2hfp

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[[Image:2hfp.gif|left|200px]]
[[Image:2hfp.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2hfp |SIZE=350|CAPTION= <scene name='initialview01'>2hfp</scene>, resolution 2.000&Aring;
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The line below this paragraph, containing "STRUCTURE_2hfp", 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=NSI:3-(4-METHOXYPHENYL)-N-(PHENYLSULFONYL)-1-[3-(TRIFLUOROMETHYL)BENZYL]-1H-INDOLE-2-CARBOXAMIDE'>NSI</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_2hfp| PDB=2hfp | 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=2hfp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2hfp OCA], [http://www.ebi.ac.uk/pdbsum/2hfp PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2hfp RCSB]</span>
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}}
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'''Crystal Structure of PPAR Gamma with N-sulfonyl-2-indole carboxamide ligands'''
'''Crystal Structure of PPAR Gamma with N-sulfonyl-2-indole carboxamide ligands'''
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[[Category: Pokross, M E.]]
[[Category: Pokross, M E.]]
[[Category: Walter, R L.]]
[[Category: Walter, R L.]]
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[[Category: ppar ppargamma lbd]]
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[[Category: Ppar ppargamma lbd]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:14:10 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:29:42 2008''
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Revision as of 03:14, 4 May 2008

Image:2hfp.gif

Template:STRUCTURE 2hfp

Crystal Structure of PPAR Gamma with N-sulfonyl-2-indole carboxamide ligands


Overview

The synthesis and structure-activity relationships of a novel series of N-sulfonyl-2-indole carboxamides that bind to peroxisome proliferator-activated receptor gamma (PPAR-gamma) are reported. Chemical optimization of the series led to the identification of 4q (IC(50)=50 nM) as a potent binding agent of PPAR-gamma. Also reported is preliminary cell based data suggesting the use of these compounds in the treatment of osteoporosis.

About this Structure

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

Reference

Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-gamma binding agents with potential application to the treatment of osteoporosis., Hopkins CR, O'neil SV, Laufersweiler MC, Wang Y, Pokross M, Mekel M, Evdokimov A, Walter R, Kontoyianni M, Petrey ME, Sabatakos G, Roesgen JT, Richardson E, Demuth TP Jr, Bioorg Med Chem Lett. 2006 Nov 1;16(21):5659-63. Epub 2006 Aug 21. PMID:16919947 Page seeded by OCA on Sun May 4 06:14:10 2008

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OCA

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