Enzyme kinetic and molecular modelling studies of sulphur-containing substrates of phenylalanine 4-monooxygenase.

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.

authors

Patel NG,Iliadou C,Boonyapiwat B,Barlow DJ,Forbes B,Mitchell SC,Steventon GB

doi

10.1080/14756360701810280

subject

Has Abstract

pub_date

2008-12-01 00:00:00

pages

958-63

issue

6

eissn

1475-6366

issn

1475-6374

pii

788264435

journal_volume

23

pub_type

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