The DOI matches its Crossref record; 32 of the 32 references it cites were found in a registry or an index.
Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors
Open accessAbstract
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 PPARα (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 PPARα and histidine in PPARγ, 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.
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Cites
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Self-citationActivation of a member of the steroid hormone receptor superfamily by peroxisome proliferators
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Cited by
Pawlak, M., Lefebvre, P., & Staels, B. (2015) · Journal of Hepatology · doi:10.1016/j.jhep.2014.10.039 · Cited by 1,578
Peroxisome Proliferator-Activated Receptor Alpha Target Genes
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Molecular Actions of PPARα in Lipid Metabolism and Inflammation
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Metadata
- Authors
- 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, R. T., McKee, D. D., Moore, J. T., & Willson, T. M.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2001-11-06
- Volume
- 98
- Issue
- 24
- Pages
- 13919-13924
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2165610631
- Cited by
- 538
- References
- 32
- FWCI
- 7.49
- Type
- journal article
- Language
- en
- Open access
- green
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