Drug Metabolism in Drug Design and Development Basic Concepts and Practice

TABLE 3.1 UGT1A nomenclature:seehttp://som.flinders.edu.au/FUSA/
ClinPharm/UGT/.

UGT1
gene

Trivial

names

Endogenous

substrates

Tissue

expression Comments

UGT1A1 Rat B1
HUGBr-1

Bilirubin

Estradiol

(3-OH)

Liver, intestine,

mammary

gland

Polymorphic

regulation

UgtBr1

(mouse)

Morphine

(3-OH)

Catechol

estrogens

(2OH>4OH)

Retinoic acid

leukotriene B4

12 and 15-HETE

13-HODE

Defective

genesCrigler–

Najjar

syndrome

Lowered

expression

Gilbert’s

syndrome

Trans-retinoic

acid is a

substrate for

rat UGT1A1

but not human?

UGT1A2 Rat B2 Bilirubin Pseudogene in
humans
Rapidly declines
in tissue
culture of rat
hepatocytes
UGT1A3 Bile acid Liver, intestine,
Catechol testes, prostate
estrogens
(2OH>4OH)
leukotriene B4
12 and 15-HETE
13-HODE
UGT1A4 HP3
HUGBr-2

12 and 15-HETE

13-HODE

Liver, intestine Pseudogene in
rats and mice
UGT1A6 HP1
HlugP1
Ugt1-6
Rat4NP

Liver, kidney,

intestine, brain,

ovary, testes

Pseudogene

in cats

Spleen, skin Polymorphic in
humans
UGT1A7 A2
1g

Gastric epithelium
esophagus
UGT1A8 Leukotriene B4 Intestine,
esophagus
UGT1A9 HP4 Catechol
estrogens
(4OH>2OH)
estradiol (low)
12 and 15-HETE
13-HODE

Liver, kidney ovary,

testes

Spleen, skin,

esophagus

UGT1A10 Intestine, lung
UGT1A11-
1A13

Pseudogenes

UDP-GLUCURONOSYLTRANSFERASES 43