Interplay between two hormone-independent activation domains in the androgen receptor

Cancer Res. 2006 Jan 1;66(1):543-53. doi: 10.1158/0008-5472.CAN-05-2389.

Abstract

The androgen receptor (AR) plays a key role in prostate cancer development, as well as its treatments, even for the hormone-refractory state. Here, we report that an earlier described lysine-to-arginine mutation at position 179 in AR leads to a more potent AR. We show that two activation domains (Tau-1 and Tau-5) are necessary and sufficient for the full activity of AR and the intrinsic activity of the AR-NTD. Two alpha-helices surrounding the Lys179 define the core of Tau-1, which can act as an autonomous activation function, independent of p160 coactivators. Furthermore, we show that although the recruitment of p160 coactivators is mediated through Tau-5, this event is attenuated by core Tau-1. This better definition of the mechanisms of action of both Tau-1 and Tau-5 is instrumental for the design of alternative therapeutic strategies against prostate cancer.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Binding Sites
  • COS Cells
  • Cell Lineage
  • Chlorocebus aethiops
  • Humans
  • Male
  • Molecular Sequence Data
  • Mutagenesis, Site-Directed
  • Prostatic Neoplasms / genetics
  • Prostatic Neoplasms / metabolism
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Receptors, Androgen / chemistry*
  • Receptors, Androgen / genetics
  • Receptors, Androgen / physiology*
  • Structure-Activity Relationship
  • Transcriptional Activation
  • Transfection

Substances

  • Receptors, Androgen