Absorption, metabolism, and excretion of darunavir, an inhibitor of human immunodeficiency virus protease, was studied in eight healthy male subjects after a single oral dose of 400 mg of [(14)C]darunavir given alone (unboosted subjects) or with ritonavir [100 mg b.i.d. 2 days before and 7 days after darunavir administration (boosted subjects)]. Plasma exposure to darunavir was 11-fold higher i...

The effects of allelic variants of CYP2C9 (CYP2C9*2 and CYP2C9*3) on lornoxicam 5'-hydroxylation were studied using the corresponding variant protein expressed in baculovirus-infected insect cells and human liver microsomes of known genotypes of CYP2C9. The results of the baculovirus expression system showed that CYP2C9.3 gives higher K(m) and lower V(max) values for lornoxicam 5'-hydroxylation...

The role of body fat as a risk factor for breast cancer has been well established. A decrease in the urinary 2/16α-hydroxyestrone ratio has also been shown to be a risk marker for breast cancer. These two observations are connected by the fact that obese women have decreased levels of 2-hydroxyestrone. To test the hypothesis that fat depots secrete factors that inhibit 2-hydroxylation, the effe...

Levetiracetam and its carboxylic metabolite (AcL) were tested for their potential inhibitory effect on 11 different drug metabolizing enzyme activities using human liver microsomes. The following specific assays were investigated: testosterone 6beta-hydroxylation [cytochrome P-450 3A4 (CYP3A4)], coumarin hydroxylation (CYP2A6), (R)-warfarin hydroxylation (CYP1A2), (S)-mephenytoin hydroxylation ...

Collagen is the major protein in extracellular matrix and plays vital roles tissue development function. also one of most processed proteins its biosynthesis. The prominent post-translational modification (PTM) collagen hydroxylation Pro residues Y-position characteristic (Gly-Xaa-Yaa) repeating amino acid sequence a triple helix. Recent studies using mass spectrometry (MS) tandem MS sequencing...