Steroid/nuclear receptor coactivators.
In higher eukaryotes, steroids/thyroid hormones and many lipophilic compounds regulate cellular physiology through binding to the steroid/nuclear receptor proteins. Steroid/nuclear receptors are ligand-dependent transcriptional activators that can stimulate gene expression. This transcriptional activation plays a pivotal role in hormone-regulated physiological and pharmacological responses. In recent years, several steroid/nuclear receptor cofactors have been identified and found to interact with the receptor and modulate its transcriptional activity. Among these cofactors, a family of three co-activators has been the focus of intense studies. Although gaps remain, progress has been made in understanding how a given co-activator interacts with the receptor and promotes transcriptional activation. We are beginning to understand co-activator action; for instance, several studies have established the molecular basis of antagonism by anti-hormones and the connection of co-activators with human cancers.
Chen
J D
JD
Department of Pharmacology and Molecular Toxicology, University of Massachusetts Medical School, Worcester 01655-0126, USA.
D000595:Amino Acid Sequence; D000818:Animals; D018360:Crystallography, X-Ray; D051548:Histone Acetyltransferases; D006801:Humans; D008969:Molecular Sequence Data; D056920:Nuclear Receptor Coactivator 1; D011987:Receptors, Steroid / Q000378:metabolism; D014157:Transcription Factors / Q000737:chemistry / Q000494:pharmacology / Q000502:physiology; D015533:Transcriptional Activation
D011987:Receptors, Steroid; D014157:Transcription Factors; D051548:Histone Acetyltransferases; C538859:NCOA1 protein, human; D056920:Nuclear Receptor Coactivator 1