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2j14

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{{STRUCTURE_2j14| PDB=2j14 | SCENE= }}
{{STRUCTURE_2j14| PDB=2j14 | SCENE= }}
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'''3,4,5-TRISUBSTITUTED ISOXAZOLES AS NOVEL PPARDELTA AGONISTS: PART2'''
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===3,4,5-TRISUBSTITUTED ISOXAZOLES AS NOVEL PPARDELTA AGONISTS: PART2===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 16931011 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16931011}}
==About this Structure==
==About this Structure==
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[[Category: Zinc]]
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[[Category: Zinc-finger]]
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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 Jul 28 02:34:05 2008''

Revision as of 23:34, 27 July 2008

Image:2j14.png

Template:STRUCTURE 2j14

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

Template:ABSTRACT PUBMED 16931011

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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