[Synthetic ligands for nuclear receptors].
Fat-soluble ligands like steroid hormones serve to activate nuclear receptors. Nuclear receptors are ligand-dependent transcription factors to transcriptionally activate sets of target genes, and such ligand-dependent transcription mediates a number of transcriptional coregulators. Since nuclear receptors form a gene superfamily, their protein structures are divided into several functional domains. The C-terminal ligand binding domain is structurally altered upon ligand binding, and switches interaction of co-transcriptional regulators; from co-repressors to co-activators. Likewise, owing to ligand-dependent structure alteration of the entire receptor proteins, the N-terminal domains of receptors become accessible to co-activators. Synthetic agonists/antagonists are potent to induce structural alteration in ligand-type dependent manner, resulting in pharmacological association with transcriptional co-regulators.
IMCB, University of Tokyo.
Shigeaki
S
Kato
D006801:Humans; D008024:Ligands; D058990:Molecular Targeted Therapy; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013256:Steroids / Q000494:pharmacology; D014158:Transcription, Genetic
D008024:Ligands; D018160:Receptors, Cytoplasmic and Nuclear; D013256:Steroids