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Titolo:
ISOLATION, IDENTIFICATION AND IMMUNOSUPPRESSIVE ACTIVITY OF A NEW IMM-125 METABOLITE FROM HUMAN LIVER-MICROSOMES - IDENTIFICATION OF ITS CYCLOPHILIN-A IMM-125 METABOLITE COMPLEX BY NANOSPRAY TANDEM MASS-SPECTROMETRY
Autore:
LHOEST GJJ; DEJONG APJM; MEIRING HD; MATON N; LATINNE D; VERBEECK RK; OTTE JB; ZURINI M;
Indirizzi:
UNIV CATHOLIQUE LOUVAIN,DEPT PHARMACEUT SCI,PHARMACOKINET & METAB UNIT B-1200 BRUSSELS BELGIUM NATL INST PUBL HLTH & ENVIRONM,ANALYT CHEM LAB NL-3720 BA BILTHOVEN NETHERLANDS UNIV CATHOLIQUE LOUVAIN,EXPT IMMUNOL UNIT B-1200 BRUSSELS BELGIUM NOVARTIS PHARMA AG,LAB BIOMOL CH-4002 BASEL SWITZERLAND
Titolo Testata:
Journal of mass spectrometry
fascicolo: 10, volume: 33, anno: 1998,
pagine: 936 - 942
SICI:
1076-5174(1998)33:10<936:IIAIAO>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
SDZ IMM-125; CYCLOSPORINE; DISPOSITION; RATS;
Keywords:
DRUG METABOLISM; IMM-125 METABOLITE; CYCLOPHILIN A COMPLEX; IMMUNOSUPPRESSIVE ACTIVITY; DRUG-RECEPTOR INTERACTION; MASS SPECTROMETRY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
15
Recensione:
Indirizzi per estratti:
Citazione:
G.J.J. Lhoest et al., "ISOLATION, IDENTIFICATION AND IMMUNOSUPPRESSIVE ACTIVITY OF A NEW IMM-125 METABOLITE FROM HUMAN LIVER-MICROSOMES - IDENTIFICATION OF ITS CYCLOPHILIN-A IMM-125 METABOLITE COMPLEX BY NANOSPRAY TANDEM MASS-SPECTROMETRY", Journal of mass spectrometry, 33(10), 1998, pp. 936-942

Abstract

The isolation from human liver microsomes and identification by electrospray mass spectrometry and tandem mass spectrometry of a neat metabolite of IMM-125 resulting from the biotransformation of the amino acid I vinylic methyl group to a carboxylic acid, called the IMM-125-COOHmetabolite, is described. It was found that the complex of this new metabolite with cyclophilin A is formed less easily than the corresponding cyclophilin A-IMM-125-CH2OH main metabolite and cyclophilin A-IMM-125 complexes. However, when formed, the IMM-125-COOH metabolite-cyclophilin A complex requires more collision-induced dissociation (CID) todissociate the complex than the complexes formed with the two other ligands. The nanospray tandem mass spectrum of the IMM-125-COOH metabolite-cyclophilin A complex (m/z 1755) gives rise to cyclophiIin A-ligand complexes of m/z 1751 by elimination of CO2 and of m/z 1749 by loss of CO2 and H2O or glycerol. Since immunosuppressive activity is known to be dependent on the formation of a binary complex between cyclophilin A and the drug and since the target for the binary complex was found to be the calcium- and calmodulin-dependent protein phosphatase, calcineuria, it could be interesting to measure for structurally related immunosuppressive drugs the CID energy necessary to dissociate the binary complexes in order to evaluate whether a correlation with the phosphatase activity could be derived. (C) 1998 John Wiley & Sons, Ltd.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 06/04/20 alle ore 04:03:53