| Autor: |
Lund, B. W., Piu, F., Gauthier, N. K., Eeg, A., Currier, E., Sherbukhin, V., Brann, M. R., Hacksell, U., Olsson, R. |
| Zdroj: |
Journal of Medicinal Chemistry; December 2005, Vol. 48 Issue: 24 p7517-7519, 3p |
| Abstrakt: |
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. |
| Databáze: |
Supplemental Index |
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