Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay
G M Dubowchik1, J L Ditta, J J Herbst
1Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492-7660, USA. gene.dubowchik@bms.com
Bioorganic & Medicinal Chemistry Letters
|March 31, 2000
Abstract:
Several fluoresceinated FKBP12 ligands have been prepared for a high-throughput fluorescence polarization assay. K(i)s for FKBP12 rotamase inhibition by these ligands range from 1.3 microM to 32 nM, and their design is based on X-ray crystal structures of FKBP12 complexed with known immunophilin ligands.
