2vin: Difference between revisions

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[[Image:2vin.jpg|left|200px]]
{{Seed}}
[[Image:2vin.png|left|200px]]


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{{STRUCTURE_2vin|  PDB=2vin  |  SCENE=  }}  
{{STRUCTURE_2vin|  PDB=2vin  |  SCENE=  }}  


'''FRAGMENT-BASED DISCOVERY OF MEXILETINE DERIVATIVES AS ORALLY BIOAVAILABLE INHIBITORS OF UROKINASE-TYPE PLASMINOGEN ACTIVATOR'''
===FRAGMENT-BASED DISCOVERY OF MEXILETINE DERIVATIVES AS ORALLY BIOAVAILABLE INHIBITORS OF UROKINASE-TYPE PLASMINOGEN ACTIVATOR===




==Overview==
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Fragment-based lead discovery has been applied to urokinase-type plasminogen activator (uPA). The (R)-enantiomer of the orally active drug mexiletine 5 (a fragment hit from X-ray crystallographic screening) was the chemical starting point. Structure-aided design led to elaborated inhibitors that retained the key interactions of (R)-5 while gaining extra potency by simultaneously occupying neighboring regions of the active site. Subsequent optimization led to 15, a potent, selective, and orally bioavailable inhibitor of uPA.
The line below this paragraph, {{ABSTRACT_PUBMED_18163548}}, adds the Publication Abstract to the page
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{{ABSTRACT_PUBMED_18163548}}


==About this Structure==
==About this Structure==
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[[Category: Urokinase-type plasminogen activator]]
[[Category: Urokinase-type plasminogen activator]]
[[Category: Zymogen]]
[[Category: Zymogen]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 18:52:47 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 09:18:50 2008''

Revision as of 06:18, 28 July 2008

File:2vin.png

Template:STRUCTURE 2vin

FRAGMENT-BASED DISCOVERY OF MEXILETINE DERIVATIVES AS ORALLY BIOAVAILABLE INHIBITORS OF UROKINASE-TYPE PLASMINOGEN ACTIVATOR

Template:ABSTRACT PUBMED 18163548

About this Structure

2VIN is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator., Frederickson M, Callaghan O, Chessari G, Congreve M, Cowan SR, Matthews JE, McMenamin R, Smith DM, Vinkovic M, Wallis NG, J Med Chem. 2008 Jan 24;51(2):183-6. Epub 2007 Dec 29. PMID:18163548

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