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Discovery of Tertiary Sulfonamides as Potent Liver X Receptor Antagonists

Year: 2010
Type: article
Abstract: Tertiary sulfonamides were identified in a HTS as dual liver X receptor (LXR, NR1H2, and NR1H3) ligands, and the binding affinity of the series was increased through iterative analogue synthesis. A ligand-bound cocrystal structure was determined which elucidated key interactions for high binding affinity. Further characterization of the tertiary sulfonamide series led to the identification of high affinity LXR antagonists. GSK2033 (17) is the first potent cell-active LXR antagonist described to date. 17 may be a useful chemical probe to explore the cell biology of this orphan nuclear receptor.
DOI: 10.1021/jm901797p
Authors: William J. Zuercher, Richard G. Buckholz, Nino Campobasso, Jon L. Collins, Cristin M. Galardi, Robert T. Gampe, Stephen M. Hyatt, Susan L. Merrihew, John T. Moore, Jeffrey A. Oplinger, Paul R. Reid, Paul K. Spearing, Thomas B. Stanley, Eugene L. Stewart, Timothy M. Willson
Language: English
Subfield: Surgery
Field: Medicine
Open Access status: green
OpenAlex ID: W2013468668
FWCI: 6.529
Cites: 17
Cited by: 96
Related to: 10