1221277-90-2Relevant articles and documents
Synthesis and structure activity relationship of the first class of LXR inverse agonists
Elgendy, Bahaa,Griffett, Kristine,Hegazy, Lamees,Di Fruscia, Paolo,Sample, Kirby,Schoepke, Emmalie,Kamenecka, Theodore M.,Burris, Thomas P.
, (2021/12/14)
Liver X Receptors (LXRs) are members of the nuclear receptor family, and they play significant role in lipid and cholesterol metabolism. Moreover, they are key regulators of several inflammatory pathways. Pharmacological modulation of LXRs holds great pot
Discovery of tertiary sulfonamides as potent liver X receptor antagonists
Zuercher, William J.,Buckholz, Richard G.,Campobasso, Nino,Collins, Jon L.,Galardi, Cristin M.,Gampe, Robert T.,Hyatt, Stephen M.,Merrihew, Susan L.,Moore, John T.,Oplinger, Jeffrey A.,Reid, Paul R.,Spearing, Paul K.,Stanley, Thomas B.,Stewart, Eugene L.,Willson, Timothy M.
supporting information; experimental part, p. 3412 - 3416 (2010/09/07)
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.
