation and mitosis in tumor cells. Our findings of aplyronine A will provide further insights into the molecular mechanisms of structurally diverse natural products that regulate cytoskeletal dynamics.
収録刊行物
-
- 有機合成化学協会誌
-
有機合成化学協会誌 73 (2), 151-160, 2015
公益社団法人 有機合成化学協会
- Tweet
キーワード
詳細情報 詳細情報について
-
- CRID
- 1390001205341346944
-
- NII論文ID
- 130005129432
-
- NII書誌ID
- AN0024521X
-
- ISSN
- 18836526
- 00379980
-
- NDL書誌ID
- 026084837
-
- 本文言語コード
- ja
-
- データソース種別
-
- JaLC
- NDL
- Crossref
- CiNii Articles
- KAKEN
-
- 抄録ライセンスフラグ
- 使用不可