Aromatase, aromatase inhibitors, and breast cancer

Chumsri, Saranya; Howes, Timothy; Bao, Ting; Sabnis, Gauri; Brodie, Angela

doi:10.1016/j.jsbmb.2011.02.001

Cited by 401Estrogen and related hormone effectsBreast Cancer Treatment StudiesAdvanced Breast Cancer Therapies

Aromatase, aromatase inhibitors, and breast cancer

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Chumsri, Saranya, Howes, Timothy, Bao, Ting, Sabnis, Gauri, Brodie, Angela·2011·The Journal of Steroid Biochemistry and Molecular Biology

DOI 10.1016/j.jsbmb.2011.02.001PMC PMC3104073

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Abstract

Estrogens are known to be important in the growth of breast cancers in both pre and postmenopausal women. As the number of breast cancer patients increases with age, the majority of breast cancer patients are postmenopausal women. Although estrogens are no longer made in the ovaries after menopause, peripheral tissues produce sufficient concentrations to stimulate tumor growth. As aromatase catalyzes the final and rate-limiting step in the biosynthesis of estrogen, inhibitors of this enzyme are effective targeted therapy for breast cancer. Three aromatase inhibitors (AIs) are now FDA approved and have been shown to be more effective than the antiestrogen tamoxifen and are well tolerated. AIs are now a standard treatment for postmenopausal patients. AIs are effective in adjuvant and first-line metastatic setting. This review describes the development of AIs and their current use in breast cancer. Recent research focuses on elucidating mechanisms of acquired resistance that may develop in some patients with long term AI treatment and also in innate resistance. Preclinical data in resistance models demonstrated that the crosstalk between ER and other signaling pathways particularly MAPK and PI3K/Akt is an important resistant mechanism. Blockade of these other signaling pathways is an attractive strategy to circumvent the resistance to AI therapy in breast cancer. Several clinical trials are ongoing to evaluate the role of these novel targeted therapies to reverse resistance to AIs. Article from the special issue on 'Targeted Inhibitors'.

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Proof-of-concept for inhibition of intracrine pathways has been established by aromatase inhibition in breast cancer and 5α-reductase inhibition in prostate hyperplasia.
“The proof-of-concept has been established by aromatase inhibition in breast cancer and 5α-reductase inhibition in prostate hyperplasia (Chumsri et al., 2011, Lowe et al., 2003, McConnell et al., 1998).”
From Intracrine androgen biosynthesis, metabolism and action revisited (2018) · cites this paper as Chumsri et al., 2011

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[35]Santen RJ Brodie H Simpson ER Siiteri PK Brodie A History of aromatase: saga of an important biological mediator and therapeutic target Endocr Rev 2009 30 4 343 375 19389994
[88]Sabnis G Gediya L Njar V Brodie A HDAC inhibitors sensitize ER negative breast cancer cells to AIs, Breast Cancer Research and Treatment 2007 30th Annual San Antonio Breast Cancer Symposium San Antonio, TX Abstract # 2096
[108]Lipton A Ali S Leitzel K HER-2 protein expression predicts response to trastuzumab in FISH-positive patients with metastatic breast cancer 2008 31st AACR-CTRC San Antonio Breast Cancer Symposium San Antonio, TX

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Authors: Chumsri, S., Howes, T., Bao, T., Sabnis, G., & Brodie, A.
Affiliations: University of Maryland, Baltimore (US)
Corresponding author: Brodie, Angela
ORCID: Chumsri, Saranya
Bao, Ting
Sabnis, Gauri
Venue: The Journal of Steroid Biochemistry and Molecular Biology
Publisher: Elsevier BV
Published: 2011-05
Volume: 125
Issue: 1-2
Pages: 13-22
ISSN: 0960-0760 (ISSN-L)
DOI: 10.1016/j.jsbmb.2011.02.001
PMC: PMC3104073
OpenAlex: W2085921275
Cited by: 401
References: 113
Citations by year: 2026: 29 · 2025: 40 · 2024: 48 · 2023: 44 · 2022: 33 · 2021: 21 · 2020: 20 · 2019: 15 · 2018: 20 · 2017: 18 · 2016: 21 · 2015: 30 · 2014: 19 · 2013: 23 · 2012: 15
FWCI: 2.20
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
doi.org/10.15223/policy-017 (stm-asf)
doi.org/10.15223/policy-037 (stm-asf)
doi.org/10.15223/policy-012 (stm-asf)
doi.org/10.15223/policy-029 (stm-asf)
doi.org/10.15223/policy-004 (stm-asf)
Locations: The Journal of Steroid Biochemistry and Molecular Biology (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: National Cancer Institute (R01CA062483)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Breast Cancer Treatment Studies
Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Advanced Breast Cancer Therapies
Keywords: aromatase inhibitors, aromatase, breast cancer, tamoxifen, hormone receptor-positive breast cancer, acquired drug resistance, non-specific immunity, MAPK signaling, PI3K/Akt signaling, estrogen synthesis, postmenopausal women, adjuvant therapy, neoadjuvant therapy, metastatic breast cancer, growth factor receptor inhibitors
MeSH terms: Trastuzumab, Antibodies, Monoclonal, Antineoplastic Agents, Aromatase, Breast Neoplasms, Estrogens, Female, Humans, Receptors, Estrogen, Signal Transduction, Phosphatidylinositol 3-Kinases, Mitogen-Activated Protein Kinases, Aromatase Inhibitors, Antibodies, Monoclonal, Humanized

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Aromatase, aromatase inhibitors, and breast cancer

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