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2gtk

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[[Image:2gtk.gif|left|200px]]
[[Image:2gtk.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2gtk |SIZE=350|CAPTION= <scene name='initialview01'>2gtk</scene>, resolution 2.10&Aring;
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The line below this paragraph, containing "STRUCTURE_2gtk", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=208:(2S)-3-(1-{[2-(2-CHLOROPHENYL)-5-METHYL-1,3-OXAZOL-4-YL]METHYL}-1H-INDOL-5-YL)-2-ETHOXYPROPANOIC+ACID'>208</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE= PPARG, NR1C3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2gtk| PDB=2gtk | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2gtk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2gtk OCA], [http://www.ebi.ac.uk/pdbsum/2gtk PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2gtk RCSB]</span>
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}}
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'''Structure-based Design of Indole Propionic Acids as Novel PPARag CO-Agonists'''
'''Structure-based Design of Indole Propionic Acids as Novel PPARag CO-Agonists'''
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[[Category: Meyer, M.]]
[[Category: Meyer, M.]]
[[Category: Mohr, P.]]
[[Category: Mohr, P.]]
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[[Category: nuclear receptor]]
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[[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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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:21:24 2008''
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Revision as of 02:31, 4 May 2008

Image:2gtk.gif

Template:STRUCTURE 2gtk

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


Overview

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.

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 Sun May 4 05:31:08 2008

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