Y2H - Identifying selective compounds for the Liver X Receptor (LXR)

A reference LXR agonist (T0901317) was compared to seven different LXR compounds found and developed at Phenex. The graph shows the results from dose response experiments with T0901317 and Cpds 1-7 with respect to recruitment of a distinct coactivator or corepressor construct. Compounds 2 and 3 clearly exhibit a distinct cofactor recruitment pattern compared to the reference compound (Ref CPD) and the other Compounds (CPD1-7): both preferentially induce corepressor (CoR) recruitment rather than coactivator (CoA) recruitment (D: vehicle). These LXR compounds also behave differently in pharmacological experiments as opposed to their "peer" compounds CPD1 and 4-7 which show a more classical agonist type behaviour (data not shown here).

 

LXRα - LBD