2j14

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|PDB= 2j14 |SIZE=350|CAPTION= <scene name='initialview01'>2j14</scene>, resolution 2.80&Aring;
|PDB= 2j14 |SIZE=350|CAPTION= <scene name='initialview01'>2j14</scene>, resolution 2.80&Aring;
|SITE= <scene name='pdbsite=AC1:Gni+Binding+Site+For+Chain+B'>AC1</scene>
|SITE= <scene name='pdbsite=AC1:Gni+Binding+Site+For+Chain+B'>AC1</scene>
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|LIGAND= <scene name='pdbligand=GNI:(3-{4-[2-(2,4-DICHLORO-PHENOXY)-ETHYLCARBAMOYL]-5-PHENYL-ISOXAZOL-3-YL}-PHENYL)-ACETIC ACID'>GNI</scene>
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|LIGAND= <scene name='pdbligand=GNI:(3-{4-[2-(2,4-DICHLORO-PHENOXY)-ETHYLCARBAMOYL]-5-PHENYL-ISOXAZOL-3-YL}-PHENYL)-ACETIC+ACID'>GNI</scene>
|ACTIVITY=
|ACTIVITY=
|GENE=
|GENE=
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|DOMAIN=
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2j14 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2j14 OCA], [http://www.ebi.ac.uk/pdbsum/2j14 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2j14 RCSB]</span>
}}
}}
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[[Category: Wityak, J.]]
[[Category: Wityak, J.]]
[[Category: Xie, Y.]]
[[Category: Xie, Y.]]
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[[Category: GNI]]
 
[[Category: activator]]
[[Category: activator]]
[[Category: alternative splicing]]
[[Category: alternative splicing]]
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[[Category: zinc-finger]]
[[Category: zinc-finger]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:36:04 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:51:37 2008''

Revision as of 00:51, 31 March 2008

Image:2j14.gif


PDB ID 2j14

Drag the structure with the mouse to rotate
, resolution 2.80Å
Sites:
Ligands:
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



3,4,5-TRISUBSTITUTED ISOXAZOLES AS NOVEL PPARDELTA AGONISTS: PART2


Overview

A series of PPARdelta-selective agonists was investigated and optimized for a favorable in vivo pharmacokinetic profile. Isoxazole LCI765 (17d) was found to be a potent and selective PPARdelta agonist with good in vivo PK properties in mouse (C(max)=5.1 microM, t(1/2)=3.1 h). LCI765 regulated expression of genes involved in energy homeostasis in relevant tissues when dosed orally in C57BL6 mice. A co-crystal structure of compound LCI765 and the LBD of PPARdelta is discussed.

About this Structure

2J14 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2., Epple R, Azimioara M, Russo R, Xie Y, Wang X, Cow C, Wityak J, Karanewsky D, Bursulaya B, Kreusch A, Tuntland T, Gerken A, Iskandar M, Saez E, Martin Seidel H, Tian SS, Bioorg Med Chem Lett. 2006 Nov 1;16(21):5488-92. Epub 2006 Aug 22. PMID:16931011

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