1FVT

THE STRUCTURE OF CYCLIN-DEPENDENT KINASE 2 (CDK2) IN COMPLEX WITH AN OXINDOLE INHIBITOR

1FVT の概要

• エントリーDOI: 10.2210/pdb1fvt/pdb
• 分子名称: CELL DIVISION PROTEIN KINASE 2, 4-[(2Z)-2-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazinyl]benzene-1-sulfonamide (3 entities in total)
• 機能のキーワード: cyclin-dependent kinase, oxindole, transferase, cell cycle
• 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: 34371.72

構造登録者

Davis, S.T.,Benson, B.G.,Bramson, H.N.,Chapman, D.E.,Dickerson, S.H.,Dold, K.M.,Eberwein, D.J.,Edelstein, M.,Frye, S.V.,Gampe Jr., R.T.,Griffin, R.J.,Harris, P.A.,Hassell, A.M.,Holmes, W.D.,Hunter, R.N.,Knick, V.B.,Lackey, K.,Lovejoy, B.,Luzzio, M.J.,Murray, D.,Parker, P.,Rocque, W.J.,Shewchuk, L.,Veal, J.M.,Walker, D.H.,Kuyper, L.K. (登録日: 2000-09-20, 公開日: 2001-01-17, 最終更新日: 2024-02-07)

主引用文献

Davis, S.T.,Benson, B.G.,Bramson, H.N.,Chapman, D.E.,Dickerson, S.H.,Dold, K.M.,Eberwein, D.J.,Edelstein, M.,Frye, S.V.,Gampe Jr, R.T.,Griffin, R.J.,Harris, P.A.,Hassell, A.M.,Holmes, W.D.,Hunter, R.N.,Knick, V.B.,Lackey, K.,Lovejoy, B.,Luzzio, M.J.,Murray, D.,Parker, P.,Rocque, W.J.,Shewchuk, L.,Veal, J.M.,Walker, D.H.,Kuyper, L.F.
Prevention of chemotherapy-induced alopecia in rats by CDK inhibitors.
Science, 291:134-137, 2001

PubMed Abstract: Most traditional cytotoxic anticancer agents ablate the rapidly dividing epithelium of the hair follicle and induce alopecia (hair loss). Inhibition of cyclin-dependent kinase 2 (CDK2), a positive regulator of eukaryotic cell cycle progression, may represent a therapeutic strategy for prevention of chemotherapy-induced alopecia (CIA) by arresting the cell cycle and reducing the sensitivity of the epithelium to many cell cycle-active antitumor agents. Potent small-molecule inhibitors of CDK2 were developed using structure-based methods. Topical application of these compounds in a neonatal rat model of CIA reduced hair loss at the site of application in 33 to 50% of the animals. Thus, inhibition of CDK2 represents a potentially useful approach for the prevention of CIA in cancer patients.

PubMed: 11141566
DOI: 10.1126/science.291.5501.134

実験手法

X-RAY DIFFRACTION (2.2 Å)