870767-08-1Relevant articles and documents
Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor β ligands
Lund, Birgitte W.,Knapp, Anne Eeg,Piu, Fabrice,Gauthier, Natalie K.,Begtrup, Mikael,Hacksell, Uli,Olsson, Roger
supporting information; experimental part, p. 1540 - 1545 (2009/12/25)
We recently discovered the isoform selective RARβ2 ligand 4′-octyl-4-biphenylcarboxylic acid (3, AC-55649). Although 3 is highly potent at RARβ2 and displays excellent selectivity, solubility issues make it unsuitable for drug development. Herein we descr
Discovery of a potent, orally available, and isoform-selective retinoic acid β2 receptor agonist
Lund, Birgitte W.,Piu, Fabrice,Gauthier, Natalie K.,Eeg, Anne,Currier, Erika,Sherbukhin, Vladimir,Brann, Mark R.,Hacksell, Uli,Olsson, Roger
, p. 7517 - 7519 (2007/10/03)
4′-Octyl-4-biphenylcarboxylic acid (1g, AC-55649) was identified as a highly isoform-selective agonist at the human RARβ2 receptor in a functional intact cell-based screening assay. The subsequent hit to lead optimization transformed the lipophilic, poorl