Drug Metabolism in Drug Design and Development Basic Concepts and Practice

UGT1A11







UGT1A12







UGT1A8 and UGT1A9 were previously mislabeled. The old UGT1A8 is now UGT1A9 and vice versa.AhR activators in humans (aromatic hydrocarbon receptor)–tetrachlorodibenzodioxin (TCDD),

b-naphthoflavone, 3-methylcloranthrene.

PXR (pregnenolone-16

a-nitrile-X-receptor) activators in rodents–pregnenolone-16

a-nitrile (PCN), dexamethasone.

PXR (pregnenolone-16

a-nitrile-X-receptor) activators in humans–clotrimazole, rifampin, and St. John’s wort.

CAR (constitutive androstane receptor) activators in humans–3-methylcholanthrene, phenylpropionic acid, phenobarbital, phenytoin, carbamaz

epine.

PPAR

a

(peroxisome proliferated-activated receptor-

a) activator in humans–clofibric acid, fenobibric acid, pirinixic acid.

PPAR

g

(peroxisome proliferated-activated receptor-

g) activator in humans–rosiglitazone.

FXR (farnesoid-X-receptor) activators in humans – chenodeoxycholic acid.LXR (liver-X-receptor).RXR (retinod-X-receptor).Underlinied substrates denote the most commonly used probes for enzymatic activity.

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