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Cited by 230

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Estrogen Receptors as Therapeutic Targets in Breast Cancer

Ariazi, Eric A., Jordan, V. Craig·2008·Methods and Principles in Medicinal Chemistry
DOI 10.1002/9783527623297.ch5
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Abstract

The estrogen receptor alpha (ERalpha) has proven to be the single most important target in breast cancer over the last 30 years. The use of the selective ER modulator (SERM) tamoxifen for the treatment and prevention of breast cancer has changed therapeutics. The SERM raloxifene, approved for the treatment of osteoporosis, lacks tamoxifen's increased risk for endometrial cancer and is being evaluated for the prevention of breast cancer. Other SERMs approved or under development for use against breast cancer or osteoporosis include toremifene, GW5638, GW7604 (the active metabolite of GW5638), idoxifene, lasofoxifene, arzoxifene, bazedoxifene, EM-800 and acolbifene (the active metabolite of EM-800). Aromatase inhibitors (AIs) have recently proven to be more efficacious than tamoxifen as first-line therapy, efficacious for second-line therapy (e.g. against tamoxifen-resistant disease), and useful for extended adjuvant therapy after tamoxifen. The AIs include the non-steroidal agents letrozole and anastrole, and the steroidal agent exemestane. The pure antiestrogen fulvestrant has proven to be just as effective as AIs. Other pure antiestrogens, ZK-703, ZK-253, RU 58668 and TAS-108 show great promise. The development of resistance to endocrine therapy remains a clinically important problem, and laboratory models based on human breast cancer cells grown as tumors in immune-compromised mice have led to important insights into this problem. Progesterone receptor-negative status of ER-positive breast cancers may reflect altered growth factor receptor signaling, and helps to explain why this subclass of tumors exhibits lower response rates to tamoxifen compared to cancers typed progesterone receptor-positive. Crosstalk among plasma membrane-localized ER, growth factor receptor signaling, and nuclear-localized ER provide further insights into antihormonal-resistant breast cancer.

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Metadata

Authors
Ariazi, E. A., & Jordan, V. C.
Venue
Methods and Principles in Medicinal Chemistry
Publisher
Wiley
Published
2008-08-20
Volume
6
Issue
3
Pages
127-199
ISSN
  • 1432-4636 (ISSN-L)
  • 1865-0562
DOI
10.1002/9783527623297.ch5
OpenAlex
W2016908879
Cited by
230
References
15
Type
other
Language
en
Open access
closed
Licence
doi.wiley.com/10.1002/tdm_license_1.1 (tdm)

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Ariazi, E. A., & Jordan, V. C. (2008). Estrogen Receptors as Therapeutic Targets in Breast Cancer. Methods and Principles in Medicinal Chemistry. https://doi.org/10.1002/9783527623297.ch5

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