Androgen Receptor: A Complex Therapeutic Target for Breast Cancer

Ramesh Narayanan1, James T Dalton2

  • 1Department of Medicine, University of Tennessee Health Science Center, Memphis, TN 38103, USA. rnaraya4@uthsc.edu.

Cancers
|December 6, 2016
PubMed

Insights

Androgen receptor (AR) is emerging as a key target for breast cancer treatment, especially in resistant cases. This review explores the complex therapeutic role of AR, including new drug developments.

Area of Science:

  • Oncology
  • Molecular Biology
  • Endocrinology

Background:

  • Estrogen receptor (ER) and human epidermal growth factor receptor (HER2) are primary breast cancer targets.
  • Androgen receptor (AR) is increasingly recognized for its role in treatment-resistant breast cancer.
  • High AR expression in breast tumors supports its investigation as a therapeutic target.

Approach:

  • This review synthesizes current research on the androgen receptor's function in breast cancer.
  • It examines the rationale for targeting AR, including novel nonsteroidal drugs.
  • The review discusses the complexities of AR agonism and antagonism in clinical trials.

Key Points:

  • AR is a promising target for overcoming resistance to conventional breast cancer therapies.
  • New nonsteroidal drugs targeting AR are in clinical development.
  • The dual role of AR agonists and antagonists presents a complex therapeutic landscape.

Conclusions:

  • Understanding the intricate role of AR is crucial for developing effective precision treatments for breast cancer.
  • Further research into AR-targeted therapies may offer new options for patients with advanced or resistant disease.

Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
9.0K
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
8.3K
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
60
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:
4.4K
mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
5.0K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
4.6K