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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 DOI10.2210/pdb1k7l/pdb
Related1fm6 1fm9 1k74
DescriptorPeroxisome 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 Keywordsthe 2.5 angstrom resolution crystal structure of the human pparalpha ligand binding domain bound with gw409544 and a coactivator peptide, transcription
Biological sourceHomo sapiens (human)
More
Cellular locationNucleus: Q07869
Total number of polymer chains8
Total formula weight142871.19
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 citationXu, 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: 11698662
DOI: 10.1073/pnas.241410198
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.5 Å)
Structure validation

226707

數據於2024-10-30公開中

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