[HTML][HTML] Identification of a novel class of retinoic acid receptor β-selective retinoid antagonists and their inhibitory effects on AP-1 activity and retinoic acid-induced …
Y Li, Y Hashimoto, A Agadir, H Kagechika… - Journal of Biological …, 1999 - ASBMB
Four candidate retinoid antagonists (LE135, LE511, LE540, and LE550) were designed on
the basis of the ligand superfamily concept and synthesized. Analysis of these related
retinoids by transient transfection assay demonstrated that LE135, LE540, and LE550 are
effective retinoic acid receptor (RAR) antagonists, whereas LE511 selectively induced RARβ
transcriptional activity. Both LE135 and LE540 inhibited retinoic acid (RA)-induced
transcriptional activation of RARβ, but not RARα, RARγ or retinoid X receptor α (RXRα), on a …
the basis of the ligand superfamily concept and synthesized. Analysis of these related
retinoids by transient transfection assay demonstrated that LE135, LE540, and LE550 are
effective retinoic acid receptor (RAR) antagonists, whereas LE511 selectively induced RARβ
transcriptional activity. Both LE135 and LE540 inhibited retinoic acid (RA)-induced
transcriptional activation of RARβ, but not RARα, RARγ or retinoid X receptor α (RXRα), on a …