1sqt
Substituted 2-Naphthamidine Inhibitors of Urokinase
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OverviewOverview
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.
DiseaseDisease
Known disease associated with this structure: Alzheimer disease, late-onset, susceptibility to OMIM:[191840]
About this StructureAbout this Structure
1SQT is a Single protein structure of sequence from Homo sapiens with as ligand. Active as U-plasminogen activator, with EC number 3.4.21.73 Full crystallographic information is available from OCA.
ReferenceReference
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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