1sqt: Difference between revisions

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[[Image:1sqt.jpg|left|200px]]
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{{STRUCTURE_1sqt|  PDB=1sqt  |  SCENE=  }}  
{{STRUCTURE_1sqt|  PDB=1sqt  |  SCENE=  }}  


'''Substituted 2-Naphthamidine Inhibitors of Urokinase'''
===Substituted 2-Naphthamidine Inhibitors of Urokinase===




==Overview==
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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.
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{{ABSTRACT_PUBMED_15149645}}


==Disease==
==Disease==
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[[Category: Plasminogen activation]]
[[Category: Plasminogen activation]]
[[Category: Serine protease]]
[[Category: Serine protease]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 09:02:17 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 03:01:54 2008''

Revision as of 03:01, 28 July 2008

File:1sqt.png

Template:STRUCTURE 1sqt

Substituted 2-Naphthamidine Inhibitors of UrokinaseSubstituted 2-Naphthamidine Inhibitors of Urokinase

Template:ABSTRACT PUBMED 15149645

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. 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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