Antagonist ligands work by inducing a conformation of the receptor which prevents coactivator and promotes corepressor binding

An example of antagonistic nuclear receptor drug is mifepristone which binds to the glucocorticoid and progesterone receptors and therefore blocks the activity of the endogenous hormones cortisol and progesterone respectively.

Other synthetic nuclear receptor ligands have no apparent effect on gene transcription in the absence of endogenous ligand. However they block the effect of agonist through competitive binding to the same binding site in the nuclear receptor. These ligands are referred to as antagonists.

Antagonists

Agonist ligands work by inducing a conformation of the receptor which favors coactivator binding.

Дата добавления: 2014-01-14