2j14
From Proteopedia
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 Page seeded by OCA on Sun May 4 08:11:57 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. | Activator | Alternative splicing | Dna-binding | Fatty acid | Metal-binding | Nuclear protein | Nuclear receptor fold | Ppar | Receptor | Transcription | Transcription regulation | Zinc | Zinc-finger
