Anticancer Drugs That Modulate Hormone Action

Avendaño, Carmen; Menéndez, J. Carlos

doi:10.1016/b978-0-444-62649-3.00003-x

Cited by 10 publications

(6 citation statements)

References 105 publications

(66 reference statements)

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“…More specifically, testosterone and androstenedione are transformed into estradiol and estrone by aromatase, respectively [ 42 ]. This aromatization of androgens includes the creation of an aromatic A ring, which is one of the distinct characteristics of estrogens, via the deletion of the C-19 methyl group [ 43 ]. The mammary adipose tissue of normal breasts has a low aromatase level via the relatively weak aromatase promoter I.4, whereas malignant cells and adjacent fibroblasts show increased aromatase expression through the activation of promoters II and I.3 [ 14 , 44 , 45 ].…”

Section: The Role Of Estrogen and Aromatase In Breast Cancer Develmentioning

confidence: 99%

Melatonin as an Oncostatic Molecule Based on Its Anti-Aromatase Role in Breast Cancer

Jin¹,

Choi²,

Heo³

et al. 2021

IJMS

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Breast cancer is the most common type of cancer. In the developmental stages of breast cancer, estrogens are strongly involved. As estrogen synthesis is regulated by the enzyme aromatase, targeting the activity of this enzyme represents a therapeutic option. The pineal hormone melatonin may exert a suppressive role on aromatase activity, leading to reduced estrogen biosynthesis. A melatonin-mediated decrease in the expression of aromatase promoters and associated genes would provide suitable evidence of this molecule’s efficacy as an aromatase inhibitor. Furthermore, melatonin intensifies radiation-induced anti-aromatase effects and counteracts the unwanted disadvantages of chemotherapeutic agents. In this manner, this review summarizes the inhibitory role of melatonin in aromatase action, suggesting its role as a possible oncostatic molecule in breast cancer.

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Section: The Role Of Estrogen and Aromatase In Breast Cancer Develmentioning

confidence: 99%

Melatonin as an Oncostatic Molecule Based on Its Anti-Aromatase Role in Breast Cancer

Jin¹,

Choi²,

Heo³

et al. 2021

IJMS

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“…Cisplatin is a complex compound with a planar structure. It contains two chlorine atoms and two ammonia molecules, linked in a cis configuration to the platinum atom in the second oxidation state, by a coordination bond [21].…”

Section: The History Of Cisplatinmentioning

confidence: 99%

Cisplatin in Ovarian Cancer Treatment—Known Limitations in Therapy Force New Solutions

Zoń

Bednarek

2023

IJMS

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Cisplatin is one of the most commonly used anticancer drugs worldwide. It is mainly used in the treatment of ovarian cancer, but also used in testicular, bladder and lung cancers. The significant advantage of this drug is the multidirectional mechanism of its anticancer action, with the most important direction being damaging the DNA of cancer cells. Unfortunately, cisplatin displays a number of serious disadvantages, including toxicity to the most important organs, such as kidneys, heart, liver and inner ear. Moreover, a significant problem among patients with ovarian cancer, treated with cisplatin, is the development of numerous resistance mechanisms during therapy, including changes in the processes of cellular drug import and export, changes in the DNA damage repair mechanisms, as well as numerous changes in the processes of apoptosis and autophagy. Due to all of the mentioned problems, strategies to increase the effectiveness of cisplatin in the treatment of ovarian cancer are intensively sought. The most important strategy includes the development of less toxic cisplatin analogs. Another important direction is combination therapy, involving the simultaneous use of cisplatin with different anticancer drugs, substances derived from plants, temperature or radiotherapy. Many years of observations accompanying the presence of cisplatin in the therapy made it possible to provide a series of verifiable, statistically significant data, but also to show how, over time, with the new information and scientific discoveries, it is possible to describe and understand the therapeutic problems observed in practice, such as the acquisition of drug resistance by tumor cells or induction of changes in the tumor microenvironment. According to the authors, confronting what we knew so far with what new trends offer has a profound meaning. This paper presents information on the history of cisplatin and describes the molecular mechanisms of its action and the development of resistance by cancer cells. In addition, our goal was to highlight a number of therapeutic strategies to increase the effectiveness of cisplatin in the treatment of ovarian cancer, as well as to identify methods to eliminate problems associated with the use of cisplatin.

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“…Tamoxifen binds to and modifies the estrogen receptors (ERs) in cells. ERs play an important role in regulating processes, such as cell proliferation and differentiation, 30 with the result that over-expression of ERs is present in ∼70% of all breast cancers. 31 Therefore, tamoxifen is used extensively to treat ER+ breast cancers by blocking their growth.…”

Section: Fluorescent Label Synthesismentioning

confidence: 99%

Multimodal imaging needle combining optical coherence tomography and fluorescence for imaging of live breast cancer cells labeled with a fluorescent analog of tamoxifen

et al. 2022

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Significance: Imaging needles consist of highly miniaturized focusing optics encased within a hypodermic needle. The needles may be inserted tens of millimeters into tissue and have the potential to visualize diseased cells well beyond the penetration depth of optical techniques applied externally. Multimodal imaging needles acquire multiple types of optical signals to differentiate cell types. However, their use has not previously been demonstrated with live cells.Aim: We demonstrate the ability of a multimodal imaging needle to differentiate cell types through simultaneous optical coherence tomography (OCT) and fluorescence imaging.Approach: We characterize the performance of a multimodal imaging needle. This is paired with a fluorescent analog of the therapeutic drug, tamoxifen, which enables cell-specific fluorescent labeling of estrogen receptor-positive (ER+) breast cancer cells. We perform simultaneous OCT and fluorescence in situ imaging on MCF-7 ER+ breast cancer cells and MDA-MB-231 ER− cells. Images are compared against unlabeled control samples and correlated with standard confocal microscopy images.Results: We establish the feasibility of imaging live cells with these miniaturized imaging probes by showing clear differentiation between cancerous cells.Conclusions: Imaging needles have the potential to aid in the detection of specific cancer cells within solid tissue.

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Anticancer Drugs That Modulate Hormone Action

Cited by 10 publications

References 105 publications

Melatonin as an Oncostatic Molecule Based on Its Anti-Aromatase Role in Breast Cancer

Melatonin as an Oncostatic Molecule Based on Its Anti-Aromatase Role in Breast Cancer

Cisplatin in Ovarian Cancer Treatment—Known Limitations in Therapy Force New Solutions

Multimodal imaging needle combining optical coherence tomography and fluorescence for imaging of live breast cancer cells labeled with a fluorescent analog of tamoxifen

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