2pob
From Proteopedia
(New page: 200px {{Structure |PDB= 2pob |SIZE=350|CAPTION= <scene name='initialview01'>2pob</scene>, resolution 2.30Å |SITE= <scene name='pdbsite=AC1:Gw4+Binding+Site+...) |
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|PDB= 2pob |SIZE=350|CAPTION= <scene name='initialview01'>2pob</scene>, resolution 2.30Å | |PDB= 2pob |SIZE=350|CAPTION= <scene name='initialview01'>2pob</scene>, resolution 2.30Å | ||
|SITE= <scene name='pdbsite=AC1:Gw4+Binding+Site+For+Residue+A+478'>AC1</scene> and <scene name='pdbsite=AC2:Gol+Binding+Site+For+Residue+B+478'>AC2</scene> | |SITE= <scene name='pdbsite=AC1:Gw4+Binding+Site+For+Residue+A+478'>AC1</scene> and <scene name='pdbsite=AC2:Gol+Binding+Site+For+Residue+B+478'>AC2</scene> | ||
| - | |LIGAND= <scene name='pdbligand= | + | |LIGAND= <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=GW4:N-[(2S)-2-[(2-BENZOYLPHENYL)AMINO]-3-{4-[2-(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)ETHOXY]PHENYL}PROPYL]ACETAMIDE'>GW4</scene> |
|ACTIVITY= | |ACTIVITY= | ||
|GENE= PPARG, NR1C3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= PPARG, NR1C3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2pob FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2pob OCA], [http://www.ebi.ac.uk/pdbsum/2pob PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2pob RCSB]</span> | ||
}} | }} | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Nolte, R T.]] | [[Category: Nolte, R T.]] | ||
| - | [[Category: GOL]] | ||
| - | [[Category: GW4]] | ||
[[Category: gene regulation]] | [[Category: gene regulation]] | ||
[[Category: nuclear receptor,ppar]] | [[Category: nuclear receptor,ppar]] | ||
[[Category: pparg]] | [[Category: pparg]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:38:38 2008'' |
Revision as of 01:38, 31 March 2008
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| , resolution 2.30Å | |||||||
|---|---|---|---|---|---|---|---|
| Sites: | and | ||||||
| Ligands: | , | ||||||
| Gene: | PPARG, NR1C3 (Homo sapiens) | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
PPARgamma Ligand binding domain complexed with a farglitazar analogue gw4709
Overview
PPARgamma-activating thiazolidinediones and carboxylic acids such as farglitazar exert their anti-diabetic effects in part in PPARgamma rich adipose. Both pro- and anti-adipogenic PPARgamma ligands promote glucose and lipid lowering in animal models of diabetes. Herein, we disclose representatives of an array of 160 farglitazar analogues with atypical inverse agonism of PPARgamma in mature adipocytes.
About this Structure
2POB is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Co-crystal structure guided array synthesis of PPARgamma inverse agonists., Trump RP, Cobb JE, Shearer BG, Lambert MH, Nolte RT, Willson TM, Buckholz RG, Zhao SM, Leesnitzer LM, Iannone MA, Pearce KH, Billin AN, Hoekstra WJ, Bioorg Med Chem Lett. 2007 Jul 15;17(14):3916-20. Epub 2007 May 18. PMID:17533125
Page seeded by OCA on Mon Mar 31 04:38:38 2008
