Related Experiment Video

Updated: May 12, 2026

Prostate Organoid Cultures as Tools to Translate Genotypes and Mutational Profiles to Pharmacological Responses
08:36

Prostate Organoid Cultures as Tools to Translate Genotypes and Mutational Profiles to Pharmacological Responses

Published on: October 24, 2019

Androgen receptor: past, present and future

Lucy J Schmidt1, Donald J Tindall

  • 1Department of Urology Research, Mayo Clinic College of Medicine, Mayo Clinic, Rochester, MN 55905, USA.

Current Drug Targets
|April 10, 2013
PubMed

Insights

Prostate cancer research focuses on androgens and the androgen receptor (AR). Despite therapies, castration-recurrent prostate cancer persists, driving research into AR mechanisms for new drug development.

Area of Science:

  • Oncology
  • Molecular Biology
  • Urology

Background:

  • Prostate cancer remains a leading cause of cancer death in men globally.
  • Androgen deprivation therapy (ADT) is a primary treatment, but castration-recurrent prostate cancer (CRPC) emerges.
  • The androgen receptor (AR) remains central to CRPC, despite decades of research.

Purpose of the Study:

  • To review the persistent role of the androgen receptor (AR) in advanced prostate cancer, particularly in castration-recurrent disease.
  • To explore the mechanisms by which prostate cancer cells evade ADT.
  • To highlight current research directions and the potential for novel therapeutic strategies targeting the AR.

Main Methods:

  • Review of historical and current research on androgens and the androgen receptor in prostate cancer.
  • Analysis of mechanisms driving castration-recurrent prostate cancer (CRPC).
  • Incorporation of findings from genome-wide association studies (GWAS).

Main Results:

  • Prostate cancer remains a significant cause of male mortality despite extensive research and ADT development.
  • CRPC develops in patients who fail ADT, with the AR playing a critical role.
  • Mechanisms of AR reactivation include amplification, mutation, splice variants, alternative pathways, coregulator activity, and intratumoral androgen synthesis.

Conclusions:

  • Understanding AR function under castrate conditions is crucial for overcoming treatment resistance.
  • Emerging knowledge from GWAS and mechanistic studies offers new avenues for drug development.
  • Targeting the AR and its associated pathways holds promise for eradicating advanced prostate cancer.

More Related Videos

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay09:07

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay

Published on: December 19, 2018

Related Concept Videos

Intracellular Hormone Receptors01:08

Intracellular Hormone Receptors

Lipid-soluble hormones diffuse across the plasma and nuclear membrane of target cells to bind to their specific intracellular receptors. These receptors act as transcription factors that regulate gene expression and protein synthesis in the target cell
Testosterone: Functions and Regulation01:26

Testosterone: Functions and Regulation

The intricate hormonal interplay essential for male reproductive health begins with the release of gonadotropin-releasing hormone (GnRH) by the hypothalamus. This hormone prompts the pituitary gland to secrete follicle-stimulating hormone (FSH) and luteinizing hormone (LH). LH targets the Leydig cells in the testes, stimulating them to produce and release testosterone. In concert with testosterone, FSH acts on the Sertoli cells within the seminiferous tubules to facilitate the release of...
Signal Transduction: Overview01:26

Signal Transduction: Overview

Cells respond to many types of information, often through receptor proteins positioned on the membrane. They respond to chemical signals, such as hormones, neurotransmitters, and other signaling molecules, initiating a series of molecular reactions to produce an appropriate response. This is called signal transduction. Cells also coordinate different responses elicited by the same signaling molecule via mediators, allowing molecular cross-talk.
Typically, signal transduction involves three...
Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
Internal Receptors01:31

Internal Receptors

Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...