1N95

Aryl Tetrahydrophyridine Inhbitors of Farnesyltranferase: Glycine, Phenylalanine and Histidine Derivatives

1N95 の概要

• エントリーDOI: 10.2210/pdb1n95/pdb
• 関連するPDBエントリー: 1N94 1N9A
• 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, histidine 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: 83867.52

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: glycine, phenylalanine and histidine derivatives.
Bioorg.Med.Chem.Lett., 13:1359-1362, 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 a series of aryl tetrahydropyridines that incorporate substituted glycine, phenylalanine and histidine residues. The design, synthesis, SAR and biological properties of these compounds will be discussed.

PubMed: 12657282
DOI: 10.1016/S0960-894X(03)00095-7

実験手法

X-RAY DIFFRACTION (2.3 Å)