1C5R

STRUCTURAL BASIS FOR SELECTIVITY OF A SMALL MOLECULE, S1-BINDING, SUB-MICROMOLAR INHIBITOR OF UROKINASE TYPE PLASMINOGEN ACTIVATOR

1C5R の概要

• エントリーDOI: 10.2210/pdb1c5r/pdb
• 分子名称: PROTEIN (TRYPSIN), CITRATE ANION, CALCIUM ION, ... (6 entities in total)
• 機能のキーワード: selective, s1 site inhibitor, structure-based drug design, urokinase, trypsin, thrombin, hydrolase
• 由来する生物種: Bos taurus (cattle)
• 細胞内の位置: Secreted, extracellular space: P00760
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 24048.73

構造登録者

Katz, B.A.,Mackman, R.,Luong, C.,Radika, K.,Martelli, A.,Sprengeler, P.A.,Wang, J.,Chan, H.,Wong, L. (登録日: 1999-12-22, 公開日: 2000-12-22, 最終更新日: 2024-10-16)

主引用文献

Katz, B.A.,Mackman, R.,Luong, C.,Radika, K.,Martelli, A.,Sprengeler, P.A.,Wang, J.,Chan, H.,Wong, L.
Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.
Chem.Biol., 7:299-312, 2000

PubMed Abstract: Urokinase-type plasminogen activator (uPA) is a protease associated with tumor metastasis and invasion. Inhibitors of uPA may have potential as drugs for prostate, breast and other cancers. Therapeutically useful inhibitors must be selective for uPA and not appreciably inhibit the related, and structurally and functionally similar enzyme, tissue-type plasminogen activator (tPA), involved in the vital blood-clotting cascade.

PubMed: 10779411
DOI: 10.1016/S1074-5521(00)00104-6

実験手法

X-RAY DIFFRACTION (1.47 Å)