2npa
From Proteopedia
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|PDB= 2npa |SIZE=350|CAPTION= <scene name='initialview01'>2npa</scene>, resolution 2.300Å | |PDB= 2npa |SIZE=350|CAPTION= <scene name='initialview01'>2npa</scene>, resolution 2.300Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= <scene name='pdbligand=MMB:(2R,3E)-2-{4-[(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)METHOXY]BENZYL}-3-(PROPOXYIMINO)BUTANOIC ACID'>MMB</scene> | + | |LIGAND= <scene name='pdbligand=MMB:(2R,3E)-2-{4-[(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)METHOXY]BENZYL}-3-(PROPOXYIMINO)BUTANOIC+ACID'>MMB</scene> |
|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2npa FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2npa OCA], [http://www.ebi.ac.uk/pdbsum/2npa PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2npa RCSB]</span> | ||
}} | }} | ||
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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. | ||
| - | |||
| - | ==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== | ||
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[[Category: Kim, S H.]] | [[Category: Kim, S H.]] | ||
[[Category: Koh, J S.]] | [[Category: Koh, J S.]] | ||
| - | [[Category: MMB]] | ||
[[Category: protein-agonist complex]] | [[Category: protein-agonist complex]] | ||
[[Category: transcription]] | [[Category: transcription]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:06:20 2008'' |
Revision as of 01:06, 31 March 2008
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| , resolution 2.300Å | |||||||
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| Ligands: | |||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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. 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
Page seeded by OCA on Mon Mar 31 04:06:20 2008
