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2viq

From Proteopedia

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[[Image:2viq.jpg|left|200px]]
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{{STRUCTURE_2viq| PDB=2viq | SCENE= }}
{{STRUCTURE_2viq| PDB=2viq | SCENE= }}
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'''FRAGMENT-BASED DISCOVERY OF MEXILETINE DERIVATIVES AS ORALLY BIOAVAILABLE INHIBITORS OF UROKINASE-TYPE PLASMINOGEN ACTIVATOR'''
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===FRAGMENT-BASED DISCOVERY OF MEXILETINE DERIVATIVES AS ORALLY BIOAVAILABLE INHIBITORS OF UROKINASE-TYPE PLASMINOGEN ACTIVATOR===
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==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.
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(as it appears on PubMed at http://www.pubmed.gov), where 18163548 is the PubMed ID number.
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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]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 18:53:36 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:55:28 2008''

Revision as of 13:55, 28 July 2008

Image:2viq.png

Template:STRUCTURE 2viq

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

Template:ABSTRACT PUBMED 18163548

About this Structure

2VIQ 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

Page seeded by OCA on Mon Jul 28 16:55:28 2008

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