TY - JOUR

T1 - Recent Advances in the Medicinal Chemistry of Liver X Receptors

AU - El-Gendy, Bahaa El Dien M.

AU - Goher, Shaimaa S.

AU - Hegazy, Lamees S.

AU - Arief, Mohamed M.H.

AU - Burris, Thomas P.

N1 - Publisher Copyright: © Copyright 2018 American Chemical Society.

PY - 2018/12/27

Y1 - 2018/12/27

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=85050034921&partnerID=8YFLogxK

U2 - 10.1021/acs.jmedchem.8b00045

DO - 10.1021/acs.jmedchem.8b00045

M3 - Review article

C2 - 30004226

AN - SCOPUS:85050034921

SN - 0022-2623

VL - 61

SP - 10935

EP - 10956

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 24

ER -