2j14: Difference between revisions

Revision as of 12:21, 30 October 2007

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

OverviewOverview

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 StructureAbout this Structure

2J14 is a [Single protein] structure of sequence from [Homo sapiens] with GNI as [ligand]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].

ReferenceReference

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 Tue Oct 30 11:26:42 2007

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

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 ==About this Structure==
-J14 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 GNI as [[http://en.wikipedia.org/wiki/ligand ligand]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2J14 OCA]].
+J14 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 GNI as [[http://en.wikipedia.org/wiki/ligand ligand]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2J14 OCA]].
 ==Reference==
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 [[Category: zinc-finger]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Oct 29 17:55:06 2007''
+''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 11:26:42 2007''