Wan-Ru Chao

TL;DR: The pharmacophoric groups necessary to confer RXR selectivity were established by evaluating the ability of 21 conformationally restricted retinoids to activate the TREpal retinoic acid receptor response element for gene transcription in the presence of one of the three RAR subtypes or RXR alpha.

TL;DR: Results suggest that RAR alpha is the retinoid receptor involved in the inhibition of adherent cell growth by retinoids and that transcriptional activation by this receptor on a RAR response element does not appear to be required for this process to occur.

TL;DR: Comparison of the conformers of these analogues generated by molecular mechanics calculations with the biological activity profiles of these compounds indicates that geometric constraints required for high biological activity are imposed on the bridge joining the two aromatic ring systems by the retinoid receptor.

TL;DR: Fragment-based QSAR analyses relating the polar termini with cancer cell growth inhibition revealed that length and van der Waals electrostatic surface potential were the most influential features on activity.

TL;DR: Retinoic acid, 7, 13, 14, and 19 inhibited papilloma tumor formation in mice, and toxicity testing indicated that 7 was more toxic than 1, 13 and 14 were less toxic than 2, and 13 and 13 were less Toxic than 1.