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Discovery of a Potent, Orally Available, and Isoform-Selective Retinoic Acid β2 Receptor Agonist
Ist Teil von
Journal of medicinal chemistry, 2005-12, Vol.48 (24), p.7517-7519
Ort / Verlag
Washington, DC: American Chemical Society
Erscheinungsjahr
2005
Quelle
Alma/SFX Local Collection
Beschreibungen/Notizen
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, poorly soluble hit into a more potent and orally available compound (2, AC-261066) with retained β2 selectivity and greatly improved physiochemical properties. Being an isoform-selective RARβ2 receptor agonist that discriminates between nuclear receptor isoforms having identical ligand binding domains, 2 will be useful as a pharmacological research tool but also a valuable starting point for drug development.