Selective Estrogen Receptor Modulators and Downregulators (SERMs and SERDs): New Possibilities in Developing Next Generation Hormone Therapies for Breast Cancer
A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Bioorganic Chemistry".
Deadline for manuscript submissions: closed (10 February 2018) | Viewed by 9172
Special Issue Editor
Interests: design, synthesis, and biological evaluation of SERMs and SERDs; novel lead compounds of antiestrogenic activities; novel lead compounds of ER downregulating activities; SERMs that are not cross-resistant to tamoxifen; SERDs that are not cross resistant to fulvestrant; SERM/SERD hybrid; Reviews and perspectives on SERM/SERD development
Special Issue Information
Dear Colleagues,
Endocrine agents, for the treatment of hormone receptor positive breast cancer patients, include selective estrogen receptor modulators (SERMs), aromatase inhibitors (AIs), and selective estrogen receptor downregulators (SERDs). The first generation SERM, tamoxifen, has been used for over four decades in the standard of care of estrogen receptor positive (ER+) breast cancer in both pre- and postmenopausal patients. Second and third generation SERMs, such as raloxifene, lasofoxifen, and bazedoxifen, have been developed as more potent and selective ER antagonists, and are used for osteoporosis and breast cancer prevention, but have not been approved for hormone therapy for breast cancer patients. Major clinical challenges with SERM therapy include de novo and acquired resistance, which inevitably lead to recurrence of disease and mortality. Fulvetrant is currently the only SERD that has been approved for clinical use, and it has a low bioavailability and can only be administered as an intramuscular injection depot. There is clearly an urgent need to improve breast cancer patient survival and quality of life by developing next generation SERM/SERD hybrids and more efficacious SERDs that are not cross-resistant to tamoxifen and AI treatment. The present Special Issue is aimed at covering new developments in the design, synthesis, and biological evaluation of novel SERMs, SERDs, and SERM/SERD hybrids that may hold clinical potential as breast cancer treatment agents.
Prof. Dr. Guangdi WangGuest Editor
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Keywords
- SERM
- SERD
- ER+ breast cancer
- endocrine therapy
- endocrine resistance
- ER downregulation
- hot flash
- osteoporosis
- antiestrogen
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