1sqt

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{{STRUCTURE_1sqt| PDB=1sqt | SCENE= }}
{{STRUCTURE_1sqt| PDB=1sqt | SCENE= }}
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'''Substituted 2-Naphthamidine Inhibitors of Urokinase'''
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===Substituted 2-Naphthamidine Inhibitors of Urokinase===
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==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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(as it appears on PubMed at http://www.pubmed.gov), where 15149645 is the PubMed ID number.
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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]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 09:02:17 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 03:01:54 2008''

Revision as of 00:01, 28 July 2008

Image:1sqt.png

Template:STRUCTURE 1sqt

Contents

Substituted 2-Naphthamidine Inhibitors of Urokinase

Template:ABSTRACT PUBMED 15149645

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. 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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