[HTML][HTML] A novel principle for partial agonism of liver X receptor ligands: competitive recruitment of activators and repressors
M Albers, B Blume, T Schlueter, MB Wright… - Journal of Biological …, 2006 - ASBMB
Partial, selective activation of nuclear receptors is a central issue in molecular endocrinology
but only partly understood. Using LXRs as an example, we show here that purely agonistic
ligands can be clearly and quantitatively differentiated from partial agonists by the cofactor
interactions they induce. Although a pure agonist induces a conformation that is
incompatible with the binding of repressors, partial agonists such as GW3965 induce a state
where the interaction not only with coactivators, but also corepressors is clearly enhanced …
but only partly understood. Using LXRs as an example, we show here that purely agonistic
ligands can be clearly and quantitatively differentiated from partial agonists by the cofactor
interactions they induce. Although a pure agonist induces a conformation that is
incompatible with the binding of repressors, partial agonists such as GW3965 induce a state
where the interaction not only with coactivators, but also corepressors is clearly enhanced …