Stereoselective synthesis and receptor activity of conformationally defined retinoid X receptor selective ligands

V Vuligonda; M E Garst; R A Chandraratna

doi:10.1016/s0960-894x(99)00048-7

Stereoselective synthesis and receptor activity of conformationally defined retinoid X receptor selective ligands

Bioorg Med Chem Lett. 1999 Feb 22;9(4):589-94. doi: 10.1016/s0960-894x(99)00048-7.

Authors

V Vuligonda¹, M E Garst, R A Chandraratna

Affiliation

¹ Retinoid Research, Department of Chemistry, Allergan Inc., Irvine, CA 92623, USA.

PMID: 10098670
DOI: 10.1016/s0960-894x(99)00048-7

Abstract

Retinoid X Receptor (RXR) specific ligands are currently being investigated for the treatment of metabolic diseases such as type II diabetes. We report the synthesis of conformationally locked retinoids, which are potent RXR selective ligands, and the attempted synthesis of 9-cyclopropyl locked analogs of RA and 9-cis RA.

MeSH terms

Binding Sites
Ligands
Protein Conformation
Receptors, Retinoic Acid / metabolism*
Retinoid X Receptors
Retinoids / chemical synthesis*
Retinoids / chemistry
Retinoids / metabolism
Stereoisomerism
Transcription Factors / metabolism*

Substances

Ligands
Receptors, Retinoic Acid
Retinoid X Receptors
Retinoids
Transcription Factors