2hfp
From Proteopedia
(New page: 200px<br /> <applet load="2hfp" size="450" color="white" frame="true" align="right" spinBox="true" caption="2hfp, resolution 2.000Å" /> '''Crystal Structure ...) |
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| - | [[Image:2hfp.gif|left|200px]]<br /> | + | [[Image:2hfp.gif|left|200px]]<br /><applet load="2hfp" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2hfp" size=" | + | |
caption="2hfp, resolution 2.000Å" /> | caption="2hfp, resolution 2.000Å" /> | ||
'''Crystal Structure of PPAR Gamma with N-sulfonyl-2-indole carboxamide ligands'''<br /> | '''Crystal Structure of PPAR Gamma with N-sulfonyl-2-indole carboxamide ligands'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The synthesis and structure-activity relationships of a novel series of | + | 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. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2HFP is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with NSI as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 2HFP is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=NSI:'>NSI</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HFP OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| - | [[Category: Evdokimov, A | + | [[Category: Evdokimov, A G.]] |
| - | [[Category: Hopkins, C | + | [[Category: Hopkins, C R.]] |
| - | [[Category: Mekel, M | + | [[Category: Mekel, M J.]] |
| - | [[Category: Pokross, M | + | [[Category: Pokross, M E.]] |
| - | [[Category: Walter, R | + | [[Category: Walter, R L.]] |
[[Category: NSI]] | [[Category: NSI]] | ||
[[Category: ppar ppargamma lbd]] | [[Category: ppar ppargamma lbd]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:41:21 2008'' |
Revision as of 15:41, 21 February 2008
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Crystal Structure of PPAR Gamma with N-sulfonyl-2-indole carboxamide ligands
Contents |
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.
Disease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[601487], Diabetes mellitus, insulin-resistant, with acanthosis nigricans and hypertension OMIM:[601487], Glioblastoma, susceptibility to OMIM:[601487], Insulin resistance, severe, digenic OMIM:[601487], Lipodystrophy, familial partial OMIM:[601487], Obesity, resistance to OMIM:[601487], Obesity, severe OMIM:[601487]
About this Structure
2HFP is a Protein complex structure of sequences from Homo sapiens with as ligand. 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
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