Hormone antagonist

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Structure of abiraterone acetate, a hormone antagonist treatment for prostate cancer. Abiraterone acetate Structural Formula V1.svg
Structure of abiraterone acetate, a hormone antagonist treatment for prostate cancer.

For the use of hormone antagonists in cancer, see hormonal therapy (oncology)

Contents

A hormone antagonist is a molecule, produced either synthetically or endogenously, that binds to a specific hormone receptor to block the effect or synthesis of that hormone. [1] There are many types of hormone antagonists, such as gonadotropin-releasing hormone (GnRH) antagonists, estrogen antagonists, and androgen antagonists.

Organisms may use hormone antagonists to modify the action of their hormone receptors. [1] For example, ghrelin is a hormone that stimulates appetite and growth hormone release by activating the growth hormone secretagogue receptor (GHSR). [2] LEAP2 was found to be a peptide hormone synthesized by the liver and small intestine that blocks the GHSR activation by ghrelin, thereby reducing appetite. [2]

Synthetically produced hormone antagonists can also be used as anticancer treatments for hormone-sensitive cancers like breast cancer and prostate cancer. [3]

Anti-cancer treatments

Breast cancer

Hormone antagonists are used widely in anticancer treatments, such as the drug tamoxifen, an anti-estrogen that binds to estrogen receptors to slow the growth of some estrogen receptor-positive breast cancers. [4] Aromatase inhibitors (AIs) are also prescribed as a breast cancer treatment, especially after mastectomies. [5] AIs work by blocking the action of the aromatase enzyme, which converts androgens, like testosterone, into estrogen. [6] Aromatase inhibitors can be used in conjunction with estrogen receptor inhibitors to treat estrogen receptor-positive breast cancers in women who have gone through menopause already. [6] [5]

Prostate cancer

Anti-androgens such as enzalutamide can be used as a treatment for prostate cancer, which, by binding to the androgen receptor, can inhibit the binding of testosterone. Androgens may promote prostate cancer, with the main androgens secreted by the testicles being testosterone and dihydroxytestosterone (DHT). [7] Some androgens can be made by the adrenal glands, which are located above the kidneys. [8] Abiraterone Acetate may also act as a hormone antagonist of androgens through its action as a CYP17 inhibitor. [9] Abarelix, a GnRH antagonist may also be used for the treatment of prostate cancer. [10]

References

  1. 1 2 Bolander, Franklyn F. (1 January 2004), Bolander, Franklyn F. (ed.), "CHAPTER 8 - Receptor Regulation" , Molecular Endocrinology (Third Edition), San Diego: Academic Press, pp. 215–232, doi:10.1016/b978-012111232-5/50008-7, ISBN   978-0-12-111232-5 , retrieved 5 May 2025
  2. 1 2 Ge, Xuecai; Yang, Hong; Bednarek, Maria A.; Galon-Tilleman, Hadas; Chen, Peirong; Chen, Michael; Lichtman, Joshua S.; Wang, Yan; Dalmas, Olivier; Yin, Yiyuan; Tian, Hui; Jermutus, Lutz; Grimsby, Joseph; Rondinone, Cristina M.; Konkar, Anish (6 February 2018). "LEAP2 Is an Endogenous Antagonist of the Ghrelin Receptor". Cell Metabolism. 27 (2): 461–469.e6. doi: 10.1016/j.cmet.2017.10.016 . ISSN   1932-7420. PMID   29233536.
  3. ↑ Malik, Muhammad Arshad; Nadeem, Muhammad Shahid (1 January 2023), Kazmi, Imran; Karmakar, Sanmoy; Shaharyar, Md. Adil; Afzal, Muhammad (eds.), "Chapter 6 - Molecular mechanism of action of estrogens, progestins, and androgens" , How Synthetic Drugs Work, Academic Press, pp. 123–159, doi:10.1016/b978-0-323-99855-0.00006-3, ISBN   978-0-323-99855-0 , retrieved 5 May 2025
  4. ↑ Patel, Preeti; Jacobs, Tibb F. (2025), "Tamoxifen", StatPearls, Treasure Island (FL): StatPearls Publishing, PMID   30422500 , retrieved 5 May 2025
  5. 1 2 "Aromatase Inhibitors". my.clevelandclinic.org. Retrieved 4 May 2025.
  6. 1 2 Chan, Hei Jason; Petrossian, Karineh; Chen, Shiuan (July 2016). "Structural and functional characterization of aromatase, estrogen receptor, and their genes in endocrine-responsive and -resistant breast cancer cells". The Journal of Steroid Biochemistry and Molecular Biology. 161: 73–83. doi:10.1016/j.jsbmb.2015.07.018. ISSN   1879-1220. PMC   4752924 . PMID   26277097.
  7. ↑ Michaud, Jason E.; Billups, Kevin L.; Partin, Alan W. (December 2015). "Testosterone and prostate cancer: an evidence-based review of pathogenesis and oncologic risk". Therapeutic Advances in Urology. 7 (6): 378–387. doi:10.1177/1756287215597633. ISSN   1756-2872. PMC   4647137 . PMID   26622322.
  8. ↑ "Hormone Therapy for Prostate Cancer". www.cancer.org. Retrieved 5 May 2025.
  9. ↑ Attard, Gerhardt; Reid, Alison H.M.; A'Hern, Roger; Parker, Christopher; Oommen, Nikhil Babu; Folkerd, Elizabeth; Messiou, Christina; Molife, L. Rhoda; Maier, Gal; Thompson, Emilda; Olmos, David; Sinha, Rajesh; Lee, Gloria; Dowsett, Mitch; Kaye, Stan B. (10 August 2009). "Selective Inhibition of CYP17 With Abiraterone Acetate Is Highly Active in the Treatment of Castration-Resistant Prostate Cancer". Journal of Clinical Oncology. 27 (23): 3742–3748. doi:10.1200/JCO.2008.20.0642. ISSN   0732-183X.
  10. ↑ Mongiat-Artus, Pierre; Teillac, Pierre (1 October 2004). "Abarelix: the first gonadotrophin-releasing hormone antagonist for the treatment of prostate cancer". Expert Opinion on Pharmacotherapy. 5 (10): 2171–2179. doi:10.1517/14656566.5.10.2171. ISSN   1465-6566. PMID   15461552.
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