Work

Recent Advances in the Medicinal Chemistry of Liver X Receptors

Year: 2018

Type: article

Abstract: Nuclear hormone receptors represent a large family of ligand-activated transcription factors that include steroid receptors, thyroid/retinoid receptors, and orphan receptors. Among nuclear hormone receptors, the liver X receptors have emerged as very important drug targets. These receptors regulate some of the most important metabolic functions, and they were also identified as anti-inflammatory transcription factors and regulators of the immune system. The development of drugs targeting liver X receptors continues to be a challenge, but advances in our knowledge of receptor structure and function move us forward, toward achieving this goal. This review highlights the latest advances in the development of synthetic LXR modulators in the primary literature from 2013 to 2017. In this review, we place great emphasis on the structure and function of LXRs because of their essential role in the drug design process. The structure-activity relationships of the most active and promising synthetic modulators are discussed.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.8b00045

Authors: Bahaa El-Dien M. El-Gendy, Shaimaa S. Goher, Lamees S. Hegazy, Mohamed M. H. Arief, Thomas P. Burris

Institutions: Benha University, Saint Louis University, University of Health Sciences and Pharmacy, Washington University in St. Louis

Language: English

Topic: Cholesterol and Lipid Metabolism

Subfield: Surgery

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: green

Funder: Science and Technology Development Fund