期刊
EXPERT OPINION ON THERAPEUTIC TARGETS
卷 15, 期 2, 页码 219-232出版社
TAYLOR & FRANCIS LTD
DOI: 10.1517/14728222.2011.547853
关键词
cancer; human diseases; LXR; nuclear receptors; pharmacology; reproduction
资金
- Association de Recherche sur les Tumeurs Prostatiques
- Ligue Allier contre le Cancer
- Fondation pour la Recherche Medicale (FRM)
- Fondation BNP-Paribas
- Region Auvergne
- Fond Europeen de DEveloppement Regional (FEDER)
- Ministry of Education, Research and Technology (MNERT)
- Algerian Government
Introduction: Liver X receptors (LXR) are transcription factors that belong to the nuclear receptor superfamily. Natural derivatives of cholesterol, known as oxysterols, have been identified as agonistic ligands of LXR. They are thus mainly considered to be intracellular cholesterol 'sensors' whose activation leads to decreased plasma cholesterol. Their implication in other physiologic processes currently prevents their use as therapeutic targets, because of potentially deleterious side effects. Areas covered: The various LXR agonists and antagonists, along with the physiological functions of LXR. Putative clinical targets including atherosclerosis, diabetes, Alzheimer's disease, skin disorders, reproductive disorders and cancer. Expert opinion: LXR are promising pharmacological targets because of the high potential to develop ligands owing to the variety of natural or synthetic agonists. Three aspects should be developed to select a LXR-ligand for treatment of human disease: bio-availability; isoform specificity; tissue specificity. This will allow the development of selective liver X modulators (SLiMs). The challenge is to overcome deleterious side effects to establish LXR as new pharmacological targets.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据