2NPA

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

Summary for 2NPA

• Entry DOI: 10.2210/pdb2npa/pdb
• Descriptor: Peroxisome proliferator-activated receptor alpha, SRC- peptide from Nuclear receptor coactivator 1, (2R,3E)-2-{4-[(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)METHOXY]BENZYL}-3-(PROPOXYIMINO)BUTANOIC ACID, ... (4 entities in total)
• Functional Keywords: protein-agonist complex, transcription
• Biological source: Homo sapiens (human); More
• Cellular location: Nucleus: Q07869
• Total number of polymer chains: 4
• Total formula weight: 65596.55

Authors

Kim, K.H.,Chung, H.K.,Han, H.O.,Kim, S.H.,Koh, J.S.,Kim, G.T. (deposition date: 2006-10-26, release date: 2007-10-30, Last modification date: 2023-10-25)

Primary citation

Han, H.O.,Kim, S.H.,Kim, K.H.,Hur, G.C.,Yim, H.J.,Chung, H.K.,Woo, S.H.,Koo, K.D.,Lee, C.S.,Koh, J.S.,Kim, G.T.
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists
Bioorg.Med.Chem.Lett., 17:937-941, 2007

PubMed Abstract: 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.

PubMed: 17157019
DOI: 10.1016/j.bmcl.2006.11.050

Experimental method

X-RAY DIFFRACTION (2.3 Å)