Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor–Positive Breast Cancer Models with a Distinct Mechanism of Action

@article{Yu2017SelectiveAR,
  title={Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor–Positive Breast Cancer Models with a Distinct Mechanism of Action},
  author={Ziyang Yu and Suqin He and Dannie Wang and Hitisha K. Patel and Chris P. Miller and Jeffrey L. Brown and G. Hattersley and Jamal C. Saeh},
  journal={Clinical Cancer Research},
  year={2017},
  volume={23},
  pages={7608 - 7620}
}
Purpose: Steroidal androgens suppress androgen receptor and estrogen receptor positive (AR/ER+) breast cancer cells and were used to treat breast cancer, eliciting favorable response. The current study evaluates the activity and efficacy of the oral selective AR modulator RAD140 in in vivo and in vitro models of AR/ER+ breast cancer. Experimental Design: A series of in vitro assays were used to determine the affinity of RAD140 to 4 nuclear receptors and evaluate its tissue-selective AR activity… 

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References

SHOWING 1-10 OF 73 REFERENCES

Targeting androgen receptor in estrogen receptor-negative breast cancer.

Targeting the Androgen Receptor in Breast Cancer

The emerging literature dissecting the role of AR signalling in a context-dependent manner in breast cancer and the renewed interest and wave of clinical trials targeting the AR are reviewed.

Down-regulation of estrogen receptors by androgens in the ZR-75-1 human breast cancer cell line.

It is shown that androgens strongly suppress estrogen receptor (ER) and progesterone receptor contents in this model, as measured by radioligand binding and anti-ER monoclonal antibodies, and that the specific inhibitory effects of androgen therapy could be additive to the standard treatment limited to blockade of estrogens by antiestrogens.

Role of the androgen receptor in breast cancer and preclinical analysis of enzalutamide

This preclinical study supports the initiation of clinical studies evaluating enzalutamide for treatment of AR+ tumors regardless of ER status, since it blocks both androgen- and estrogen- mediated tumor growth.

Pushing estrogen receptor around in breast cancer.

This review will focus on the established and emerging clinical evidence for activating PR or AR in ER-positive breast cancer to inhibit the tumour growth-promoting functions of ER.

Targeting the androgen receptor in prostate and breast cancer: several new agents in development.

An overview of available agents which target the AR axis in both PCa and BCa is offered and insights into the novel drugs in development for targeting this signaling pathway are provided.

Importance of Breast Cancer Subtype in the Development of Androgen-Receptor-Directed Therapy

It is critical that studies of the effect of AR expression and signaling in breast cancer should be context and subtype specific, to successfully translate AR modulation into a clinical strategy for breast cancer.

Steroid Hormone Receptor Positive Breast Cancer Patient-Derived Xenografts

The derivation of steroid hormone receptor positive breast cancer PDX, several pitfalls in their genesis, and their utility in preclinical and translational steroids hormone receptor research are discussed.

Androgen receptor functions in castration-resistant prostate cancer and mechanisms of resistance to new agents targeting the androgen axis

AR functions that contribute to PCa development and progression, the roles of intratumoral androgen synthesis and AR structural alterations in driving AR activity in CRPC, mechanisms of action for abiraterone and enzalutamide, and possible mechanisms of resistance to these agents are outlined.

Antiproliferative actions of the synthetic androgen, mibolerone, in breast cancer cells are mediated by both androgen and progesterone receptors

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