Stereoselective synthesis and receptor activity of conformationally defined retinoid X receptor selective ligands.
Article Details
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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
Drug Target Property Measurement pH Temperature (°C) Tretinoin Retinoic acid receptor alpha Kd (nM) 15 N/A N/A Details Tretinoin Retinoic acid receptor alpha Kd (nM) 93 N/A N/A Details Tretinoin Retinoic acid receptor beta Kd (nM) 13 N/A N/A Details Tretinoin Retinoic acid receptor beta Kd (nM) 97 N/A N/A Details Tretinoin Retinoic acid receptor gamma Kd (nM) 18 N/A N/A Details Tretinoin Retinoic acid receptor gamma Kd (nM) 148 N/A N/A Details Tretinoin Retinoic acid receptor RXR-alpha Kd (nM) >0.001 N/A N/A Details Tretinoin Retinoic acid receptor RXR-alpha Kd (nM) 8 N/A N/A Details Tretinoin Retinoic acid receptor RXR-beta Kd (nM) >0.001 N/A N/A Details Tretinoin Retinoic acid receptor RXR-beta Kd (nM) 15 N/A N/A Details Tretinoin Retinoic acid receptor RXR-gamma Kd (nM) >0.001 N/A N/A Details Tretinoin Retinoic acid receptor RXR-gamma Kd (nM) 14 N/A N/A Details