Distinct approaches of raloxifene: Its far-reaching beneficial effects implicating the ho-system

Denise Börzsei, Renáta Szabó, Alexandra Hoffmann, Médea Veszelka, Imre Pávó, Zsolt Turcsán, Csaba Viczián, Krisztina Kupai, Csaba Varga, Anikó Pósa

Research output: Contribution to journalReview article

Abstract

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.

Original languageEnglish
Article number375
JournalBiomolecules
Volume10
Issue number3
DOIs
Publication statusPublished - Mar 2020

Keywords

  • Antioxidant
  • Cardiometabolic
  • HO
  • HO-1
  • Neuroprotective
  • Raloxifene

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology

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    Börzsei, D., Szabó, R., Hoffmann, A., Veszelka, M., Pávó, I., Turcsán, Z., Viczián, C., Kupai, K., Varga, C., & Pósa, A. (2020). Distinct approaches of raloxifene: Its far-reaching beneficial effects implicating the ho-system. Biomolecules, 10(3), [375]. https://doi.org/10.3390/biom10030375