Screening for liver X receptor modulators: Where are we and for what use?
Julio BuñayAllan FouacheAmalia TroussonCyrille De JoussineauErwan BoucharebZhekun ZhuAyhan KocerLaurent MorelSilvère BaronJean Marc A LobaccaroPublished in: British journal of pharmacology (2020)
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.
Keyphrases
- drug discovery
- small molecule
- inflammatory response
- type diabetes
- high fat diet induced
- healthcare
- public health
- metabolic syndrome
- low density lipoprotein
- cardiovascular disease
- poor prognosis
- insulin resistance
- binding protein
- mental health
- genome wide
- human health
- weight loss
- adipose tissue
- toll like receptor
- physical activity
- dna methylation
- health information
- gene expression
- benign prostatic hyperplasia
- transcription factor
- risk assessment
- body mass index
- lower urinary tract symptoms
- wild type
- genome wide identification