2j14

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[[Image:2j14.gif|left|200px]]
[[Image:2j14.gif|left|200px]]
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{{Structure
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|PDB= 2j14 |SIZE=350|CAPTION= <scene name='initialview01'>2j14</scene>, resolution 2.80&Aring;
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The line below this paragraph, containing "STRUCTURE_2j14", creates the "Structure Box" on the page.
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|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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{{STRUCTURE_2j14| PDB=2j14 | SCENE= }}
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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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'''3,4,5-TRISUBSTITUTED ISOXAZOLES AS NOVEL PPARDELTA AGONISTS: PART2'''
'''3,4,5-TRISUBSTITUTED ISOXAZOLES AS NOVEL PPARDELTA AGONISTS: PART2'''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 08:11:57 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:51:37 2008''
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Revision as of 05:11, 4 May 2008

Image:2j14.gif

Template:STRUCTURE 2j14

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 Page seeded by OCA on Sun May 4 08:11:57 2008

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OCA

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