PMID- 6223181
OWN - NLM
STAT- MEDLINE
DCOM- 19830811
LR  - 20190817
IS  - 0022-4731 (Print)
IS  - 0022-4731 (Linking)
VI  - 18
IP  - 1
DP  - 1983 Jan
TI  - Inhibition of 17 beta-hydroxysteroid dehydrogenase activity in human endometrium 
      by adrenal androgens.
PG  - 59-64
AB  - The effect of dehydroepiandrosterone sulphate (DHA-S) and its metabolites 
      dehydroepiandrosterone (DHA) and 5-androstene-3 beta, 17 beta-diol (ADIOL) on the 
      activity of 17 beta-hydroxysteroid dehydrogenase in human endometrial tissue was 
      investigated by an isotope ratio technique. The apparent KM for oestradiol was 
      1.59 X 10(-6) M. All three androgens inhibited the metabolism of oestradiol and 
      the apparent Ki values were: ADIOL, 2.05 X 10(-6) M; DHA-S and DHA, 1.59 X 10(-6) 
      M. However, ADIOL acted by direct competition with oestradiol for the active 
      enzyme site whereas inhibition by DHA and its sulphate was non-competitive. DHA-S 
      and DHA were more potent inhibitors of oestradiol metabolism than was ADIOL. 
      These results support the hypothesis that adrenal androgens could be involved in 
      the development of endometrial hyperplasia and adenocarcinoma. Inhibition of 
      oestradiol metabolism could increase the concentration of oestradiol in 
      endometrial tissue and if unopposed by progesterone, e.g. after the menopause or 
      in subjects with ovulatory defects, could stimulate abnormal endometrial growth.
FAU - Bonney, R C
AU  - Bonney RC
FAU - Reed, M J
AU  - Reed MJ
FAU - James, V H
AU  - James VH
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - J Steroid Biochem
JT  - Journal of steroid biochemistry
JID - 0260125
RN  - 0 (Androgens)
RN  - 2DI9HA706A (Estrone)
RN  - 459AG36T1B (Dehydroepiandrosterone)
RN  - 4TI98Z838E (Estradiol)
RN  - 57B09Q7FJR (Dehydroepiandrosterone Sulfate)
RN  - 95PS51EMXY (Androstenediol)
RN  - EC 1.1.- (17-Hydroxysteroid Dehydrogenases)
SB  - IM
MH  - 17-Hydroxysteroid Dehydrogenases/*antagonists & inhibitors
MH  - Adrenal Glands/*metabolism
MH  - Androgens/metabolism/*pharmacology
MH  - Androstenediol/pharmacology
MH  - Dehydroepiandrosterone/analogs & derivatives/pharmacology
MH  - Dehydroepiandrosterone Sulfate
MH  - Endometrium/*enzymology
MH  - Estradiol/metabolism
MH  - Estrone/metabolism
MH  - Female
MH  - Humans
MH  - Kinetics
EDAT- 1983/01/01 00:00
MHDA- 1983/01/01 00:01
CRDT- 1983/01/01 00:00
PHST- 1983/01/01 00:00 [pubmed]
PHST- 1983/01/01 00:01 [medline]
PHST- 1983/01/01 00:00 [entrez]
AID - 10.1016/0022-4731(83)90331-x [doi]
PST - ppublish
SO  - J Steroid Biochem. 1983 Jan;18(1):59-64. doi: 10.1016/0022-4731(83)90331-x.