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Screening for liver X receptor modulators: Where are we and for what use?
Author(s) -
Buñay Julio,
Fouache Allan,
Trousson Amalia,
Joussineau Cyrille,
Bouchareb Erwan,
Zhu Zhekun,
Kocer Ayhan,
Morel Laurent,
Baron Silvere,
Lobaccaro JeanMarc A.
Publication year - 2021
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.15286
Subject(s) - liver x receptor , nuclear receptor , endocrine system , bioinformatics , receptor , biology , neuroscience , medicine , endocrinology , genetics , hormone , transcription factor , gene
Liver X receptors (LXRs) are members of the nuclear receptor superfamily that are canonically activated by oxidized derivatives of cholesterol. Since the mid-90s, numerous groups have identified LXRs as endocrine receptors that are involved in the regulation of various physiological functions. As a result, when their expression is genetically modified in mice, phenotypic analyses reveal endocrine disorders ranging from infertility to diabetes and obesity, nervous system pathologies such Alzheimer's or Parkinson's disease, immunological disturbances, inflammatory response, and enhancement of tumour development. Based on such findings, it appears that LXRs could constitute good pharmacological targets to prevent and/or to treat these diseases. This review discusses the various aspects of LXR drug discovery, from the tools available for the screening of potential LXR modulators to the current situational analysis of the drugs in development. LINKED ARTICLES: This article is part of a themed issue on Oxysterols, Lifelong Health and Therapeutics. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v178.16/issuetoc.