2B52

Human cyclin dependent kinase 2 (CDK2) complexed with DPH-042562

2B52 の概要

• エントリーDOI: 10.2210/pdb2b52/pdb
• 関連するPDBエントリー: 2B53 2B54 2B55
• 分子名称: Cell division protein kinase 2, 1-(3-(2,4-DIMETHYLTHIAZOL-5-YL)-4-OXO-2,4-DIHYDROINDENO[1,2-C]PYRAZOL-5-YL)-3-(4-METHYLPIPERAZIN-1-YL)UREA (3 entities in total)
• 機能のキーワード: protein kinase, cell cycle, phosphorylation, cell division, mitosis, inhibition, transferase
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 34414.01

構造登録者

Muckelbauer, J. (登録日: 2005-09-27, 公開日: 2005-10-11, 最終更新日: 2024-02-14)

主引用文献

Yue, E.W.,Dimeo, S.V.,Higley, C.A.,Markwalder, J.A.,Burton, C.R.,Benfield, P.A.,Grafstrom, R.H.,Cox, S.,Muckelbauer, J.K.,Smallwood, A.,Chen, H.,Chang, C.-H.,Trainor, G.L.,Seitz, S.P.
Synthesis and Evaluation of Indenopyrazoles as Cyclin-Dependent Kinase Inhibitors. Part 4: Heterocycles at C3
Bioorg.Med.Chem.Lett., 14:343-346, 2004

PubMed Abstract: New indeno[1,2-c]pyrazol-4-one cyclin dependent kinase inhibitors have been disclosed. The most promising compounds are nanomolar enzyme inhibitors with excellent activity against tumor cells. The most advanced compound retains cell culture activity even in the presence of human serum proteins. The most advanced compound did not kill the normal fibroblast line AG1523.

PubMed: 14698155
DOI: 10.1016/j.bmcl.2003.11.008

実験手法

X-RAY DIFFRACTION (1.88 Å)