1C5R

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

Summary for 1C5R

Entry DOI	10.2210/pdb1c5r/pdb
Descriptor	PROTEIN (TRYPSIN), CITRATE ANION, CALCIUM ION, ... (6 entities in total)
Functional Keywords	selective, s1 site inhibitor, structure-based drug design, urokinase, trypsin, thrombin, hydrolase
Biological source	Bos taurus (cattle)
Cellular location	Secreted, extracellular space: P00760
Total number of polymer chains	1
Total formula weight	24048.73
Authors	Katz, B.A.,Mackman, R.,Luong, C.,Radika, K.,Martelli, A.,Sprengeler, P.A.,Wang, J.,Chan, H.,Wong, L. (deposition date: 1999-12-22, release date: 2000-12-22, Last modification date: 2024-10-16)
Primary citation	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 Cited by 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 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.47 Å)

Structure validation