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J Steroid Biochem Mol Biol. 2021 Dec 14;217:106046. doi: 10.1016/j.jsbmb.2021.106046. Epub 2021 Dec 14.

Insights into estrogen receptor alpha modulation by cholestenoic acids.

The Journal of steroid biochemistry and molecular biology

María V Dansey, Marcos D Palavecino Ruiz, María F Ogara, Adalí Pecci, Gerardo Burton, Lautaro D Alvarez

Affiliations

  1. Universidad de Buenos Aires, Facultad de Ciencias Exactas y Naturales, Departamento de Química Biológica, Buenos Aires, Argentina; CONICET-Universidad de Buenos Aires, UMYMFOR, Buenos Aires, Argentina.
  2. CONICET-Universidad de Buenos Aires, IFIBYNE, Buenos Aires, Argentina.
  3. Universidad de Buenos Aires, Facultad de Ciencias Exactas y Naturales, Departamento de Química Biológica, Buenos Aires, Argentina; CONICET-Universidad de Buenos Aires, IFIBYNE, Buenos Aires, Argentina.
  4. Universidad de Buenos Aires, Facultad de Ciencias Exactas y Naturales, Departamento de Química Orgánica, Buenos Aires, Argentina; CONICET-Universidad de Buenos Aires, UMYMFOR, Buenos Aires, Argentina. Electronic address: [email protected].
  5. Universidad de Buenos Aires, Facultad de Ciencias Exactas y Naturales, Departamento de Química Biológica, Buenos Aires, Argentina; CONICET-Universidad de Buenos Aires, UMYMFOR, Buenos Aires, Argentina. Electronic address: [email protected].

PMID: 34920079 DOI: 10.1016/j.jsbmb.2021.106046

Abstract

Oxysterols are a family of over 25 cholesterol metabolites naturally produced by enzymatic or radical oxidation. They are involved in many physiological and pathological pathways. Although their activity has been mainly attributed to the modulation of the Liver X Receptors (LXR), it is currently accepted that oxysterols are quite promiscuous compounds, acting at several targets at the same time. The promiscuity of the oxysterols with the Estrogen Receptor α (ERα) is crucial in several pathologies such as ER

Copyright © 2021 Elsevier Ltd. All rights reserved.

Keywords: Cholestenoic acids; Estrogen receptor; Molecular dynamics simulation; Oxysterols

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