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Cited by 434

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 access
Collins, Jon L., Fivush, Adam M., Watson, Michael A., Galardi, Cristin M., Lewis, Michael C., Moore, Linda B., Parks, Derek J., Wilson, Joan G., Tippin, Tim K., Binz, Jane G., Plunket, Kelli D., Morgan, Daniel G., Beaudet, Elizabeth J., Whitney, Karl D., Kliewer, Steven A., Willson, Timothy M.·2002·Journal of Medicinal Chemistry

Abstract

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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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
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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CoChat. (2026). Citation check: Identification of a Nonsteroidal Liver X Receptor Agonist through Parallel Array Synthesis of Tertiary Amines. https://app.cochat.ai/papers/10.1021/jm0255116
The paper
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

Data sources

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.