2vip: Difference between revisions

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


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{{STRUCTURE_2vip|  PDB=2vip  |  SCENE=  }}  
{{STRUCTURE_2vip|  PDB=2vip  |  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
(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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