1N9A

Farnesyltransferase complex with tetrahydropyridine inhibitors

1N9A の概要

• エントリーDOI: 10.2210/pdb1n9a/pdb
• 関連するPDBエントリー: 1N94 1N95
• 分子名称: Protein farnesyltransferase alpha subunit, Protein farnesyltransferase beta subunit, ZINC ION, ... (5 entities in total)
• 機能のキーワード: farnesyltransferase, tetrahydropyridine, prenyltransferase, transferase
• 由来する生物種: Rattus norvegicus (Norway rat); 詳細
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 83824.45

構造登録者

Gwaltney II, S.L.,O'Conner, S.J.,Nelson, L.T.,Sullivan, G.M.,Imade, H.,Wang, W.,Hasvold, L.,Li, Q.,Cohen, J.,Gu, W.Z. (登録日: 2002-11-22, 公開日: 2003-01-07, 最終更新日: 2024-02-14)

主引用文献

Gwaltney II, S.L.,O'Connor, S.J.,Nelson, L.T.,Sullivan, G.M.,Imade, H.,Wang, W.,Hasvold, L.,Li, Q.,Cohen, J.,Gu, W.Z.,Tahir, S.K.,Bauch, J.,Marsh, K.,Ng, S.C.,Frost, D.J.,Zhang, H.,Muchmore, S.,Jakob, C.G.,Stoll, V.,Hutchins, C.,Rosenberg, S.H.,Sham, H.L.
Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.
Bioorg.Med.Chem.Lett., 13:1363-1366, 2003

PubMed Abstract: Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered bioavailable aryl tetrahydropyridines that are potent in cell culture. The design, synthesis, SAR and biological properties of these compounds will be discussed.

PubMed: 12657283
DOI: 10.1016/S0960-894X(03)00094-5

実験手法

X-RAY DIFFRACTION (3.2 Å)