Drug Metabolism in Drug Design and Development Basic Concepts and Practice

TABLE 3.5 Human SULT isoforms, substrates, and genetic polymorphisms.

Human
SULT cDNA Substrates

Common genetic

polymorphisms

SULT1A1 Simple phenols 17b-estradiol SULT1A1^ 2 (Arg213His)
Iodothyronines Acetaminophen SULT1A1^ 3 (Met223Val)
Minoxidil
17 a-ethinylestradiol Isoflavones
Hydroxy-tamoxifen
SULT1A2 Catecholestrogens SULT1A2^ 2 (Ile7Thr)
Simple phenols SULT1A2^ 3 (Pro19Leu)
SULT1A3 Dopamine (catecholamines) Lys234Asn
Tyramine
Serotonin
Salbutamol
Isoprenaline
Dobutamine
Hydroxylated tibolone
4-Hydroxypropranalol
SULT1B1 Simple phenols
Catechols
Iodothyronines
0-desmethylnaproxen
SULT1C2 N-hydroxy-2-acetylaminfluorene
SULT1C4 N-hydroxy-2-acetylaminfluorene
SULT1E1 Estrone Asp22Tyr
17 b-Estradiol Ala32Val
17 a-Ethinylestradiol Pro253His
Equilenin
Diethylstilbestrol
Thyroxine
0-desmethylnaproxen
3-OH-benozo[a]pyrene
Phytoestrogens
SULT2A1 DHEA Ala63Pro
Pregnolone Lys227Glu
Cholesterol Ala261Thr
Cortisol
Testosterone
Bile salts
PAHs (benzylic alcohols)
Hydroxy-tamoxifen
SULT2B1_v1 DHEA
Pregnenolone
3 b-Hydroxy steroids
SULT2B1_v2 DHEA
Pregnenolone
3 b-Hydroxy steroids
SULT4A1?

66 CONJUGATIVE METABOLISM OF DRUGS