Anticancer Drug Conjugates Incorporating Estrogen Receptor Ligands

Hormone-dependent cancers, such as certain types of breast cancer are characterized by over-expression of estrogen receptors (ERs). Anticancer drug conjugates combining ER ligands with other classes of anticancer agents may not only benefit from dual action at both anti-cancer targets but also from...

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Bibliographic Details
Published in:Pharmaceutics 2022-12, Vol.15 (1), p.67
Main Authors: Zlotos, Darius P, Kronenberger, Thales, Laufer, Stefan A
Format: Article
Language:English
Subjects:
anticancer drug conjugates
Breast cancer
Cancer therapies
Cytotoxicity
Drug therapy
estrogen receptor ligands
Estrogens
Gene expression
Kinases
Ligands
Melatonin
Review
tumor targeting
Tumors
Uterus
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Summary:Hormone-dependent cancers, such as certain types of breast cancer are characterized by over-expression of estrogen receptors (ERs). Anticancer drug conjugates combining ER ligands with other classes of anticancer agents may not only benefit from dual action at both anti-cancer targets but also from selective delivery of cytotoxic agents to ER-positive tumor cells resulting in less toxicity and adverse effects. Moreover, they could also take advantage of overcoming resistance typical for anti-hormonal monotherapy such as tamoxifen. In this review, we discuss the design, structures and pharmacological effects of numerous series of drug conjugates containing ER ligands such as selective ER modulators (tamoxifen, 4-hydroxytamoxifen, endoxifen), selective ER degraders (ICI-164384) and ER agonists (estradiol) linked to diverse anti-cancer agents including histone-deacetylase inhibitors, DNA-alkylating agents, antimitotic agents and epidermal growth factor receptor inhibitors.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics15010067