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Shedding light on the roles of liver X receptors in cancer by using chemical probes
Author(s) -
Pontini Lorenzo,
Marinozzi Maura
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.15200
Subject(s) - liver x receptor , nuclear receptor , liver cancer , receptor , cancer , biology , energy homeostasis , cancer research , biochemistry , genetics , transcription factor , gene
Nuclear receptors, liver X receptor-α (LXRα; NR1H3) and liver X receptor-β (LXRβ; NR1H2), are considered master regulators of lipid homeostasis. During the last couple of decades, their pivotal roles in several physiological and pathological processes ranging from energy supply, immunity, cardiovascular, neurodegenerative disorders and cancer have been highlighted. In this review, the main results achieved during more recent years about our understanding of the LXR involvement in cancer has been mainly obtained using small-molecule chemical probes. Remarkably, all these probes, albeit having different structure and biological properties, have a well demonstrated anti-tumoral activity arising from LXR modulation, indicating a high potential of LXR targeting for the treatment of cancer. 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.