1sqa | pdb_00001sqa
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| 1sqa, resolution 2.00Å | |||||||||||||
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| Ligands: | SO4, UI1 | ||||||||||||
| Gene: | PLAU (Homo sapiens) | ||||||||||||
| Activity: | U-plasminogen activator, with EC number 3.4.21.73 | ||||||||||||
| Related: | 1OWD, 1OWE, 1OWH, 1OWI, 1OWJ, 1OWK, 1SQO, 1SQT
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
Substituted 2-Naphthamidine Inhibitors of Urokinase
Overview
Several 8-substituted 2-naphthamidine-based inhibitors of the serine protease urokinase plasminogen activator (uPA) are described. Direct attachment of five-membered saturated or unsaturated rings improved inhibitor performance; substitution with sulfones further improved binding profiles. Combination of these substituents or of previously described NH-linked heteroaromatic rings with 6-phenyl amide substituents provided further enhancements to potency and selectivity.
Disease
Known disease associated with this structure: Alzheimer disease, late-onset, susceptibility to OMIM:[191840]
About this Structure
1SQA is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors., Wendt MD, Geyer A, McClellan WJ, Rockway TW, Weitzberg M, Zhao X, Mantei R, Stewart K, Nienaber V, Klinghofer V, Giranda VL, Bioorg Med Chem Lett. 2004 Jun 21;14(12):3063-8. PMID:15149645
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