STUDIES ON NONCOVALENT ASSOCIATIONS OF IMMUNOSUPPRESSIVE DRUGS WITH SERUM-ALBUMIN USING PNEUMATICALLY ASSISTED ELECTROSPRAY-IONIZATION MASS-SPECTROMETRY

被引:18
作者
BAKHTIAR, R
STEARNS, RA
机构
[1] Department of Drug Metabolism (I), Merck Research Laboratories, Rahway, New Jersey, 07065-0900
关键词
D O I
10.1002/rcm.1290090313
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Pneumatically assisted electrospray ionization (ion-spray) mass spectrometry was employed in the detection of non-covalent interactions of inmunosuppressive drugs with proteins. Non-covalent complexes of albumin (rat and bovine) with FK506, dihydro-FK506, and FK520 were observed. No complexation was detected between albumin and cyclosporin A (CsA), even at a protein-ligand molar ratio of 1:20. It is suggested that the lack of detection of an albumin-CsA non covalent complex may be attributed to dissociation of the weakly associated species during ion vaporization. Nonetheless, preliminary results indicate that ion-spray mass spectrometry has potential in qualitative evaluation of drug-plasma protein interaction.
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页码:240 / 244
页数:5
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