Identification of a unique PPAR ligand with an unexpected binding mode and antibetic activity

Summary for 4FGY

DescriptorPeroxisome proliferator-activated receptor gamma, Nuclear receptor coactivator 1, (4R,6S,8S,12R,14R,16Z,18R,19R,20S,21S)-19,21-dihydroxy-22-{(2S,2'R,5S,5'S)-5'-[(1R)-1-hydroxyethyl]-2,5'-dimethyloctahydro-2,2'-bifuran-5-yl}-4,6,8,12,14,18,20-heptamethyl-9,11-dioxodocos-16-enoic acid, ... (4 entities in total)
Functional Keywordsppar lbd, nuclear receptor fold, ligand binding, gene transcription, transcription-transferase-antibiotic complex, transcription/transferase/antibiotic
Biological sourceHomo sapiens (human)
Cellular locationNucleus P37231 Q15788
Total number of polymer chains2
Total molecular weight32990.6
Wang, R.,Li, Y. (deposition date: 2012-06-05, release date: 2013-03-20, Last modification date: 2018-05-02)
Primary citation
Zheng, W.,Feng, X.,Qiu, L.,Pan, Z.,Wang, R.,Lin, S.,Hou, D.,Jin, L.,Li, Y.
Identification of the antibiotic ionomycin as an unexpected peroxisome proliferator-activated receptor Gamma (PPAR-gamma) ligand with a unique binding mode and effective glucose-lowering activity in a mouse model of diabetes.
Diabetologia, 56:401-411, 2013
PubMed: 23178929 (PDB entries with the same primary citation)
DOI: 10.1007/s00125-012-2777-9
MImport into Mendeley
Experimental method

Structure validation

RfreeClashscoreRamachandran outliersSidechain outliersRSRZ outliers0.285333.7%18.1%2.2%MetricValuePercentile RanksWorseBetterPercentile relative to all X-ray structuresPercentile relative to X-ray structures of similar resolution
Download full validation report