| Autor: |
Trepanier DJ; Isotechnika Inc., Edmonton, Alberta, Canada., Abel MD, Freitag DG, Yatscoff RW |
| Jazyk: |
angličtina |
| Zdroj: |
Therapeutic drug monitoring [Ther Drug Monit] 1999 Jun; Vol. 21 (3), pp. 274-80. |
| DOI: |
10.1097/00007691-199906000-00003 |
| Abstrakt: |
Electrospray ionization mass spectrometry was used to study several non-covalent FK-binding protein (FKBP) immunosuppressant complexes in the gas phase. Relative FKBP binding affinities were determined from the signal ratio for the 7+ charge states of bound and unbound complexes as a function of capillary exit voltage. All complexes displayed a 1:1 binding stoichiometry. The relative gas-phase binding affinities were found to be well correlated with in vitro FKBP binding and in vitro immunosuppression (rapamycin > FK506 > or = 31-demethyl FK506 > 13-demethyl FK506 >> Cyclosporin A; CsA). The method demonstrates potential as a simple, rapid, and automatable technique for prediction of the immunosuppressive activity of FKBP:drug complexes. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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