Membrane Localization and Rapid Non-Transcriptional Action of the Androgen Receptor

  title={Membrane Localization and Rapid Non-Transcriptional Action of the Androgen Receptor},
  author={S. Mink and L. Shatkina and A. Nestl and A. Cato},
Androgens play a major role in male sexual development and in prostate growth during later life (for a review, see Brinkman 2001). They function by binding a cytoplasmic androgen receptor (AR) that is present in target cells in an inactive state in association with molecular chaperones and co-chaperones. Upon hormone binding, the receptor is thought to dissociate from the inactivating proteins and is transported into the nucleus where it binds discrete nucleotide sequences to modulate the… Expand
1 Citations
Ultrastructural evidence that androgen receptors are located at extranuclear sites in the rat hippocampal formation
Results suggest that ARs may serve as both a genomic and non-genomic transducer of androgen action in the hippocampal formation. Expand


The Androgen Receptor as Mediator of Gene Expression and Signal Transduction Pathways
Findings have shown that the receptor also mediates non-conventional responses attributed hitherto only to activated growth factor receptors, which suggest that in addition to its genomic functions, the androgen receptor also regulates non-genomic processes. Expand
Nongenotropic, Sex-Nonspecific Signaling through the Estrogen or Androgen Receptors Dissociation from Transcriptional Activity
A novel paradigm of sex steroid action on osteoblasts, osteocytes, embryonic fibroblasts, and HeLa cells involving activation of a Src/Shc/ERK signaling pathway and attenuating apoptosis is demonstrated, providing proof of principle for the development of function-specific-as opposed to tissue-selective-and gender-neutral pharmacotherapeutics. Expand
Interaction of oestrogen receptor with the regulatory subunit of phosphatidylinositol-3-OH kinase
It is shown that the ER isoform, ERα, binds in a ligand-dependent manner to the p85α regulatory subunit of phosphatidylinositol-3-OH kinase (PI(3)K). Expand
Rapid signalling by androgen receptor in prostate cancer cells
A novel regulatory action of the androgen receptor is demonstrated and it is proved that in addition to its known transcriptional effects, it also uses non-conventional means to modulate several cellular signalling processes. Expand
Progesterone receptor contains a proline-rich motif that directly interacts with SH3 domains and activates c-Src family tyrosine kinases.
It is shown that rapid progestin-induced activation of Src and downstream MAP kinase in mammalian cells is dependent on PR-SH3 domain interaction, but not on the transcriptional activity of PR. Expand
Testosterone signaling through internalizable surface receptors in androgen receptor-free macrophages.
The data provide evidence for the existence of G-protein-coupled, agonist-sequestrable receptors for testosterone in plasma membranes, which initiate a transcription-independent signaling pathway of testosterone. Expand
Molecular basis of androgen insensitivity
  • A. Brinkmann
  • Medicine, Biology
  • Molecular and Cellular Endocrinology
  • 2001
In exon 2 of the androgen receptor gene of a patient with receptor-positive androgen insensitivity, a cytosine-to-adenine transition, converting alanine 564 into an aspartic acid residue, resulted in defective DNA binding and transactivation. Expand
Testosterone induces Ca2+ influx via non‐genomic surface receptors in activated T cells
Data indicate a novel mode of direct action of testosterone on T cells which is not mediated through the classical androgen receptor response, but through unconventional plasma membrane receptors. Expand
Androgens increase intracellular calcium concentration and inositol 1,4,5-trisphosphate and diacylglycerol formation via a pertussis toxin-sensitive G-protein.
The results suggest that male rat osteoblasts bear nongenomic unconventional cell-surface receptors for testosterone that belong to the class of the membrane receptors coupled to a phospholipase C via a pertussis toxin-sensitive G-protein. Expand
Steroid‐induced androgen receptor–oestradiol receptor β–Src complex triggers prostate cancer cell proliferation
Hormone‐stimulated Src interaction with the androgen receptor and oestradiol receptor α or β is detected using glutathione S‐transferase fusion constructs and the role of this phosphotyrosine is stressed by its requirement for association of oestrogens receptor α with Src and consequent activation of Src in intact Cos cells. Expand