Therapeutic potential of selective modulators of nuclear receptor action.
Nuclear receptors belong to a superfamily of ligand-inducible transcription factors that, in addition to directly regulating their cognate gene programs, can also mutually interfere with other signaling pathways. The recent identification of selective agonists/antagonists of the glucocorticoid, retinoid and estrogen receptors suggests that it might be possible to selectively elicit only a subset of the nuclear receptor functions that are induced by the natural ligand, with the aim of increasing the functional and, perhaps, tissue selectivity of nuclear receptor ligands and reducing unwanted side effects.
Resche-Rigon
M
M
Hoechst Marion Roussel, Romainville, France. michele.resche-rigon@hmrag.com
Gronemeyer
H
H
D000595:Amino Acid Sequence; D000818:Animals; D005786:Gene Expression Regulation; D006801:Humans; D008024:Ligands; D008969:Molecular Sequence Data; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism*; D011960:Receptors, Estrogen / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D011965:Receptors, Glucocorticoid / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D018168:Receptors, Retinoic Acid / Q000378:metabolism; D012176:Retinoids / Q000378:metabolism / Q000494:pharmacology; D015398:Signal Transduction; D018808:Transcription Factor AP-1 / Q000235:genetics / Q000378:metabolism; D014157:Transcription Factors / Q000235:genetics / Q000378:metabolism*
D008024:Ligands; D018160:Receptors, Cytoplasmic and Nuclear; D011960:Receptors, Estrogen; D011965:Receptors, Glucocorticoid; D018168:Receptors, Retinoic Acid; D012176:Retinoids; D018808:Transcription Factor AP-1; D014157:Transcription Factors