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Ligands
Code Name Style Show Link
9RA 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl]benzoic acid
D30 [(4-{[2-(pent-2-yn-1-yloxy)-4-{[4-(trifluoromethyl)phenoxy]methyl}phenyl]sulfanyl}-5,6,7,8-tetrahydronaphthalen-1-yl)oxy]acetic acid
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Glycosylation
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Code : 3H0A   PDBj   RCSB PDB   PDBe
Header : TRANSCRIPTION
Title : Crystal Structure of Peroxisome Proliferator-Activated Receptor Gamma (PPARg) and Retinoic Acid Receptor Alpha (RXRa) in Complex with 9-cis Retinoic Acid, Co-activator Peptide, and a Partial Agonist
Release Data : 2009-06-09
Compound :
mol_id molecule chains synonym
1 Retinoic acid receptor RXR-alpha A Retinoid X receptor alpha, Nuclear receptor subfamily 2 group B member 1
fragment: UNP RESIDUES 228-455
mol_id molecule chains synonym
2 Peroxisome proliferator-activated receptor gamma D PPAR-gamma, Nuclear receptor subfamily 1 group C member 3
fragment: UNP RESIDUES 234-505
mol_id molecule chains synonym
3 Nuclear receptor coactivator 1, Co-activator Peptide B,E NCoA-1, Steroid receptor coactivator 1, SRC-1, RIP160, Protein Hin-2, Renal carcinoma antigen NY-REN-52
ec: 2.3.1.48
fragment: UNP RESIDUES 629-640
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
gene: RXRA, NR2B1
expression_system_strain: BL21(DE3)
expression_system_vector_type: plasmid
expression_system_plasmid: pET30
mol_id organism_scientific organism_common expression_system
2 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
gene: PPARG, NR1C3
expression_system_strain: BL21(DE3)
expression_system_vector_type: plasmid
expression_system_plasmid: pET30
mol_id organism_scientific organism_common
3 Homo sapiens  (taxid:9606) Human
synthetic: yes
Authors : Wang, Z., Sudom, A., Walker, N.P.
Keywords : PPAR, transcription, nuclear receptor fold, transcription regulation, hormone, growth factor receptor, complex, DNA-binding, Host-virus interaction, Isopeptide bond, Metal-binding, Nucleus, Receptor, Zinc-finger, Activator, Diabetes mellitus, Disease mutation, Obesity, Phosphoprotein, Acyltransferase, Proto-oncogene, Transferase
Exp. method : X-RAY DIFFRACTION ( 2.10 Å )
Citation :

Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.

Connors, R.V.,Wang, Z.,Harrison, M.  et al.
(2009)  Bioorg.Med.Chem.Lett.  19 : 3550 - 3554

PubMed: 19464171
DOI: 10.1016/j.bmcl.2009.04.151

Chain : A
UniProt : P19793 (RXRA_HUMAN)
Reaction : -
Chain : D
UniProt : P37231 (PPARG_HUMAN)
Reaction : -
Chain : B, E
UniProt : Q15788 (NCOA1_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
acetyl-CoA + L-lysyl-[protein] = CoA + H(+) + N(6)-acetyl-L- lysyl-[protein] 2.3.1.48 -
-