Nuclear receptors (NRs) are one of the most abundant classes of transcriptional regulators in animals. These receptors regulate diverse biological functions, including homeostasis, reproduction, development, and metabolism in normal as well as in pathological settings. The liver X receptors (LXRs) are NRs that act as oxysterol sensors, regulating genes involved in cholesterol and lipid metabolism. The primary role of the liver X receptors (LXRs) is the regulation of cellular and serum cholesterol and lipid concentrations. Because of this function, there are self-evident reasons that novel ligands are being developed to target LXRs for new treatments of atherosclerosis. More recently, the LXRs have been shown to play roles in several important diseases, including cancers (principally colorectal, breast, and prostate), Alzheimer’s disease, and diabetes. Thus, as these protein receptors are important mediators of metabolic functions and diseases, the LXRs have become the objects of intensive scientific investigation and important targets in the development of novel ligands that can potentially serve as new therapeutics against many devastating diseases. In this study, we use computational chemistry methods, namely scaffold hopping and computational methyl scanning, in order to develop new ligands that bind to the LXRα receptor. We are also presenting the synthesis and biological studies of developed ligands.<br/>

Design, synthesis and bio evaluation of novel liver X receptor ligands

255th National Meeting (2018)

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