1sqa: Difference between revisions
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'''Substituted 2-Naphthamidine Inhibitors of Urokinase'''<br /> | '''Substituted 2-Naphthamidine Inhibitors of Urokinase'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
1SQA is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4 and UI1 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] Full crystallographic information is available from [http:// | 1SQA is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=UI1:'>UI1</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SQA OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: serine protease]] | [[Category: serine protease]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:54:22 2008'' | ||
Revision as of 17:54, 15 February 2008
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Substituted 2-Naphthamidine Inhibitors of Urokinase
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
1SQA is a Single protein structure of sequence from Homo sapiens with and as ligands. 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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