2j14

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[[Image:2j14.gif|left|200px]]<br /><applet load="2j14" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2j14.gif|left|200px]]
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caption="2j14, resolution 2.80&Aring;" />
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'''3,4,5-TRISUBSTITUTED ISOXAZOLES AS NOVEL PPARDELTA AGONISTS: PART2'''<br />
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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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|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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|ACTIVITY=
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|GENE=
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}}
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'''3,4,5-TRISUBSTITUTED ISOXAZOLES AS NOVEL PPARDELTA AGONISTS: PART2'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2J14 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=GNI:'>GNI</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:Gni+Binding+Site+For+Chain+B'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2J14 OCA].
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2J14 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2J14 OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16931011 16931011]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/16931011 16931011]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: alternative splicing]]
[[Category: alternative splicing]]
[[Category: dna-binding]]
[[Category: dna-binding]]
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[[Category: fatty acids]]
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[[Category: fatty acid]]
[[Category: metal-binding]]
[[Category: metal-binding]]
[[Category: nuclear protein]]
[[Category: nuclear protein]]
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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 Feb 21 17:58:12 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:36:04 2008''

Revision as of 15:36, 20 March 2008

Image:2j14.gif


PDB ID 2j14

Drag the structure with the mouse to rotate
, resolution 2.80Å
Sites:
Ligands:
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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