Lipid Homeostasis and Ligands for Liver X Receptors: Identification and Characterization

2016 ◽  
pp. 13-19 ◽  
Author(s):  
Jean-Marc A. Lobaccaro ◽  
Claude Beaudoin ◽  
Bagora Bayala ◽  
Silvère Baron ◽  
Amalia Trousson
Keyword(s):  
Lipid Homeostasis ◽  
Liver X Receptors ◽  
X Receptors ◽  
Identification And Characterization

scholarly journals Development of Agonist-Based PROTACs Targeting Liver X Receptor

2021 ◽  
Vol 9 ◽  
Author(s):  
Hanqiao Xu ◽  
Nobumichi Ohoka ◽  
Hidetomo Yokoo ◽  
Kanako Nemoto ◽  
Takashi Ohtsuki ◽  
...  
Keyword(s):  
Ubiquitin Proteasome System ◽  
Nuclear Hormone Receptor ◽  
Cholesterol Homeostasis ◽  
Lipid Homeostasis ◽  
Liver X Receptors ◽  
Ubiquitin Proteasome ◽  
Antagonists And Inhibitors ◽  
X Receptors ◽  
And Function ◽  
Complementary Strategy

Liver X receptors (LXRs) belong to the nuclear hormone receptor superfamily and function as ligand-dependent transcription factors that regulate cholesterol homeostasis, lipid homeostasis, and immune responses. LXR antagonists are promising treatments for hypercholesterolemia and diabetes. However, effective LXR antagonists and inhibitors are yet to be developed. Thus, we aimed to develop LXR degraders (proteolysis targeting chimeras PROTACs against LXR) as a complementary strategy to provide a similar effect to LXR inhibition. In this study, we report the development of GW3965-PEG5-VH032 (3), a PROTAC capable of effectively degrading LXRβ protein. Compound 3 induced the ubiquitin-proteasome system-dependent degradation of the LXRβ protein, which requires VHL E3 ligase. We hope that PROTACs targeting LXR proteins will become novel therapeutic agents for LXR-related diseases.

scholarly journals Liver X receptors in the central nervous system: From lipid homeostasis to neuronal degeneration

2002 ◽  
Vol 99 (21) ◽  
pp. 13878-13883 ◽  
Author(s):  
L. Wang ◽  
G. U. Schuster ◽  
K. Hultenby ◽  
Q. Zhang ◽  
S. Andersson ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Neuronal Degeneration ◽  
Lipid Homeostasis ◽  
Liver X Receptors ◽  
The Central Nervous System ◽  
X Receptors

Using integrative lipid systems biology to understand the role of Liver X receptors (LXRs) in male reproduction

2018 ◽  
Author(s):  
Sheba Jarvis ◽  
Lee Gethings ◽  
Raffaella Gadeleta ◽  
Emmanuelle Claude ◽  
Robert Winston ◽  
...  
Keyword(s):  
Systems Biology ◽  
Male Reproduction ◽  
Liver X Receptors ◽  
X Receptors

Chromene and chromone derivatives as liver X receptors modulators from a marine-derived Pestalotiopsis neglecta fungus

2021 ◽  
pp. 104927
Author(s):  
Zhi Liang ◽  
Tanwei Gu ◽  
Jianjiao Wang ◽  
Jianglian She ◽  
Yuxiu Ye ◽  
...  
Keyword(s):  
Liver X Receptors ◽  
Chromone Derivatives ◽  
X Receptors ◽  
Pestalotiopsis Neglecta

Regulation of glycolytic genes in human macrophages by oxysterols: a potential role for Liver X receptors Oxysterols modulate glycolysis in human macrophages

2020 ◽  
Author(s):  
Louise Ménégaut ◽  
Antoine Jalil ◽  
Thomas Pilot ◽  
Kevin Dongen ◽  
Valentin Crespy ◽  
...  
Keyword(s):  
Potential Role ◽  
Liver X Receptors ◽  
Human Macrophages ◽  
X Receptors

scholarly journals Cytoplasmic LXR expression is an independent marker of poor prognosis for patients with early stage primary breast cancer

2021 ◽  
Author(s):  
Wanting Shao ◽  
Christina Kuhn ◽  
Doris Mayr ◽  
Nina Ditsch ◽  
Magdalena Kailuwait ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Primary Breast Cancer ◽  
Poor Prognosis ◽  
Early Stage ◽  
Clinicopathological Characteristics ◽  
Clinicopathological Parameters ◽  
Liver X Receptors ◽  
X Receptors ◽  
Independent Marker ◽  
Overall Survival Analysis

Abstract Purpose The aim of this study was to investigate the expression of liver X receptors α/β (LXR) in primary breast cancer (BC) tissues and to analyze its correlations with clinicopathological parameters including patient survival. Methods In a well-characterized cohort of 305 primary BC, subcellular distribution of LXR was evaluated by immunohistochemistry. Correlations with clinicopathological characteristics as well as with patient outcome were analyzed. Results LXR was frequently localized in both nuclei and cytoplasms of BC cells, with stronger staining in nuclei. Total and nuclear LXR expression was positively correlated with ER and PR status. Overall survival analysis demonstrated that cytoplasmic LXR was significantly correlated with poor survival and appeared as an independent marker of poor prognosis, in stage I but not in stage II–III tumors Conclusion Altogether, these data suggest that cytoplasmic LXR could be defined as a prognostic marker in early stage primary BC.

scholarly journals Reciprocal Regulation of Hepatic and Adipose Lipogenesis by Liver X Receptors in Obesity and Insulin Resistance

2013 ◽  
Vol 18 (1) ◽  
pp. 106-117 ◽  
Author(s):  
Simon W. Beaven ◽  
Aleksey Matveyenko ◽  
Kevin Wroblewski ◽  
Lily Chao ◽  
Damien Wilpitz ◽  
...  
Keyword(s):  
Insulin Resistance ◽  
Liver X Receptors ◽  
Reciprocal Regulation ◽  
X Receptors
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