Stereoselective synthesis and receptor activity of conformationally defined retinoid X receptor selective ligands.
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.
Vuligonda
V
V
Retinoid Research, Department of Chemistry, Allergan Inc., Irvine, CA 92623, USA.
Garst
M E
ME
Chandraratna
R A
RA
D001665:Binding Sites; D008024:Ligands; D011487:Protein Conformation; D018168:Receptors, Retinoic Acid / Q000378:metabolism*; D047488:Retinoid X Receptors; D012176:Retinoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D013237:Stereoisomerism; D014157:Transcription Factors / Q000378:metabolism*
D008024:Ligands; D018168:Receptors, Retinoic Acid; D047488:Retinoid X Receptors; D012176:Retinoids; D014157:Transcription Factors