The DOI matches its Crossref record; 14 of the 14 references it cites were found in a registry or an index.
Identification of a Nonsteroidal Liver X Receptor Agonist through Parallel Array Synthesis of Tertiary Amines
Open accessAbstract
A potent, selective, orally active LXR agonist was identified from focused libraries of tertiary amines. GW3965 (12) recruits the steroid receptor coactivator 1 to human LXRalpha in a cell-free ligand-sensing assay with an EC(50) of 125 nM and profiles as a full agonist on hLXRalpha and hLXRbeta in cell-based reporter gene assays with EC(50)'s of 190 and 30 nM, respectively. After oral dosing at 10 mg/kg to C57BL/6 mice, 12 increased expression of the reverse cholesterol transporter ABCA1 in the small intestine and peripheral macrophages and increased the plasma concentrations of HDL cholesterol by 30%. 12 will be a valuable chemical tool to investigate the role of LXR in the regulation of reverse cholesterol transport and lipid metabolism.
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Cites
Glass, C. K., & Witztum, J. L. (2001) · Cell · doi:10.1016/s0092-8674(01)00238-0 · Cited by 3,051
Mutations in ABC1 in Tangier disease and familial high-density lipoprotein deficiency
Brooks-Wilson, A., Marcil, M., Clee, S. M., Zhang, L.-H., Roomp, K., van Dam, M., Yu, L., Brewer, C., Collins, J. A., Molhuizen, H. O. F., et al. (1999) · Nature Genetics · doi:10.1038/11905 · Cited by 1,687
Self-citationThe gene encoding ATP-binding cassette transporter 1 is mutated in Tangier disease
Bodzioch, M., Orsó, E., Klucken, J., Langmann, T., Böttcher, A., Diederich, W., Drobnik, W., Barlage, S., Büchler, C., Porsch-Özcürümez, M., et al. (1999) · Nature Genetics · doi:10.1038/11914 · Cited by 1,512
Role of LXRs in control of lipogenesis
Schultz, J. R., Tu, H., Luk, A., Repa, J. J., Medina, J. C., Li, L., Schwendner, S., Wang, S., Thoolen, M., Mangelsdorf, D. J., et al. (2000) · Genes & Development · doi:10.1101/gad.850400 · Cited by 1,499
Tangier disease is caused by mutations in the gene encoding ATP-binding cassette transporter 1
Rust, S., Rosier, M., Funke, H., Real, J., Amoura, Z., Piette, J.-C., Deleuze, J.-F., Brewer, H. B., Duverger, N., Denèfle, P., et al. (1999) · Nature Genetics · doi:10.1038/11921 · Cited by 1,433
Control of cellular cholesterol efflux by the nuclear oxysterol receptor LXRα
Venkateswaran, A., Laffitte, B. A., Joseph, S. B., Mak, P. A., Wilpitz, D. C., Edwards, P. A., & Tontonoz, P. (2000) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.200367697 · Cited by 1,005
Sterol-dependent Transactivation of theABC1 Promoter by the Liver X Receptor/Retinoid X Receptor
Costet, P., Luo, Y., Wang, N., & Tall, A. R. (2000) · Journal of Biological Chemistry · doi:10.1074/jbc.m003337200 · Cited by 979
McNeish, J., Aiello, R. J., Guyot, D., Turi, T., Gabel, C., Aldinger, C., Hoppe, K. L., Roach, M. L., Royer, L. J., de Wet, J., et al. (2000) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.97.8.4245 · Cited by 537
ABC1 Gene Expression and ApoA-I-Mediated Cholesterol Efflux Are Regulated by LXR
Schwartz, K., Lawn, R. M., & Wade, D. P. (2000) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.2000.3243 · Cited by 410
Pharmacophore Analysis of the Nuclear Oxysterol Receptor LXRα
Spencer, T. A., Li, D., Russel, J. S., Collins, J. L., Bledsoe, R. K., Consler, T. G., Moore, L. B., Galardi, C. M., McKee, D. D., Moore, J. T., et al. (2001) · Journal of Medicinal Chemistry · doi:10.1021/jm0004749 · Cited by 125
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Cited by
The promise and peril of chemical probes
Arrowsmith, C. H., Audia, J. E., Austin, C., Baell, J., Bennett, J., Blagg, J., Bountra, C., Brennan, P. E., Brown, P. J., Bunnage, M. E., et al. (2015) · Nature Chemical Biology · doi:10.1038/nchembio.1867 · Cited by 839
Self-citationA-Gonzalez, N., Bensinger, S. J., Hong, C., Beceiro, S., Bradley, M. N., Zelcer, N., Deniz, J., Ramirez, C., Díaz, M., Gallardo, G., et al. (2009) · Immunity · doi:10.1016/j.immuni.2009.06.018 · Cited by 677
Liver X receptors in lipid metabolism: opportunities for drug discovery
Hong, C., & Tontonoz, P. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4280 · Cited by 587
Structural Overview of the Nuclear Receptor Superfamily: Insights into Physiology and Therapeutics
Huang, P., Chandra, V., & Rastinejad, F. (2010) · Annual Review of Physiology · doi:10.1146/annurev-physiol-021909-135917 · Cited by 533
The liver X receptor gene team: Potential new players in atherosclerosis
Repa, J. J., & Mangelsdorf, D. J. (2002) · Nature Medicine · doi:10.1038/nm1102-1243 · Cited by 388
Metadata
- Authors
- Collins, J. L., Fivush, A. M., Watson, M. A., Galardi, C. M., Lewis, M. C., Moore, L. B., Parks, D. J., Wilson, J. G., Tippin, T. K., Binz, J. G., Plunket, K. D., Morgan, D. G., Beaudet, E. J., Whitney, K. D., Kliewer, S. A., & Willson, T. M.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2002-04-17
- Volume
- 45
- Issue
- 10
- Pages
- 1963-1966
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2046658442
- Cited by
- 434
- References
- 14
- FWCI
- 13.61
- Type
- journal article
- Language
- en
- Open access
- green
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- Collins, J. L., Fivush, A. M., Watson, M. A., Galardi, C. M., Lewis, M. C., Moore, L. B., Parks, D. J., Wilson, J. G., Tippin, T. K., Binz, J. G., Plunket, K. D., Morgan, D. G., Beaudet, E. J., Whitney, K. D., Kliewer, S. A., & Willson, T. M. (2002). Identification of a Nonsteroidal Liver X Receptor Agonist through Parallel Array Synthesis of Tertiary Amines. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm0255116
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
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.