9OLC
Crystal structure of PPARg ligand-binding domain in complex with NCoR1 peptide and FTX-6746
This is a non-PDB format compatible entry.
Summary for 9OLC
| Entry DOI | 10.2210/pdb9olc/pdb |
| Descriptor | Peroxisome proliferator-activated receptor gamma, Nuclear receptor corepressor 1 peptide, (3P)-4-chloro-3-(5,7-difluoro-4-oxo-1,4-dihydroquinolin-2-yl)benzonitrile, ... (4 entities in total) |
| Functional Keywords | inverse agonist, transcription factor, small-molecule, covalent, transcription |
| Biological source | Homo sapiens (human) More |
| Total number of polymer chains | 8 |
| Total formula weight | 133788.41 |
| Authors | |
| Primary citation | Stuckey, J.I.,Mertz, J.A.,Wilson, J.E.,Williamson, K.E.,Li, Y.,Kuljanin, M.,Setser, J.W.,DeLaBarre, B.,Chenail, G.,Nguyen, P.A.,Bailey, C.M.,Motley, W.W.,Audia, J.E.,Sims 3rd, R.J. Discovery and characterization of FX-909, a covalent inverse agonist of PPARG rationally designed to impose a powerful repressive bias in PPARG for the treatment of PPARG/RXRA-activated muscle-invasive urothelial cancers To Be Published, |
| Experimental method | X-RAY DIFFRACTION (2.83 Å) |
Structure validation
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