2gtk: Difference between revisions

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Bots, Bureaucrats, journal, Administrators
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OCA (talk | contribs)
Bots, Bureaucrats, journal, Administrators
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No edit summary
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[[Image:2gtk.gif|left|200px]]
{{Seed}}
[[Image:2gtk.png|left|200px]]


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{{STRUCTURE_2gtk|  PDB=2gtk  |  SCENE=  }}  
{{STRUCTURE_2gtk|  PDB=2gtk  |  SCENE=  }}  


'''Structure-based Design of Indole Propionic Acids as Novel PPARag CO-Agonists'''
===Structure-based Design of Indole Propionic Acids as Novel PPARag CO-Agonists===




==Overview==
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In the quest for novel PPARalpha/gamma co-agonists as putative drugs for the treatment of type 2 diabetes and dyslipidemia, we have used a structure-based design approach to identify propionic acids with a 1,5-disubstituted indole scaffold as potent PPARalpha/gamma activators. Compounds 13, 24, and 28 are examples of submicromolar dual agonists with different alpha/gamma EC50 ratios that are selective against the delta-isoform. Analysis of the X-ray complex structure of PPARgamma with the indole propionic acid 13 provides a rationalization for some of the observed SAR.
The line below this paragraph, {{ABSTRACT_PUBMED_16737814}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 16737814 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16737814}}


==About this Structure==
==About this Structure==
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[[Category: Mohr, P.]]
[[Category: Mohr, P.]]
[[Category: Nuclear receptor]]
[[Category: Nuclear receptor]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 05:31:08 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 09:16:10 2008''
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