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For the reference compound, conjugation of the racemic 2-fluoropropionate resulted in the formation of two epimeres, which could be separated by HPLC and tested for binding affinity separately (see below).
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Glutathione S-transferase T2 (GSTT2) is involved in cellular defence against toxic and carcinogenic electrophilic compounds by conjugation of reduced glutathione to hydrophobic electrophiles [ 41], so it was a logical finding that GSTT2 was up-regulated in response to BaP exposure.
The glutathione S-transferase MGST1 is also involved in cellular defence against toxic and carcinogenic electrophilic compounds by conjugation of reduced glutathione to hydrophobic electrophiles [ 23], so it is no surprise that this gene is up-regulated in response to BaP exposure.
Surprisingly, atips1 differed from the wild-type only for the content of myo-inositol and galactinol, a compound synthesised by conjugation of UDP-galactose and myo-inositol [33] (Figure 5A); we did not observe significant changes in glucose or sucrose accumulation.
GSTs are involved in the metabolism of a wide range of xenobiotic compounds by catalyzing the conjugation of these compounds with glutathione (Armstrong 1991).
Among these novel agents are hybrid bifunctional drugs, i.e. compounds resulting by conjugation of different drugs or containing the pharmocophores of different drugs.
In addition, lipid conjugation of the compound can provide a reservoir in the lungs allowing for a slow release of active compound (Berger 2005).
Different strategies have been suggested for the conjugation of cytotoxic compounds to antibodies.
They catalyze the conjugation of these compounds with glutathione, which can then be excreted (Hayes and Pulford 1995 ).
While conjugation of xenobiotic compounds with amino acids is a common phenomenon [ 68], the formation of a conjugate with malic acid was intriguing.
GSTs are generally recognized as detoxifying enzymes by catalyzing the conjugation of these compounds with glutathione, but they may also be involved in activation of some carcinogens.
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