Recruitment of p160 Coactivators to Androgen Receptors
Androgens control the proliferation of target cells and a number of physiological responses by means of receptors that function as ligand-dependent transcription factors. Androgen receptors (AR) function either directly by binding to response elements in the vicinity of the promoter or indirectly by modulating the activity of other transcription factors. In common with other nuclear receptors the AR is likely to undergo a characteristic conformational change upon ligand binding that allows the recruitment of cofactors which are required to stimulate transcription of target genes [1, 2, 3]. It first became obvious that nuclear receptors require common cofactors to activate transcription when “squelching” between different receptors was observed: the expression of one active receptor inhibited the activity of a second, implying the existence of an essential limiting cofactor .
KeywordsAndrogen Receptor Nuclear Receptor Steroid Receptor Coactivator LXXLL Motif Nuclear Receptor Coactivators
Unable to display preview. Download preview PDF.
- 7.Jenster G, van der Korput H, Trapman J, Brinkmann AO (1995) Identification of two transcription activation units in the N-terminal domain of the human androgen receptor. J. Biol. Chem. 270: 7341–46Google Scholar
- 8.Bevan CL, Hoare S, Claessens F, Heery DM, Parker MG (1999) The AF1 and AF2 domains of the androgen receptor interact with distinct regions of SRC1. Mol Cell Biol 20: 8383–8392Google Scholar
- 10.Mak HY, Hoare S, Henttu PMA, Parker MG (1999) Molecular determinants of the estrogen receptor-coactivator interface. Molecular Cellular Biology 19: 3895–3903Google Scholar
- 15.Berrevoets CA, Doesburg P, Sketetee K, Trapman J, Brinkmann AO (1998) Functional interactions of the AF-2 domain core region of the human androgen receptor with the amino-terminal domain and with the transcriptional coactivator TIF-2 (transcriptional intermediary factor-2). Mol Endocrinol 12: 1172–1183PubMedCrossRefGoogle Scholar
- 17.Langley E, Kemppainen JA, E.M. W (1998) Intermolecular NH2-/carboxyterminal interactions in androgen receptor dimerization revealed by mutations that cause androgen insensitivity. J Biol Chem 273: 92–101Google Scholar
- 22.Spencer TE, Jenster G, Burcin MM, Allis CD, Zhou J, Mizzen CA, McKenna NJ, Onate SA, Tsai SY, Tsai M-J, O’Malley BW (1997) Steroid receptor coactivator-1 is a histone acetyltransferase. Nature 389: I94–198Google Scholar