Dual-target inhibitors based on ERα: Novel therapeutic approaches for endocrine resistant breast cancer

Xiong, Shuangshuang; Song, Ke; Xiang, Hua; Luo, Guoshun

doi:10.1016/j.ejmech.2024.116393

Cited by 2 publications

(1 citation statement)

References 184 publications

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“…ERα is antagonized by selective estrogen receptor modulators or degraders. Because of hormonal resistance, dual target inhibitors are also seen as a possibility [ 98 ].…”

Section: Discussionmentioning

confidence: 99%

A Narrative Review of the Role of Estrogen (Receptors) in Melanoma

Caerts,

Garmyn,

Güvenç

2024

IJMS

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In this narrative review, we attempt to provide an overview of the evidence regarding the role of estrogen (receptors) in cutaneous melanoma (CM). We reviewed 68 studies and 4 systematic reviews and meta-analyses published from 2002 up to and including 2022. The prevailing presence of estrogen receptor β (ERβ) instead of estrogen receptor α (ERα) in CM is notable, with ERβ potentially playing a protective role and being less frequently detected in progressive cases. While men with CM generally experience a less favorable prognosis, this distinction may become negligible with advancing age. The role of oral contraceptives (OC) and hormone replacement therapy (HRT) in CM remains controversial. However, recent studies tend to associate the use of these exogenous hormones with a heightened risk of CM, mostly only when using estrogen therapy and not in combination with progesterone. On the contrary, the majority of studies find no substantial influence of in vitro fertilization (IVF) treatment on CM risk. Reproductive factors, including younger age at first childbirth, higher parity, and shorter reproductive life, show conflicting evidence, with some studies suggesting a lower CM risk. We suggest an important role for estrogens in CM. More research is needed, but the integration of estrogens and targeting the estrogen receptors in melanoma therapy holds promise for future developments in the field.

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“…ERα is antagonized by selective estrogen receptor modulators or degraders. Because of hormonal resistance, dual target inhibitors are also seen as a possibility [ 98 ].…”

Section: Discussionmentioning

confidence: 99%

A Narrative Review of the Role of Estrogen (Receptors) in Melanoma

Caerts,

Garmyn,

Güvenç

2024

IJMS

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Cancer Cells Show Higher Sensitivity to Melatonin-Tamoxifen Drug Conjugates than to Combination of Melatonin and Tamoxifen

Marzouk,

Greco,

Gbahou

et al. 2024

ACS Omega

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Drug conjugates of tamoxifen and melatonin linked through the amide side chain of melatonin (4a,4b) were reported as promising agents for future treatment of breast cancer, possibly reversing the adverse effects of tamoxifen. Here, we report the synthesis and pharmacological evaluation of a novel series of anticancer drug conjugates linking melatonin with tamoxifen through polymethylene spacers through the ether oxygen of melatonin (16a−c, 19a−c, 21) and compare them to the previously reported amide-linked analogues 4a and 4b. All hybrid ligands are antagonists of estrogen receptor alpha and agonists of the melatonin MT 1 receptor with variable potencies. Several drug conjugates including the (CH 2 ) 4 -linked analogues 4a and 16a and the (CH 2 ) 6 -linked compound 16c showed higher potency to inhibit cell viability than the combination of melatonin and tamoxifen on at least one cancer cell line including MCF-7, MDA-MB-231, and HT-1080.

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Dual-target inhibitors based on ERα: Novel therapeutic approaches for endocrine resistant breast cancer

Cited by 2 publications

References 184 publications

A Narrative Review of the Role of Estrogen (Receptors) in Melanoma

A Narrative Review of the Role of Estrogen (Receptors) in Melanoma

Cancer Cells Show Higher Sensitivity to Melatonin-Tamoxifen Drug Conjugates than to Combination of Melatonin and Tamoxifen

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