Androgen Receptor (AR) Coregulators: An Overview

The biological action of androgens is mediated through the androgen receptor (AR). Androgen-bound AR functions as a transcription factor to regulate genes involved in an array of physiological processes, most notably male sexual differentiation and maturation, and the maintenance of spermatogenesis. The transcriptional activity of AR is affected by coregulators that influence a number of functional properties of AR, including ligand selectivity and DNA binding capacity. As the promoter of target genes, coregulators participate in DNA modification, either directly through modification of histones or indirectly by the recruitment of chromatin-modifying com-plexes, as well as functioning in the recruitment of the basal transcriptional machinery. Aberrant coregulator activity due to mutation or altered expression levels may be a contributing factor in the progression of diseases related to AR activity, such as prostate cancer. AR demonstrates distinct differences in its interaction with coregulators from other steroid receptors due to differences in the functional interaction between AR domains, possibly resulting in alterations in the dynamic interactions between coregulator complexes. ( The Androgen Receptor (AR) III. Interaction of AR with General Transcription Factors (GTFs) IV. AR Coactivators A. The steroid receptor coactivator (SRC) family B. The PIAS [protein inhibitor of activated signal transducer and activator of transcription (STAT)] family C. Filamentous actin (f-actin)-binding proteins D. Coactivators that mediate ligand binding and receptor stability E. Coactivators that influence nuclear-cytoplasmic trafficking of AR F. Chromatin remodeling and coactivators G. AR coactivators as mediators of signal transduction V. AR Corepressors VI. AR Coregulators and Cancer VII.