Domain interactions between coregulator ARA(70) and the androgen receptor (AR)

Mol Endocrinol. 2002 Feb;16(2):287-300. doi: 10.1210/mend.16.2.0765.

Abstract

The coregulator function of AR-associated protein 70 (ARA(70)) was investigated to further characterize its interaction with the AR. Using a yeast two-hybrid assay, androgen-dependent binding of ARA(70) deletion mutants to the AR ligand-binding domain (LBD) was strongest with ARA(70) amino acids 321-441 of the 614 amino acid ARA(70) protein. Mutations adjacent to or within an FxxLF motif in this 120-amino acid region abolished androgen-dependent binding to the AR-LBD both in yeast and in glutathione-S-transferase affinity matrix assays. Yeast one-hybrid assays revealed an intrinsic ARA(70) transcriptional activation domain within amino acids 296-441. In yeast assays the ARA(70) domains for transcriptional activation and for binding to the AR-LBD were inhibited by the C-terminal region of ARA(70). Full-length ARA(70) increased androgen-dependent AR transactivation in transient cotransfection assays using a mouse mammary tumor virus-luciferase reporter in CV1 cells. ARA(70) also increased constitutive transcriptional activity of an AR NH(2)-terminal-DNA binding domain fragment and bound this region in glutathione-S-transferase affinity matrix assays. Binding was independent of the ARA(70) FxxLF motif. The results identify an ARA(70) motif required for androgen-dependent interaction with the AR-LBD and demonstrate that ARA(70) can interact with the NH(2)-terminal and carboxyl-terminal regions of AR.

Publication types

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

MeSH terms

  • Amino Acid Motifs
  • Androgens / pharmacology
  • Animals
  • Binding Sites
  • Cell Line
  • Gene Library
  • Humans
  • Male
  • Nuclear Receptor Coactivators
  • Oncogene Proteins*
  • Protein Binding
  • Protein Structure, Tertiary
  • Receptors, Androgen / chemistry*
  • Receptors, Androgen / genetics
  • Receptors, Androgen / metabolism*
  • Receptors, Glucocorticoid / metabolism
  • Receptors, Progesterone / metabolism
  • Sequence Deletion
  • Trans-Activators / chemistry*
  • Trans-Activators / genetics
  • Trans-Activators / metabolism*
  • Transcription Factors*
  • Transcriptional Activation / drug effects
  • Transfection
  • Two-Hybrid System Techniques
  • Yeasts

Substances

  • Androgens
  • NCOA4 protein, human
  • Nuclear Receptor Coactivators
  • Oncogene Proteins
  • Receptors, Androgen
  • Receptors, Glucocorticoid
  • Receptors, Progesterone
  • Trans-Activators
  • Transcription Factors