1fv9: Difference between revisions

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[[Image:1fv9.gif|left|200px]]
{{Seed}}
[[Image:1fv9.png|left|200px]]


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{{STRUCTURE_1fv9|  PDB=1fv9  |  SCENE=  }}  
{{STRUCTURE_1fv9|  PDB=1fv9  |  SCENE=  }}  


'''Crystal structure of human microurokinase in complex with 2-amino-5-hydroxy-benzimidazole'''
===Crystal structure of human microurokinase in complex with 2-amino-5-hydroxy-benzimidazole===




==Overview==
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Using an NMR-based screen, a novel class of urokinase inhibitors were identified that contain a 2-aminobenzimidazole moiety. The inhibitory potency of this family of inhibitors is similar to that of inhibitors containing a guanidine or amidine group. However, unlike previously described guanidino- or amidino-based inhibitors which have pK(a) values greater than 9.0, urokinase inhibitors containing a 2-aminobenzimidazole have pK(a) values of 7.5. Thus, 2-aminobenzimidazoles may have improved pharmacokinetic properties which could increase the bioavailability of inhibitors which contain this moiety. A crystal structure of one of the lead inhibitors, 2-amino-5-hydroxybenzimidazole, complexed with urokinase reveals the electrostatic and hydrophobic interactions that stabilize complex formation and suggests nearby subsites that may be accessed to increase the potency of this new series of urokinase inhibitors.
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{{ABSTRACT_PUBMED_11052791}}


==About this Structure==
==About this Structure==
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[[Category: Nienaber, V.]]
[[Category: Nienaber, V.]]
[[Category: Plasminogen activation]]
[[Category: Plasminogen activation]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 16:48:08 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 03:59:46 2008''

Revision as of 00:59, 1 July 2008

File:1fv9.png

Template:STRUCTURE 1fv9

Crystal structure of human microurokinase in complex with 2-amino-5-hydroxy-benzimidazole

Template:ABSTRACT PUBMED 11052791

About this Structure

1FV9 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Identification of novel inhibitors of urokinase via NMR-based screening., Hajduk PJ, Boyd S, Nettesheim D, Nienaber V, Severin J, Smith R, Davidson D, Rockway T, Fesik SW, J Med Chem. 2000 Oct 19;43(21):3862-6. PMID:11052791

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