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Androgen receptor: structure, role in prostate cancer and drug discovery

M H Eileen Tan1, Jun Li2, H Eric Xu3

  • 11] Department of Obstetrics & Gynecology, National University Hospital, Yong Loo Lin School of Medicine, National University of Singapore, Singapore [2] Laboratory of Structural Sciences, Center for Structural Biology and Drug Discovery, Van Andel Research Institute, Grand Rapids, MI 49503, USA.

Acta Pharmacologica Sinica
|June 10, 2014
PubMed

Insights

Androgen receptors (AR) are key in male traits and diseases like prostate cancer. Understanding AR structure aids in developing new drugs to overcome treatment resistance in castration-resistant prostate cancer (CRPC).

Area of Science:

  • Molecular Biology
  • Endocrinology
  • Oncology

Background:

  • Androgens and androgen receptors (AR) are critical for male sexual characteristics.
  • Dysfunctional AR signaling is implicated in diseases including androgen insensitivity syndrome (AIS) and prostate cancer.
  • Current treatments for prostate cancer involve androgen blockade, but resistance often leads to castration-resistant prostate cancer (CRPC).

Purpose of the Study:

  • To provide an overview of androgen receptor structure and activity.
  • To discuss the role of AR in prostate cancer progression and resistance.
  • To explore the application of structural information and high-throughput screening in drug discovery for prostate cancer.

Main Methods:

  • Review of existing literature on androgen receptor structure and function.
  • Analysis of the impact of AR alterations in prostate cancer.
  • Discussion of structure-based drug design principles and high-throughput screening methodologies.

Main Results:

  • Elucidation of the AR DNA binding domain (DBD) and ligand binding domain (LBD) structures offers insights into receptor function.
  • The AR remains a critical regulator in CRPC, highlighting the need for targeted therapies.
  • Structural information facilitates rational drug design for improved prostate cancer treatment.

Conclusions:

  • Understanding AR structure and function is crucial for developing effective therapies against prostate cancer.
  • Structural insights pave the way for novel drug discovery strategies to combat CRPC and treatment resistance.
  • Integrated approaches using structural biology and high-throughput screening can accelerate the development of targeted therapeutics.

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