2j14
From Proteopedia
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==Overview== | ==Overview== | ||
| - | A series of PPARdelta-selective agonists was investigated and optimized | + | 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== | ==About this Structure== | ||
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[[Category: Russo, R.]] | [[Category: Russo, R.]] | ||
[[Category: Saez, E.]] | [[Category: Saez, E.]] | ||
| - | [[Category: Seidel, H | + | [[Category: Seidel, H M.]] |
| - | [[Category: Tian, S | + | [[Category: Tian, S S.]] |
[[Category: Tuntland, T.]] | [[Category: Tuntland, T.]] | ||
[[Category: Wang, X.]] | [[Category: Wang, X.]] | ||
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[[Category: zinc-finger]] | [[Category: zinc-finger]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:58:12 2008'' |
Revision as of 15:58, 21 February 2008
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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 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 Thu Feb 21 17:58:12 2008
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
