The DOI matches its Crossref record; 9 of the 9 references it cites were found in a registry or an index.
The discovery and mechanism of action of letrozole
Open accessAbstract
Because estrogen contributes to the promotion and progression of breast cancer, a greater understanding of the role of estrogen in breast cancer has led to therapeutic strategies targeting estrogen synthesis, the estrogen receptor, and intracellular signaling pathways. The enzyme aromatase catalyses the final step in estrogen biosynthesis and was identified as an attractive target for selective inhibition. Modern third-generation aromatase inhibitors (AIs) effectively block the production of estrogen without exerting effects on other steroidogenic pathways. The discovery of letrozole (Femara) achieved the goal of discovering a highly potent and totally selective AI. Letrozole has greater potency than other AIs, including anastrozole, exemestane, formestane, and aminoglutethimide. Moreover, letrozole produces near complete inhibition of aromatase in peripheral tissues and is associated with greater suppression of estrogen than is achieved with other AIs. The potent anti-tumor effects of letrozole were demonstrated in several animal models. Studies with MCF-7Ca xenografts successfully predicted that letrozole would be clinically superior to the previous gold standard tamoxifen and also indicated that it may be more effective than other AIs. An extensive program of randomized clinical trials has demonstrated the clinical benefits of letrozole across the spectrum of hormone-responsive breast cancer in postmenopausal women.
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Aromatization of Androgens by Muscle and Adipose Tissue in Vivo*
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Nitrile-Containing Pharmaceuticals: Efficacious Roles of the Nitrile Pharmacophore
Fleming, F. F., Yao, L., Ravikumar, P. C., Funk, L., & Shook, B. C. (2010) · Journal of Medicinal Chemistry · doi:10.1021/jm100762r · Cited by 1,754
Ahmadi, S., Seraj, M., Chiani, M., Hosseini, S., Bazzazan, S., Akbarzadeh, I., Saffar, S., & Mostafavi, E. (2022) · International Journal of Nanomedicine · doi:10.2147/ijn.s384085 · Cited by 44
Vanol, P. G., Singhal, P., Shah, P. A., Shah, J. V., Shrivastav, P. S., & Sanyal, M. (2016) · Journal of Pharmaceutical Analysis · doi:10.1016/j.jpha.2016.05.004 · Cited by 22
Metadata
- Authors
- Bhatnagar, A. S.
- Venue
- Breast Cancer Research and Treatment
- Published
- 2007-10
- Volume
- 105
- Issue
- S1
- Pages
- 7-17
- ISSN
- 0167-6806 (ISSN-L)
- 1573-7217
- OpenAlex
- W1987147125
- Cited by
- 219
- References
- 9
- FWCI
- 2.34
- Type
- journal article
- Language
- en
- Open access
- hybrid
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
