2npa
From Proteopedia
(New page: 200px<br /> <applet load="2npa" size="450" color="white" frame="true" align="right" spinBox="true" caption="2npa, resolution 2.300Å" /> '''the crystal struct...) |
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| - | [[Image:2npa.gif|left|200px]]<br /> | + | [[Image:2npa.gif|left|200px]]<br /><applet load="2npa" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2npa" size=" | + | |
caption="2npa, resolution 2.300Å" /> | caption="2npa, resolution 2.300Å" /> | ||
'''the crystal structure of the human PPARaplpha ligand binding domain in complex with a a-hydroxyimino phenylpropanoic acid'''<br /> | '''the crystal structure of the human PPARaplpha ligand binding domain in complex with a a-hydroxyimino phenylpropanoic acid'''<br /> | ||
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==Overview== | ==Overview== | ||
Oxime ethers of alpha-acyl-beta-phenylpropanoic acids were prepared to, apply as PPARalpha and gamma dual agonists. Among them, compound 11l, proved to exhibit potent in vitro activities with EC(50) of 19 and 13nM in, PPARalpha and gamma, respectively. It showed better glucose lowering, effects than rosiglitazone 1 and ameliorated the lipid profile like plasma, triglyceride in db/db mice model. | Oxime ethers of alpha-acyl-beta-phenylpropanoic acids were prepared to, apply as PPARalpha and gamma dual agonists. Among them, compound 11l, proved to exhibit potent in vitro activities with EC(50) of 19 and 13nM in, PPARalpha and gamma, respectively. It showed better glucose lowering, effects than rosiglitazone 1 and ameliorated the lipid profile like plasma, triglyceride in db/db mice model. | ||
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| - | ==Disease== | ||
| - | Known diseases associated with this structure: Hyperapobetalipoproteinemia, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=170998 170998]] | ||
==About this Structure== | ==About this Structure== | ||
| - | 2NPA is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with MMB as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 2NPA is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=MMB:'>MMB</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2NPA OCA]. |
==Reference== | ==Reference== | ||
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[[Category: transcription]] | [[Category: transcription]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:36:15 2008'' |
Revision as of 10:36, 23 January 2008
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the crystal structure of the human PPARaplpha ligand binding domain in complex with a a-hydroxyimino phenylpropanoic acid
Overview
Oxime ethers of alpha-acyl-beta-phenylpropanoic acids were prepared to, apply as PPARalpha and gamma dual agonists. Among them, compound 11l, proved to exhibit potent in vitro activities with EC(50) of 19 and 13nM in, PPARalpha and gamma, respectively. It showed better glucose lowering, effects than rosiglitazone 1 and ameliorated the lipid profile like plasma, triglyceride in db/db mice model.
About this Structure
2NPA is a Protein complex structure of sequences from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
Reference
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists., Oon Han H, Kim SH, Kim KH, Hur GC, Joo Yim H, Chung HK, Ho Woo S, Dong Koo K, Lee CS, Sung Koh J, Kim GT, Bioorg Med Chem Lett. 2007 Feb 15;17(4):937-41. Epub 2006 Nov 18. PMID:17157019
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