PMID- 1445950
OWN - NLM
STAT- MEDLINE
DCOM- 19921224
LR  - 20190609
IS  - 0006-3002 (Print)
IS  - 0006-3002 (Linking)
VI  - 1160
IP  - 2
DP  - 1992 Nov 20
TI  - Glycyrrhetinic acid bound to 11 beta-hydroxysteroid dehydrogenase in rat liver 
      microsomes.
PG  - 229-34
AB  - A binding protein which exhibits high affinity to [3H]glycyrrhetinic-acid in the 
      rat liver microsomal fraction was solubilized with 0.2% Triton DF-18 and then 
      purified to homogeneity. The equilibrium dissociation constant of the 
      [3H]glycyrrhetinic-acid binding reaction and the maximal concentration for the 
      binding of the purified protein, as determined by Scatchard plot analysis, were 
      27.6 nM and 7.79 nmol/mg protein, respectively. The molecular mass of the subunit 
      (34 kDa) and 30 amino acids of N-terminal sequence of the purified protein were 
      entirely the same as those of the reported 11 beta-hydroxysteroid dehydrogenase 
      (11 beta-HSD). In each purification step, the recovery and purification (fold) of 
      the glycyrrhetinic-acid binding activity corresponded to the values of 11 
      beta-HSD activity. These results show that the purified [3H]glycyrrhetinic-acid 
      binding protein is 11 beta-HSD. From the molecular mass of 11 beta-HSD (135 kDa) 
      and the maximal concentration of the binding site, it was calculated that one 
      glycyrrhetinic acid molecule binds to one 11 beta-HSD molecule. The inhibitory 
      effects of various glycyrrhetinic-acid derivatives on [3H]glycyrrhetinic acid 
      binding and 11 beta-HSD activity indicate that the C30-carboxyl and C11-carbonyl 
      groups of glycyrrhetinic acid are the principal structures for the 11 beta-HSD 
      inhibition.
FAU - Irie, A
AU  - Irie A
AD  - Department of Physiological Chemistry, Faculty of Pharmaceutical Sciences, Kyoto 
      University, Japan.
FAU - Fukui, T
AU  - Fukui T
FAU - Negishi, M
AU  - Negishi M
FAU - Nagata, N
AU  - Nagata N
FAU - Ichikawa, A
AU  - Ichikawa A
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PL  - Netherlands
TA  - Biochim Biophys Acta
JT  - Biochimica et biophysica acta
JID - 0217513
RN  - EC 1.1.- (Hydroxysteroid Dehydrogenases)
RN  - EC 1.1.1.146 (11-beta-Hydroxysteroid Dehydrogenases)
RN  - P540XA09DR (Glycyrrhetinic Acid)
SB  - IM
MH  - 11-beta-Hydroxysteroid Dehydrogenases
MH  - Animals
MH  - Binding Sites
MH  - Glycyrrhetinic Acid/*metabolism
MH  - Hydroxysteroid Dehydrogenases/antagonists & inhibitors/isolation & 
      purification/metabolism
MH  - Microsomes, Liver/*enzymology
MH  - Rats
EDAT- 1992/11/20 00:00
MHDA- 1992/11/20 00:01
CRDT- 1992/11/20 00:00
PHST- 1992/11/20 00:00 [pubmed]
PHST- 1992/11/20 00:01 [medline]
PHST- 1992/11/20 00:00 [entrez]
AID - 0167-4838(92)90012-3 [pii]
AID - 10.1016/0167-4838(92)90012-3 [doi]
PST - ppublish
SO  - Biochim Biophys Acta. 1992 Nov 20;1160(2):229-34. doi: 
      10.1016/0167-4838(92)90012-3.