Nuclear receptors (NRs) are one of the most abundant classes of transcriptional regulators in animals. The liver X receptors (LXRs) are NRs that act as oxysterol sensors, regulating genes involved in cholesterol and lipid metabolism. Based on the coding genes LXRs are classified as LXRα (NR1H3) and LXRβ (NRIH2). LXRα is expressed most highly in the liver and to a lesser extent in the kidney, small intestine, spleen, and adrenal gland. In contrast to the restricted expression pattern of LXRα, LXRβ is ubiquitously expressed. Concurrent with our increasing knowledge of the roles of LXRs in lipid homeostasis, development of selective and potent ligands of the hormone receptors has gained significant grounds toward clinical applications of LXR modulations. Here we are presenting our computational approach to develop a new series of LXR ligands based on scaffold replacement studies. We are also presenting the synthesis of a library of designed molecules and their biological evaluation studies towards LXR activity. <br/>

Design, synthesis and biological evaluation of Liver X Receptor (LXR) ligands

253rd National Meeting (2017)

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