RXR-LXR heterodimer modulators for the potential treatment of dyslipidemia

Bharat Lagu; Barbara Pio; Rimma Lebedev; Maria Yang; Patricia D Pelton

doi:10.1016/j.bmcl.2007.01.047

RXR-LXR heterodimer modulators for the potential treatment of dyslipidemia

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3497-503. doi: 10.1016/j.bmcl.2007.01.047. Epub 2007 Jan 24.

Authors

Bharat Lagu¹, Barbara Pio, Rimma Lebedev, Maria Yang, Patricia D Pelton

Affiliation

¹ Johnson and Johnson Pharmaceutical Research and Development, Cranbury, NJ 08869, USA. blagu@prdus.jnj.com

PMID: 17485209
DOI: 10.1016/j.bmcl.2007.01.047

Abstract

A number of RXR agonists were synthesized and screened in functional assays. The synthesis and the structure-activity relationship (SAR) within the series of compounds will be presented. Some in vivo data in rodent models for dyslipidemia and diabetes will also be presented.

MeSH terms

Animals
DNA-Binding Proteins / agonists*
DNA-Binding Proteins / metabolism
Diabetes Mellitus / drug therapy*
Dimerization
Disease Models, Animal
Dyslipidemias / drug therapy*
Hypoglycemic Agents / chemical synthesis
Hypoglycemic Agents / pharmacology*
Hypoglycemic Agents / therapeutic use
Liver X Receptors
Orphan Nuclear Receptors
Rats
Rats, Sprague-Dawley
Receptors, Cytoplasmic and Nuclear / agonists*
Receptors, Cytoplasmic and Nuclear / metabolism
Retinoid X Receptors / agonists*
Retinoid X Receptors / metabolism
Structure-Activity Relationship

Substances

DNA-Binding Proteins
Hypoglycemic Agents
Liver X Receptors
Orphan Nuclear Receptors
Receptors, Cytoplasmic and Nuclear
Retinoid X Receptors