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

2021 ◽  
Vol 22 (12) ◽  
pp. 6551
Author(s):  
Nikita Abramenko ◽  
Fréderic Vellieux ◽  
Petra Tesařová ◽  
Zdeněk Kejík ◽  
Robert Kaplánek ◽  
...  

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.

Biomolecules ◽  
2020 ◽  
Vol 10 (3) ◽  
pp. 375
Author(s):  
Denise Börzsei ◽  
Renáta Szabó ◽  
Alexandra Hoffmann ◽  
Médea Veszelka ◽  
Imre Pávó ◽  
...  

Selective estrogen receptor modulators (SERMs) were discovered in the mid-1900s in connection with estrogen-related pathological conditions. They were developed to antagonize the adverse effects of estrogen and have been shown to be effective against postmenopausal disorders manifested by estrogen deficiency. Raloxifene (RAL), one of the most widely used SERMs, expresses estrogen-like effects on bones, while it is found to be an antagonist on breast and uterus. RAL has multiple beneficial effects throughout the body, including antioxidant and anti-inflammatory properties, because of which it gains particular attention. Additionally, previous studies have revealed that RAL is an efficient modulator of heme-oxygenase (HO) expression. HO, through its general activity, participates in comprehensive cell defense processes, thus the induction of HO by RAL administration indicates a major role in its therapeutic efficacy. In this review, we compile the current knowledge about the overall metabolic, neurocognitive, and cardiovascular effects of RAL involving the cytoprotective HO-system.


Author(s):  
Carlo I. Rosales ◽  
Lauren M. Gutgesell ◽  
Kiira M. Ratia ◽  
Gregory R.J. Thatcher

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