1K7L
The 2.5 Angstrom resolution crystal structure of the human PPARalpha ligand binding domain bound with GW409544 and a co-activator peptide.
Summary for 1K7L
Entry DOI | 10.2210/pdb1k7l/pdb |
Related | 1fm6 1fm9 1k74 |
Descriptor | Peroxisome proliferator activated receptor alpha, steroid receptor coactivator, 2-(1-METHYL-3-OXO-3-PHENYL-PROPYLAMINO)-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-PHENYL}-PROPIONIC ACID, ... (5 entities in total) |
Functional Keywords | the 2.5 angstrom resolution crystal structure of the human pparalpha ligand binding domain bound with gw409544 and a coactivator peptide, transcription |
Biological source | Homo sapiens (human) More |
Cellular location | Nucleus: Q07869 |
Total number of polymer chains | 8 |
Total formula weight | 142871.19 |
Authors | Xu, H.E.,Lambert, M.H.,Montana, V.G.,Moore, L.B.,Collins, J.L.,Oplinger, J.A.,Kliewer, S.A.,Gampe Jr., R.T.,McKee, D.D.,Moore, J.T.,Willson, T.M. (deposition date: 2001-10-19, release date: 2001-12-05, Last modification date: 2024-02-07) |
Primary citation | Xu, H.E.,Lambert, M.H.,Montana, V.G.,Plunket, K.D.,Moore, L.B.,Collins, J.L.,Oplinger, J.A.,Kliewer, S.A.,Gampe Jr., R.T.,McKee, D.D.,Moore, J.T.,Willson, T.M. Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors. Proc.Natl.Acad.Sci.USA, 98:13919-13924, 2001 Cited by PubMed Abstract: The peroxisome proliferator-activated receptors (PPARs) are transcriptional regulators of glucose, lipid, and cholesterol metabolism. We report the x-ray crystal structure of the ligand binding domain of PPAR alpha (NR1C1) as a complex with the agonist ligand GW409544 and a coactivator motif from the steroid receptor coactivator 1. Through comparison of the crystal structures of the ligand binding domains of the three human PPARs, we have identified molecular determinants of subtype selectivity. A single amino acid, which is tyrosine in PPAR alpha and histidine in PPAR gamma, imparts subtype selectivity for both thiazolidinedione and nonthiazolidinedione ligands. The availability of high-resolution cocrystal structures of the three PPAR subtypes will aid the design of drugs for the treatments of metabolic and cardiovascular diseases. PubMed: 11698662DOI: 10.1073/pnas.241410198 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.5 Å) |
Structure validation
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