2ZIS

Crystal Structure of rat protein farnesyltransferase complexed with a bezoruran inhibitor and FPP

2ZIS の概要

• エントリーDOI: 10.2210/pdb2zis/pdb
• 関連するPDBエントリー: 2ZIR
• 分子名称: Protein farnesyltransferase subunit alpha, Protein farnesyltransferase subunit beta, ACETIC ACID, ... (8 entities in total)
• 機能のキーワード: prenyltransferase, transferase, metal-binding, phosphoprotein
• 由来する生物種: Rattus norvegicus (Rat); 詳細
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 94410.23

構造登録者

Fukami, T.A.,Sogabe, S.,Nagata, Y.,Kondoh, O.,Ishii, N. (登録日: 2008-02-22, 公開日: 2009-02-24, 最終更新日: 2023-11-01)

主引用文献

Asoh, K.,Kohchi, M.,Hyoudoh, I.,Ohtsuka, T.,Masubuchi, M.,Kawasaki, K.,Ebiike, H.,Shiratori, Y.,Fukami, T.A.,Kondoh, O.,Tsukaguchi, T.,Ishii, N.,Aoki, Y.,Shimma, N.,Sakaitani, M.
Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors
Bioorg.Med.Chem.Lett., 19:1753-1757, 2009

PubMed Abstract: A series of benzofuran-based farnesyltransferase inhibitors have been designed and synthesized as antitumor agents. Among them, 11f showed the most potent enzyme inhibitory activity (IC(50)=1.1nM) and antitumor activity in human cancer xenografts in mice.

PubMed: 19217288
DOI: 10.1016/j.bmcl.2009.01.074

実験手法

X-RAY DIFFRACTION (2.6 Å)