1C5X

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

Summary for 1C5X

• Entry DOI: 10.2210/pdb1c5x/pdb
• Descriptor: PROTEIN (UROKINASE-TYPE PLASMINOGEN ACTIVATOR), CITRATE ANION, 4-IODOBENZO[B]THIOPHENE-2-CARBOXAMIDINE, ... (5 entities in total)
• Functional Keywords: selective, s1 site inhibitor, structure-based drug design, urokinase, trypsin, thrombin, blood clotting
• Biological source: Homo sapiens (human); More
• Cellular location: Secreted: P00749 P00749
• Total number of polymer chains: 2
• Total formula weight: 32014.05

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: 2024-04-03)

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

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

Experimental method

X-RAY DIFFRACTION (1.75 Å)