Abstract:
:Previous investigations into the binding of substrates/cofactors to the PAH active site have only concentrated on Phe, thienylalanine and BH(4). This is the first reported investigation to model aliphatic thioether amino acid substrates to PAH. The clearance of the thioether substrates (4.82-79.09% of Phe) in the rat and human (1.19-37.41% of Phe) showed species differences. The xenobiotic thioether substrates (SMC and SCMC) were predicted to be poor substrates for PAH by the molecular modelling investigation and this has now been confirmed by the in vitro enzyme kinetic data. However, reaction phenotyping investigations have found that PAH was the major enzyme involved in the metabolism of SCMC in vitro and in vivo.
journal_name
J Enzyme Inhib Med Chemjournal_title
Journal of enzyme inhibition and medicinal chemistryauthors
Patel NG,Iliadou C,Boonyapiwat B,Barlow DJ,Forbes B,Mitchell SC,Steventon GBdoi
10.1080/14756360701810280subject
Has Abstractpub_date
2008-12-01 00:00:00pages
958-63issue
6eissn
1475-6366issn
1475-6374pii
788264435journal_volume
23pub_type
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