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1u6q

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==Overview==
==Overview==
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A series of non-amide-linked 6-substituted-2-naphthamidine urokinase, plasminogen activator (uPA) inhibitors are described. These compounds, possess excellent binding activities and selectivities with significantly, improved pharmacokinetic profiles versus previously described amide-linked, inhibitors.
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A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors.
==Disease==
==Disease==
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[[Category: U-plasminogen activator]]
[[Category: U-plasminogen activator]]
[[Category: Bruncko, M.]]
[[Category: Bruncko, M.]]
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[[Category: Dalton, C.R.]]
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[[Category: Dalton, C R.]]
[[Category: Geyer, A.]]
[[Category: Geyer, A.]]
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[[Category: Giranda, V.L.]]
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[[Category: Giranda, V L.]]
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[[Category: Kaminski, M.K.]]
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[[Category: Kaminski, M K.]]
[[Category: McClellan, W.]]
[[Category: McClellan, W.]]
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[[Category: Nienaber, V.L.]]
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[[Category: Nienaber, V L.]]
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[[Category: Rockway, T.R.]]
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[[Category: Rockway, T R.]]
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[[Category: Sauer, D.R.]]
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[[Category: Sauer, D R.]]
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[[Category: Wendt, M.D.]]
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[[Category: Wendt, M D.]]
[[Category: 745]]
[[Category: 745]]
[[Category: hydrolase]]
[[Category: hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:59:23 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:21:08 2008''

Revision as of 13:21, 21 February 2008


1u6q, resolution 2.02Å

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Substituted 2-Naphthamadine inhibitors of Urokinase

Contents

Overview

A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors.

Disease

Known disease associated with this structure: Alzheimer disease, late-onset, susceptibility to OMIM:[191840]

About this Structure

1U6Q 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

Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties., Bruncko M, McClellan WJ, Wendt MD, Sauer DR, Geyer A, Dalton CR, Kaminski MA, Weitzberg M, Gong J, Dellaria JF, Mantei R, Zhao X, Nienaber VL, Stewart K, Klinghofer V, Bouska J, Rockway TW, Giranda VL, Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8. PMID:15582418

Page seeded by OCA on Thu Feb 21 15:21:08 2008

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