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Updated: May 31, 2026

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
Recent developments in antiandrogens and selective androgen receptor modulators
Bernard Haendler1, Arwed Cleve
1TRG Oncology, Global Drug Discovery, Bayer HealthCare, D-13342 Berlin, Germany. bernard.haendler@bayer.com
Abstract:
The androgens testosterone and dihydrotestosterone play an essential role in the development and maintenance of primary and secondary male characteristics. Androgens bind to a specific androgen receptor (AR), a ligand-dependent transcription factor which controls the expression of a large number of downstream target genes. The AR is an essential player in early and late prostate cancer, and may also be involved in some forms of breast cancer. It also represents a drug target for the treatment of hypogonadism. Recent studies furthermore indicate that targeting the AR in pathologies such as frailty syndrome, cachexia or polycystic ovary syndrome may have clinical benefit. Numerous AR ligands with very different pharmacological properties have been identified in the last 40 years and helped to treat several of these diseases. However, progress still needs to be made in order to find compounds with an improved profile with regard to efficacy, differentiation and side-effects. This will only be achieved through a better understanding of the mechanisms involved in normal and aberrant AR signaling.
Insights
Androgens like testosterone are vital for male traits and influence diseases such as prostate cancer. Understanding androgen receptor (AR) signaling is key to developing better treatments for various conditions.
Area of Science:
- Endocrinology
- Molecular Biology
- Oncology
Background:
- Androgens, including testosterone and dihydrotestosterone, are crucial for male sexual development and characteristics.
- The androgen receptor (AR) is a transcription factor that mediates androgen action and is implicated in prostate and breast cancers.
Purpose of the Study:
- To explore the role of androgen receptor (AR) signaling in various physiological and pathological conditions.
- To highlight the therapeutic potential of targeting AR in diseases beyond cancer, such as hypogonadism, frailty, cachexia, and polycystic ovary syndrome.
Main Methods:
- Review of existing literature on AR function and AR-targeting drugs.
- Analysis of the mechanisms underlying normal and aberrant AR signaling pathways.
Main Results:
- AR plays a critical role in both normal development and diseases like prostate cancer.
- AR targeting shows promise for treating conditions including hypogonadism, frailty, cachexia, and PCOS.
Conclusions:
- Despite numerous AR ligands developed over 40 years, improved compounds are needed for better efficacy and fewer side effects.
- Further understanding of AR signaling mechanisms is essential for developing next-generation AR-targeting therapeutics.
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