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Special Issue "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)

Special Issue Editor

Guest Editor
Prof. Dr. Guangdi Wang

RCMI Cancer Research Center, Xavier University of Louisiana, New Orleans, Louisiana 70125, United States
Website | E-Mail
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 Wang
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.


  • SERM
  • SERD
  • ER+ breast cancer
  • endocrine therapy
  • endocrine resistance
  • ER downregulation
  • hot flash
  • osteoporosis
  • antiestrogen

Published Papers (1 paper)

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Open AccessArticle Exosome-Mediated Transfer of Cancer Cell Resistance to Antiestrogen Drugs
Molecules 2018, 23(4), 829; https://doi.org/10.3390/molecules23040829
Received: 9 February 2018 / Revised: 29 March 2018 / Accepted: 2 April 2018 / Published: 4 April 2018
Cited by 2 | PDF Full-text (14118 KB) | HTML Full-text | XML Full-text
Exosomes are small vesicles which are produced by the cells and released into the surrounding space. They can transfer biomolecules into recipient cells. The main goal of the work was to study the exosome involvement in the cell transfer of hormonal resistance. The
[...] Read more.
Exosomes are small vesicles which are produced by the cells and released into the surrounding space. They can transfer biomolecules into recipient cells. The main goal of the work was to study the exosome involvement in the cell transfer of hormonal resistance. The experiments were performed on in vitro cultured estrogen-dependent MCF-7 breast cancer cells and MCF-7 sublines resistant to SERM tamoxifen and/or biguanide metformin, which exerts its anti-proliferative effect, at least in a part, via the suppression of estrogen machinery. The exosomes were purified by differential ultracentrifugation, cell response to tamoxifen was determined by MTT test, and the level and activity of signaling proteins were determined by Western blot and reporter analysis. We found that the treatment of the parent MCF-7 cells with exosomes from the resistant cells within 14 days lead to the partial resistance of the MCF-7 cells to antiestrogen drugs. The primary resistant cells and the cells with the exosome-induced resistance were characterized with these common features: decrease in ERα activity and parallel activation of Akt and AP-1, NF-κB, and SNAIL1 transcriptional factors. In general, we evaluate the established results as the evidence of the possible exosome involvement in the transferring of the hormone/metformin resistance in breast cancer cells. Full article

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