1sqt
From Proteopedia
(New page: 200px<br /> <applet load="1sqt" size="450" color="white" frame="true" align="right" spinBox="true" caption="1sqt, resolution 1.90Å" /> '''Substituted 2-Napht...) |
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caption="1sqt, resolution 1.90Å" /> | caption="1sqt, resolution 1.90Å" /> | ||
'''Substituted 2-Naphthamidine Inhibitors of Urokinase'''<br /> | '''Substituted 2-Naphthamidine Inhibitors of Urokinase'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1SQT 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 UI3 as [http://en.wikipedia.org/wiki/ligand ligand]. 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:// | + | 1SQT 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=UI3:'>UI3</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. 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=1SQT 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 16:54:30 2008'' |
Revision as of 14:54, 15 February 2008
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Substituted 2-Naphthamidine Inhibitors of Urokinase
Contents |
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
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.
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
Page seeded by OCA on Fri Feb 15 16:54:30 2008
Categories: Homo sapiens | Single protein | U-plasminogen activator | Geyer, A. | Giranda, V.L. | Klinghofer, V. | Mantei, R. | McClellan, W.J. | Nienaber, V. | Rockway, T.W. | Stewart, K. | Weitzberg, M. | Wendt, M.D. | Zhang, X. | UI3 | Egf-like domain | Glycoprotein | Hydrolase | Kringle | Plasminogen activation | Serine protease
