2j14
From Proteopedia
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| - | [[Image:2j14.gif|left|200px]]<br /> | + | [[Image:2j14.gif|left|200px]]<br /><applet load="2j14" size="450" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2j14" size="450" color="white" frame="true" align="right" spinBox="true" | + | |
caption="2j14, resolution 2.80Å" /> | caption="2j14, resolution 2.80Å" /> | ||
'''3,4,5-TRISUBSTITUTED ISOXAZOLES AS NOVEL PPARDELTA AGONISTS: PART2'''<br /> | '''3,4,5-TRISUBSTITUTED ISOXAZOLES AS NOVEL PPARDELTA AGONISTS: PART2'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 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 GNI as [http://en.wikipedia.org/wiki/ligand ligand]. | + | 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 GNI 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://ispc.weizmann.ac.il/oca-bin/ocashort?id=2J14 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: zinc-finger]] | [[Category: zinc-finger]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Dec 18 19:43:44 2007'' |
Revision as of 17:33, 18 December 2007
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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 with GNI as ligand. Known structural/functional Site: . 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 Tue Dec 18 19:43:44 2007
Categories: Homo sapiens | Single protein | Azimioara, M. | Bursulaya, B. | Cow, C. | Epple, R. | Gerken, A. | Iskandar, M. | Karanewsky, D. | Kreusch, A. | Russo, R. | Saez, E. | Seidel, H.M. | Tian, S.S. | Tuntland, T. | Wang, X. | Wityak, J. | Xie, Y. | GNI | Activator | Alternative splicing | Dna-binding | Fatty acids | Metal-binding | Nuclear protein | Nuclear receptor fold | Ppar | Receptor | Transcription | Transcription regulation | Zinc | Zinc-finger
