Therapeutic potential for clomiphene, a selective estrogen receptor modulator, in the treatment of COVID‐19

Ghasemnejad‐Berenji, Morteza; Pashapour, Sarvin; Ghasemnejad‐Berenji, Hojat

doi:10.1016/j.mehy.2020.110354

Cited by 16 publications

(15 citation statements)

References 11 publications

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“…Sorafenib is a protein kinase inhibitor with activity against the Raf/Mek/Erk pathway [Liu et al, 2006]. Several authors have explored the role of MAP Kinase signalling pathway in the coronavirus family at large [Cai et al, 2007] and for SARS-cov2 in particular [Hemmat et al, 2021], [Ghasemnejad-Berenji and Pashapour, 2021], and [Zhou et al, 2020a].…”

Section: Drugmerge Results On Covid-19mentioning

confidence: 99%

Drug Repositioning by Merging Active Subnetworks Validated in Cancer and COVID-19

Lucchetta

Pellegrini

2021

Preprint

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Computational Drug Repositioning aims at ranking and selecting existing drugs for use in novel diseases or existing diseases for which these drugs were not originally designed. Using vast amounts of available omic data in digital form within an in silico screening has the potential for speeding up considerably the shortlisting of promising candidates in response to outbreaks of diseases such as COVID-19 for which no satisfactory cure has yet been found. We describe DrugMerge as a methodology for preclinical computational drug repositioning based on merging multiple drug rankings obtained with an ensemble of Disease Active Subnetwork construction algorithms. DrugMerge uses differential transcriptomic data from cell lines/tissues of patients affected by the disease and differential transcriptomic data from drug perturbation assays, in the context of a large gene co-expression network. Experiments with four benchmark diseases (Asthma, Rheumatoid Arthritis, Prostate Cancer, and Colorectal Cancer) demonstrate that our method detects in first position drugs in clinical use for the specified disease, in all four cases. Our method is competitive with the state-of-the-art tools such as CMAP (Connectivity Map). Application of DrugMerge to COVID-19 data found rankings with many drugs currently in clinical trials for COVID-19 in top positions, thus showing that DrugMerge is able to mimic human expert judgment

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Section: Drugmerge Results On Covid-19mentioning

confidence: 99%

Drug Repositioning by Merging Active Subnetworks Validated in Cancer and COVID-19

Lucchetta

Pellegrini

2021

Preprint

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“…Clomiphene is primarily used to treat female infertility due to anovulation and acts as both an estrogenic agonist and antagonist ( 59 ). Clomiphene may inhibit SARS-CoV-2 entry by impairing endosome/lysosome function ( 60 ) ( Table 1 ).…”

Section: Effect Of Serms On Sars-cov-2 Infection In Breast Cancermentioning

confidence: 99%

Estrogen and Estrogen Receptor Modulators: Potential Therapeutic Strategies for COVID-19 and Breast Cancer

Yin

Nie

et al. 2022

Front. Endocrinol.

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Owing to the ongoing coronavirus disease 2019 (COVID-19) pandemic, we need to pay a particular focus on the impact of coronavirus infection on breast cancer patients. Approximately 70% of breast cancer patients express estrogen receptor (ER), and intervention therapy for ER has been the primary treatment strategy to prevent the development and metastasis of breast cancer. Recent studies have suggested that selective estrogen receptor modulators (SERMs) are a potential therapeutic strategy for COVID-19. With its anti-ER and anti-viral combined functions, SERMs may be an effective treatment for COVID-19 in patients with breast cancer. In this review, we explore the latent effect of SERMs, especially tamoxifen, and the mechanism between ER and virus susceptibility.

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“…These mechanisms were also dependent on the interaction of hormones with their receptors. The inhibitory effect of estrogens on replication was documented [ 36 , 37 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 ]. in a panel of viruses (for particulars see Table 1 ).…”

Section: Effect Of Oestrogen Receptor Modulators (Erms) On Viral Replicationmentioning

confidence: 99%

“…Unfortunately, the precise molecular mechanisms of action were deciphered only in a few cases and are usually independent of the interaction with the receptor. Clomifene, raloxifene, ridaifene (+XL-147) and toremifene act via attenuation of the interaction of SARS−CoV−2 or EBOLA with their target cells [ 37 , 40 , 41 , 42 , 43 , 44 ], where some role of the inhibition of SARS−CoV−2 spike protein interaction with receptor ACE2 may be expected [ 36 , 37 , 39 , 44 , 45 , 67 ]. ERMs seem to inhibit the glycan–glycan interaction between the spike protein and ACE2 and so reduces the virus entry to permissive cells [ 43 , 68 ].…”

Section: Effect Of Oestrogen Receptor Modulators (Erms) On Viral Replicationmentioning

confidence: 99%

See 1 more Smart Citation

Estrogen Receptor Modulators in Viral Infections Such as SARS−CoV−2: Therapeutic Consequences

Abramenko

Vellieux

Tesařová

et al. 2021

IJMS

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COVID−19 is a pandemic respiratory disease caused by the SARS−CoV−2 coronavirus. The worldwide epidemiologic data showed higher mortality in males compared to females, suggesting a hypothesis about the protective effect of estrogens against severe disease progression with the ultimate end being patient’s death. This article summarizes the current knowledge regarding the potential effect of estrogens and other modulators of estrogen receptors on COVID−19. While estrogen receptor activation shows complex effects on the patient’s organism, such as an influence on the cardiovascular/pulmonary/immune system which includes lower production of cytokines responsible for the cytokine storm, the receptor-independent effects directly inhibits viral replication. Furthermore, it inhibits the interaction of IL−6 with its receptor complex. Interestingly, in addition to natural hormones, phytestrogens and even synthetic molecules are able to interact with the estrogen receptor and exhibit some anti-COVID−19 activity. From this point of view, estrogen receptor modulators have the potential to be included in the anti-COVID−19 therapeutic arsenal.

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Therapeutic potential for clomiphene, a selective estrogen receptor modulator, in the treatment of COVID‐19

Cited by 16 publications

References 11 publications

Drug Repositioning by Merging Active Subnetworks Validated in Cancer and COVID-19

Drug Repositioning by Merging Active Subnetworks Validated in Cancer and COVID-19

Estrogen and Estrogen Receptor Modulators: Potential Therapeutic Strategies for COVID-19 and Breast Cancer

Estrogen Receptor Modulators in Viral Infections Such as SARS−CoV−2: Therapeutic Consequences

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