1KKQ

Crystal structure of the human PPAR-alpha ligand-binding domain in complex with an antagonist GW6471 and a SMRT corepressor motif

Summary for 1KKQ

• Entry DOI: 10.2210/pdb1kkq/pdb
• Related: 1k74 1k7L
• Descriptor: PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR, NUCLEAR RECEPTOR CO-REPRESSOR 2, N-((2S)-2-({(1Z)-1-METHYL-3-OXO-3-[4-(TRIFLUOROMETHYL) PHENYL]PROP-1-ENYL}AMINO)-3-{4-[2-(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)ETHOXY]PHENYL}PROPYL)PROPANAMIDE, ... (4 entities in total)
• Functional Keywords: nuclear corepressor nuclear hormone receptors antagonist, transcription
• Biological source: Homo sapiens (human); More
• Cellular location: Nucleus: Q07869 Q9Y618
• Total number of polymer chains: 8
• Total formula weight: 133211.69

Authors

Xu, H.E.,Stanley, T.B.,Montana, V.G.,Lambert, M.H.,Shearer, B.G.,Cobb, J.E.,McKee, D.D.,Galardi, C.M.,Nolte, R.T.,Parks, D.J. (deposition date: 2001-12-10, release date: 2002-02-20, Last modification date: 2023-08-16)

• Primary citation: Xu, H.E.,Stanley, T.B.,Montana, V.G.,Lambert, M.H.,Shearer, B.G.,Cobb, J.E.,McKee, D.D.,Galardi, C.M.,Plunket, K.D.,Nolte, R.T.,Parks, D.J.,Moore, J.T.,Kliewer, S.A.,Willson, T.M.,Stimmel, J.B.; Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha.; Nature, 415:813-817, 2002; PubMed: 11845213

Experimental method

X-RAY DIFFRACTION (3 Å)