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1k74
From Proteopedia
| 1k74, resolution 2.30Å () | |||||||||
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| Sites: | and | ||||||||
| Ligands: | , | ||||||||
| Related: | 1fm6, 1fm9, 1k7l | ||||||||
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
The 2.3 Angstrom resolution crystal structure of the heterodimer of the human PPARgamma and RXRalpha ligand binding domains respectively bound with GW409544 and 9-cis retinoic acid and co-activator peptides.
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.
Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors., Xu HE, Lambert MH, Montana VG, Plunket KD, Moore LB, Collins JL, Oplinger JA, Kliewer SA, Gampe RT Jr, McKee DD, Moore JT, Willson TM, Proc Natl Acad Sci U S A. 2001 Nov 20;98(24):13919-24. Epub 2001 Nov 6. PMID:11698662
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
1K74 is a 4 chains structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.
See PPAR for additional structural information.
Reference
- Xu HE, Lambert MH, Montana VG, Plunket KD, Moore LB, Collins JL, Oplinger JA, Kliewer SA, Gampe RT Jr, McKee DD, Moore JT, Willson TM. Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors. Proc Natl Acad Sci U S A. 2001 Nov 20;98(24):13919-24. Epub 2001 Nov 6. PMID:11698662 doi:10.1073/pnas.241410198
Page seeded by OCA on Wed Feb 18 08:36:04 2009
Categories: Homo sapiens | Collins, J L. | Jr., R T.Gampe. | Kliewer, S A. | Lambert, M H. | McKee, D D. | Montana, V G. | Moore, J T. | Moore, L B. | Oplinger, J A. | Willson, T M. | Xu, H E. | The heterodimer of the nuclear receptor ligand binding domains of rxralpha and ppargamma bound respectively with 9-cis retinoic acid and gw409544 and coactivator peptide
