The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
A peroxisome proliferator-activated receptor γ ligand inhibits adipocyte differentiation
Open accessAbstract
The peroxisome proliferator-activated receptors (PPARs) are nuclear hormone receptors that regulate glucose and lipid homeostasis. The PPARγ subtype plays a central role in the regulation of adipogenesis and is the molecular target for the 2,4-thiazolidinedione class of antidiabetic drugs. Structural studies have revealed that agonist ligands activate the PPARs through direct interactions with the C-terminal region of the ligand-binding domain, which includes the activation function 2 helix. GW0072 was identified as a high-affinity PPARγ ligand that was a weak partial agonist of PPARγ transactivation. X-ray crystallography revealed that GW0072 occupied the ligand-binding pocket by using different epitopes than the known PPAR agonists and did not interact with the activation function 2 helix. In cell culture, GW0072 was a potent antagonist of adipocyte differentiation. These results establish an approach to the design of PPAR ligands with modified biological activities.
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Cites
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Molecular recognition of fatty acids by peroxisome proliferator-activated receptors
Xu, H. E., Lambert, M. H., Montana, V. G., Parks, D. J., Blanchard, S. G., Brown, P. J., Sternbach, D. D., Lehmann, J. M., Wisely, G. B., Willson, T. M., et al. (1999) · Molecular Cell · doi:10.1016/s1097-2765(00)80467-0 · Cited by 1,169
Self-citationDiverse signaling pathways modulate nuclear receptor recruitment of N-CoR and SMRT complexes.
Lavinsky, R. M., Jepsen, K., Heinzel, T., Torchia, J., Mullen, T.-M., Schiff, R., Del-Rio, A. L., Ricote, M., Ngo, S., Gemsch, J., et al. (1998) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.95.6.2920 · Cited by 660
Cited by
The mechanisms of action of PPARs
Berger, J., & Moller, D. E. (2002) · Annual Review of Medicine · doi:10.1146/annurev.med.53.082901.104018 · Cited by 2,659
Transcriptional regulation of adipogenesis
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The PPARs: From Orphan Receptors to Drug Discovery
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Self-citationA SUMOylation-dependent pathway mediates transrepression of inflammatory response genes by PPAR-γ
Pascual, G., Fong, A. L., Ogawa, S., Gamliel, A., Li, A. C., Perissi, V., Rose, D. W., Willson, T. M., Rosenfeld, M. G., & Glass, C. K. (2005) · Nature · doi:10.1038/nature03988 · Cited by 1,254
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Metadata
- Authors
- Oberfield, J. L., Collins, J. L., Holmes, C. P., Goreham, D. M., Cooper, J. P., Cobb, J. E., Lenhard, J. M., Hull-Ryde, E. A., Mohr, C. P., Blanchard, S. G., Parks, D. J., Moore, L. B., Lehmann, J. M., Plunket, K., Miller, A. B., Milburn, M. V., Kliewer, S. A., & Willson, T. M.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1999-05-25
- Volume
- 96
- Issue
- 11
- Pages
- 6102-6106
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W1527827101
- Cited by
- 316
- References
- 5
- FWCI
- 9.46
- Type
- journal article
- Language
- en
- Open access
- green
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- Oberfield, J. L., Collins, J. L., Holmes, C. P., Goreham, D. M., Cooper, J. P., Cobb, J. E., Lenhard, J. M., Hull-Ryde, E. A., Mohr, C. P., Blanchard, S. G., Parks, D. J., Moore, L. B., Lehmann, J. M., Plunket, K., Miller, A. B., Milburn, M. V., Kliewer, S. A., & Willson, T. M. (1999). A peroxisome proliferator-activated receptor γ ligand inhibits adipocyte differentiation. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.96.11.6102
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
