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2gtk

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{{STRUCTURE_2gtk| PDB=2gtk | SCENE= }}
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'''Structure-based Design of Indole Propionic Acids as Novel PPARag CO-Agonists'''
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===Structure-based Design of Indole Propionic Acids as Novel PPARag CO-Agonists===
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==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.
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(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]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:31:08 2008''
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Revision as of 06:16, 28 July 2008

Image:2gtk.png

Template:STRUCTURE 2gtk

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

Template:ABSTRACT PUBMED 16737814

About this Structure

2GTK is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure-based design of indole propionic acids as novel PPARalpha/gamma co-agonists., Kuhn B, Hilpert H, Benz J, Binggeli A, Grether U, Humm R, Marki HP, Meyer M, Mohr P, Bioorg Med Chem Lett. 2006 Aug 1;16(15):4016-20. Epub 2006 Jun 5. PMID:16737814

Page seeded by OCA on Mon Jul 28 09:16:10 2008

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