Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist.

@article{Lund2005DiscoveryOA,
  title={Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist.},
  author={B. W. Lund and F. Piu and N. Gauthier and Anne Eeg and E. Currier and V. Sherbukhin and M. Brann and U. Hacksell and R. Olsson},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 24},
  pages={
          7517-9
        }
}
  • B. W. Lund, F. Piu, +6 authors R. Olsson
  • Published 2005
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • 4'-Octyl-4-biphenylcarboxylic acid (1g, AC-55649) was identified as a highly isoform-selective agonist at the human RARbeta2 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 beta2 selectivity and greatly improved physiochemical properties. Being an isoform-selective RARbeta2 receptor agonist that discriminates between… CONTINUE READING
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