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

Article Details

Citation

Vuligonda V, Garst ME, Chandraratna RA

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

Bioorg Med Chem Lett. 1999 Feb 22;9(4):589-94.

PubMed ID
10098670 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TretinoinRetinoic acid receptor alphaKd (nM)15N/AN/ADetails
TretinoinRetinoic acid receptor alphaKd (nM)93N/AN/ADetails
TretinoinRetinoic acid receptor betaKd (nM)13N/AN/ADetails
TretinoinRetinoic acid receptor betaKd (nM)97N/AN/ADetails
TretinoinRetinoic acid receptor gammaKd (nM)18N/AN/ADetails
TretinoinRetinoic acid receptor gammaKd (nM)148N/AN/ADetails
TretinoinRetinoic acid receptor RXR-alphaKd (nM)>0.001N/AN/ADetails
TretinoinRetinoic acid receptor RXR-alphaKd (nM)8N/AN/ADetails
TretinoinRetinoic acid receptor RXR-betaKd (nM)>0.001N/AN/ADetails
TretinoinRetinoic acid receptor RXR-betaKd (nM)15N/AN/ADetails
TretinoinRetinoic acid receptor RXR-gammaKd (nM)>0.001N/AN/ADetails
TretinoinRetinoic acid receptor RXR-gammaKd (nM)14N/AN/ADetails