Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives

Shagufta,; Ahmad, Irshad

doi:10.1016/j.ejmech.2017.11.056

Cited by 201 publications

(143 citation statements)

References 189 publications

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“…The vast majority (75%) of breast cancers are positive for hormonal receptors [95,96] . These molecular subtypes are sensible to endocrine therapy, thus the ER blocker Tamoxifen, is considered the first-line hormonal treatment for estrogen receptor positive (ER+) breast cancer [97,98] . Xu et al [99] described the lncRNA Urothelial cancer associated 1 (UCA1) as an exosomal transmitter of tamoxifen drug resistance in breast cancer.…”

Section: Hormone Therapymentioning

confidence: 99%

The role of exosomal long non-coding RNAs in cancer drug resistance

Santos

Dragomir

2019

CDR

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One of the major challenges in oncology is drug resistance, which triggers relapse and shortens patients' survival. In order to promote drug desensitization, cancer cells require the establishment of an ideal tumor microenvironment that accomplishes specific conditions. To achieve this objective, cellular communication is a key factor. Classically, cells were believed to restrictively communicate by ligand-receptor binding, physical cell-to-cell interactions and synapses. Nevertheless, the crosstalk between tumor cells and stroma cells has also been recently reported to be mediated through exosomes, the smallest extracellular vesicles, which transport a plethora of functionally active molecules, such as: proteins, lipids, messenger RNA, DNA, microRNA or long non-coding RNA (lncRNAs). LncRNAs are RNA molecules greater than 200 base pairs that are deregulated in cancer and other diseases. Exosomal lncRNAs are highly stable and can be found in several body fluids, being considered potential biomarkers for tumor liquid biopsy. Exosomal lncRNAs promote angiogenesis, cell proliferation and drug resistance. The role of exosomal lncRNAs in drug resistance affects the main treatment strategies in oncology: chemotherapy, targeted therapy, hormone therapy and immunotherapy. Overall, knowing the molecular mechanisms by which exosomal lncRNA induce pharmacologic resistance could improve further drug development and identify drug resistance biomarkers.

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Section: Hormone Therapymentioning

confidence: 99%

The role of exosomal long non-coding RNAs in cancer drug resistance

Santos

Dragomir

2019

CDR

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“…The SERMs were developed in the 1950s by the corporation that would become AstraZeneca when attempting to develop a postcoital contraceptive (Shagufta & Ahmad, ). Recognizing the potential of targeting estrogen receptor signaling in breast cancer, the company created tamoxifen, now the most commonly used drug for the treatment of estrogen receptor‐(ER) positive breast cancer.…”

Section: Selective Estrogen Receptor Modulators (Serms)mentioning

confidence: 99%

“…Tamoxifen has been shown to reduce the risk of recurrent breast cancer in women treated for ER‐positive disease as well as decrease overall breast cancer mortality. It also has antifungal and antiviral properties and can restrict angiogenesis and promote TGF‐β production, a cytokine that acts as a tumor suppressor particularly during the early stages of carcinogenesis (Shagufta & Ahmad, ).…”

Section: Selective Estrogen Receptor Modulators (Serms)mentioning

confidence: 99%

Repurposing existing medications in oncology and their potential role in oral cancer

Basile

Czerninski

2018

Oral Diseases

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“…Third-generation aromatase inhibitors (anastrozole, letrozole, and exemestane) are only used in postmenopausal patients, but can be used to replace TMX due to their better tolerability and safety. 1,6 Considering that 70% of the breast neoplasms are estrogen receptor-positive (ER þ ), the use of TMX is commonly recommended as the first choice hormonal therapy for breast cancer. 2,5,7 An important limitation to the use of TMX therapy is the development of drug resistance, which occurs in between 30 and 50% of the cases and may result from complex epigenetic mechanisms, response to stress, inhibition of Bcl-2 familyregulated apoptosis, autophagy, and pharmacologic mechanisms.…”

Section: Introductionmentioning

confidence: 99%

Impacts of Cytochrome P450 2D6 (CYP2D6) Genetic Polymorphism in Tamoxifen Therapy for Breast Cancer

Bezerra

Santos-Veloso

Bezerra

et al. 2018

Rev Bras Ginecol Obstet

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Tamoxifen (TMX) is the main drug used both in pre and postmenopausal women as adjuvant treatment for hormone receptor-positive breast cancer. An important barrier to the use of TMX is the development of drug resistance caused by molecular processes related to genetic and epigenetic mechanisms, such as the actions of cytochrome P450 2D6 (CYP2D6) polymorphisms and of its metabolites. The present study aimed to review recent findings related to the impact of CYP2D6 polymorphisms and how they can affect the results of TMX in breast cancer treatment. The keywords CYP2D6, tamoxifen, and breast cancer were searched in the PubMed, Scopus, The Cochrane Library, Scielo, and Bireme databases. Studies related to other types of neoplasms or based on other isoenzymes from cytochrome P450, but not on CYP2D6, were excluded. The impact of CYP2D6 polymorphisms in the TMX resistance mechanism remains unclear. The CYP2D6 gene seems to contribute to decreasing the efficacy of TMX, while the main mechanism responsible for therapy failure, morbidity, and mortality is the progression of the disease.

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Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives

Cited by 201 publications

References 189 publications

The role of exosomal long non-coding RNAs in cancer drug resistance

The role of exosomal long non-coding RNAs in cancer drug resistance

Repurposing existing medications in oncology and their potential role in oral cancer

Impacts of Cytochrome P450 2D6 (CYP2D6) Genetic Polymorphism in Tamoxifen Therapy for Breast Cancer

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