Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.
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.
Dubowchik
G M
GM
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492-7660, USA. gene.dubowchik@bms.com
Ditta
J L
JL
Herbst
J J
JJ
Bollini
S
S
Vinitsky
A
A
D018360:Crystallography, X-Ray; D019793:Fluorescein / Q000737:chemistry; D016231:Fluorescence Polarization Immunoassay; D005456:Fluorescent Dyes / Q000138:chemical synthesis* / Q000494:pharmacology; D020104:Immunophilins / Q000737:chemistry*; D008024:Ligands; D011485:Protein Binding; D016559:Tacrolimus / Q000378:metabolism; D022021:Tacrolimus Binding Proteins
D005456:Fluorescent Dyes; D008024:Ligands; D022021:Tacrolimus Binding Proteins; D020104:Immunophilins; D019793:Fluorescein; D016559:Tacrolimus