2npa

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==Overview==
==Overview==
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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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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==
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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: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Protein complex]]
[[Category: Protein complex]]
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[[Category: Chung, H.K.]]
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[[Category: Chung, H K.]]
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[[Category: Han, H.O.]]
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[[Category: Han, H O.]]
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[[Category: Kim, G.T.]]
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[[Category: Kim, G T.]]
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[[Category: Kim, K.H.]]
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[[Category: Kim, K H.]]
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[[Category: Kim, S.H.]]
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[[Category: Kim, S H.]]
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[[Category: Koh, J.S.]]
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[[Category: Koh, J S.]]
[[Category: MMB]]
[[Category: MMB]]
[[Category: protein-agonist complex]]
[[Category: protein-agonist complex]]
[[Category: transcription]]
[[Category: transcription]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:36:15 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:09:21 2008''

Revision as of 16:09, 21 February 2008


2npa, resolution 2.300Å

Drag the structure with the mouse to rotate

the crystal structure of the human PPARaplpha ligand binding domain in complex with a a-hydroxyimino phenylpropanoic acid

Contents

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.

Disease

Known diseases associated with this structure: Hyperapobetalipoproteinemia, susceptibility to OMIM:[170998]

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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