Searched for: subject%3A%22Drug%255C%2Bconjugation%22
(1 - 5 of 5)
document
de Koning, M.C. (author), van Grol, M. (author), Noort, D. (author)
Commonly employed pyridinium-oxime (charged) reactivators of nerve agent inhibited acetylcholinesterase (AChE) do not readily pass the blood brain barrier (BBB) because of the presence of charge(s). Conversely, non-ionic oxime reactivators often suffer from a lack of reactivating potency due to a low affinity for the active site of AChE. It was...
article 2011
document
Elliott, C.T. (author), Baxter, G.A. (author), Hewitt, S.A. (author), Arts, C.J.M. (author), van Baak, M. (author), Hellenäs, K.-E. (author), Johannson, A. (author), Centraal Instituut voor Voedingsonderzoek TNO (author)
The drug salbutamol (SBL) is a β-agonist that may be used illegally as an animal growth promoter. SBL is also a good example of a drug which is excreted in the form of glucuronides and sulfates. Such metabolites cause complexities in analysing for the presence of drug residues. In the majority of cases a process of deconjugation and sample clean...
article 1998
document
Centraal Instituut voor Voedingsonderzoek TNO (author), van Iersel, M.L.P.S. (author), van Lipzig, M.M.H. (author), Rietjens, I.M.C.M. (author), Vervoort, J. (author), van Bladeren, P.J. (author)
Using 1H NMR two diastereoisomers of the ethacrynic acid glutathione conjugate (EASG) as well as ethacrynic acid (EA) could be distinguished and quantified individually. Chemically prepared EASG consists of equal amounts of both diastereoisomers. GSTP1-1 stereospecifically catalyzes formation of one of the diastereoisomers (A). The GSTP1-1...
article 1998
document
Dirven, H.A.A.M. (author), Megens, L. (author), Oudshoorn, M.J. (author), Dingemanse, M.A. (author), van Ommen, B. (author), van Bladeren, P.J. (author), Instituut CIVO-Toxicologie en Voeding TNO (author)
Development of drug resistance against alkylating cytostatic drugs has been associated with higher intracellular concentrations of glutathione (GSH) and increased expression of glutathione S-transferase (GST) enzymes. Therefore, enhanced detoxification by the glutathione/glutathione S-transferase pathway has been proposed as a major factor in...
article 1995
document
Dirven, H.A.A.M. (author), Dictus, E.L.J.T. (author), Broeders, N.L.H.L. (author), van Ommen, B. (author), van Bladeren, P.J. (author), Instituut CIVO-Toxicologie en Voeding TNO (author)
Nonenzymatic and glutathione S-transferase (GST) catalyzed glutathione (GSH) conjugation has been postulated as a mechanism by which alkylating cytostatic drugs can be inactivated intracellularly. In this study, we describe studies on the glutathione-dependent biotransformation of thiotepa (tris(1-aziridinyl)phosphine sulfide), a trifunctional...
article 1995
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