Targeting liver X receptors in cancer therapeutics

Chin Yo Lin; Jan Åke Gustafsson

doi:10.1038/nrc3912

Targeting liver X receptors in cancer therapeutics

Chin Yo Lin, Jan Åke Gustafsson

Research output: Contribution to journal › Review article › peer-review

144 Scopus citations

Abstract

Members of the nuclear receptor superfamily of ligand-dependent transcription factors carry out vital cellular functions and are highly druggable therapeutic targets. Liver X receptors (LXRs) are nuclear receptor family members that function in cholesterol transport, glucose metabolism and the modulation of inflammatory responses. There is now accumulating evidence to support the involvement of LXRs in a variety of malignancies and the potential efficacy of their ligands in these diseases. This Review summarizes the discovery and characterization of LXRs and their ligands, their effects and mechanisms in preclinical cancer models, and the future directions of basic and translational LXR research in cancer therapeutics.

Original language	English (US)
Pages (from-to)	216-224
Number of pages	9
Journal	Nature Reviews Cancer
Volume	15
Issue number	4
DOIs	https://doi.org/10.1038/nrc3912
State	Published - Apr 27 2015

ASJC Scopus subject areas

Oncology
Cancer Research

Access to Document

10.1038/nrc3912

Cite this

@article{cf3f262742894e229d8f11e57afa5c2f,

title = "Targeting liver X receptors in cancer therapeutics",

abstract = "Members of the nuclear receptor superfamily of ligand-dependent transcription factors carry out vital cellular functions and are highly druggable therapeutic targets. Liver X receptors (LXRs) are nuclear receptor family members that function in cholesterol transport, glucose metabolism and the modulation of inflammatory responses. There is now accumulating evidence to support the involvement of LXRs in a variety of malignancies and the potential efficacy of their ligands in these diseases. This Review summarizes the discovery and characterization of LXRs and their ligands, their effects and mechanisms in preclinical cancer models, and the future directions of basic and translational LXR research in cancer therapeutics.",

author = "Lin, {Chin Yo} and Gustafsson, {Jan {\AA}ke}",

note = "Funding Information: The authors thank X. Lou for preparing the image of the three-dimensional structure of the LXR–RXR heterodimer. This work was supported by grants to C.-Y.L. from Golfers Against Cancer and to J.-{\AA}.G. from the Emerging Technology Fund of Texas (agreement 300-9-1958), the Robert A. Welch Foundation (E-0004) and the Swedish Science Council. Publisher Copyright: {\textcopyright} 2015 Macmillan Publishers Limited. All rights reserved. Copyright: Copyright 2015 Elsevier B.V., All rights reserved.",

year = "2015",

month = apr,

day = "27",

doi = "10.1038/nrc3912",

language = "English (US)",

volume = "15",

pages = "216--224",

journal = "Nature Reviews Cancer",

issn = "1474-175X",

publisher = "Nature Publishing Group",

number = "4",

}

TY - JOUR

T1 - Targeting liver X receptors in cancer therapeutics

AU - Lin, Chin Yo

AU - Gustafsson, Jan Åke

N1 - Funding Information: The authors thank X. Lou for preparing the image of the three-dimensional structure of the LXR–RXR heterodimer. This work was supported by grants to C.-Y.L. from Golfers Against Cancer and to J.-Å.G. from the Emerging Technology Fund of Texas (agreement 300-9-1958), the Robert A. Welch Foundation (E-0004) and the Swedish Science Council. Publisher Copyright: © 2015 Macmillan Publishers Limited. All rights reserved. Copyright: Copyright 2015 Elsevier B.V., All rights reserved.

PY - 2015/4/27

Y1 - 2015/4/27

N2 - Members of the nuclear receptor superfamily of ligand-dependent transcription factors carry out vital cellular functions and are highly druggable therapeutic targets. Liver X receptors (LXRs) are nuclear receptor family members that function in cholesterol transport, glucose metabolism and the modulation of inflammatory responses. There is now accumulating evidence to support the involvement of LXRs in a variety of malignancies and the potential efficacy of their ligands in these diseases. This Review summarizes the discovery and characterization of LXRs and their ligands, their effects and mechanisms in preclinical cancer models, and the future directions of basic and translational LXR research in cancer therapeutics.

AB - Members of the nuclear receptor superfamily of ligand-dependent transcription factors carry out vital cellular functions and are highly druggable therapeutic targets. Liver X receptors (LXRs) are nuclear receptor family members that function in cholesterol transport, glucose metabolism and the modulation of inflammatory responses. There is now accumulating evidence to support the involvement of LXRs in a variety of malignancies and the potential efficacy of their ligands in these diseases. This Review summarizes the discovery and characterization of LXRs and their ligands, their effects and mechanisms in preclinical cancer models, and the future directions of basic and translational LXR research in cancer therapeutics.

UR - http://www.scopus.com/inward/record.url?scp=84925823298&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84925823298&partnerID=8YFLogxK

U2 - 10.1038/nrc3912

DO - 10.1038/nrc3912

M3 - Review article

C2 - 25786697

AN - SCOPUS:84925823298

SN - 1474-175X

VL - 15

SP - 216

EP - 224

JO - Nature Reviews Cancer

JF - Nature Reviews Cancer

IS - 4

ER -

Targeting liver X receptors in cancer therapeutics

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this