Drug Metabolism in Drug Design and Development Basic Concepts and Practice

TABLE 3.2 UGT2B nomenclature:seehttp://som.flinders.edu.au/FUSA/
ClinPharm/UGT/.

UGT1
gene Species

Endogenous

substrates Tissue expression Comments

UGT2B1 Rat Estradiol
(17-OH);
morphine
(3OH)

Liver, low in kidney,

intestine, testes

97% similar to

UGT2B2

UGT2B2 Rat Liver Gene deletion in
adrosterone-
deficient
Wistar rats
UGT2B3 Rat Bile acid
UGT2B4 Human Hyodeoxycholic
acid; 3a-OH-
pregnanes and
3 a,16a,17b-
androgens
12-HETE,
15-HETE and
13-HODE

Liver Activity of a
variant
(described as
UGT2B11)
toward steroids
described by
Jin, Mackenzie,
and Miners,
1997
UGT2B5 Rabbit
UGT2B6 Rat
UGT2B7 Human Estradiol
(17b-OH), estriol,
3 a-OH-pregnanes
3 a,16a,17b-
androgens
trans-retinoic
acid, leukotriene
B4, morphine 3/6-OH
12-HETE, 15-HETE,
and 13-HODE

Liver, kidney,

espophagus,

intestine, brain

(cerebellum)

Polymorphism

at 268

(Tyr or His)

UGT2B8 Rat Liver
UGT2B9 Cyno-
mologus
monkey

C 18 ,C 19 ,C 20

steroids, fatty

acids (C 6 –C12)

morphine

3/6-OH

Liver 89% identical to

UGT2B7

UGT2B10 Human 12-HETE,
15-HETE,
and 13-HODE
(prostaglandins)

Liver, adrenals,

prostate

UGT2B11 Human 12-HETE, 15-HETE,
and 13-HODE

RNA present in liver,

kidney, mammary

gland, prostate,

skin, adipose,

adrenal, and lung

91% identical to

UGT2B10

76% identical

to UGT2B15

and UGT2B17

44 CONJUGATIVE METABOLISM OF DRUGS