PMID- 11017892
OWN - NLM
STAT- MEDLINE
DCOM- 20001222
LR  - 20180831
IS  - 0091-6765 (Print)
IS  - 0091-6765 (Linking)
VI  - 108
IP  - 9
DP  - 2000 Sep
TI  - Interactions of dietary estrogens with human estrogen receptors and the effect on 
      estrogen receptor-estrogen response element complex formation.
PG  - 867-72
AB  - Epidemiologic and experimental studies support the hypothesis that dietary 
      estrogens from plant sources (phytoestrogens) may play a role in the prevention 
      of breast and prostate cancer. The molecular mechanisms for such chemopreventive 
      effect are still unclear. We investigated the possibility that phytoestrogens may 
      bind differentially to estrogen receptor proteins (ER[alpha] and ERss) and affect 
      the interactions of the ligand-ER complexes with different estrogen response 
      element (ERE) sequences. We used fluorescence polarization to measure the binding 
      affinities of genistein, coumestrol, daidzein, glyceollin, and zearalenone for 
      human ER[alpha] and ERss. Competition binding experiments revealed higher 
      affinity of the phytoestrogens for ERss than for ER[alpha]. Genistein [median 
      inhibitory concentration 12nM] is the most potent and has the same relative 
      binding affinity for ERss as 17ss-estradiol. We also studied the effect of these 
      phytoestrogens on the ability of ER[alpha] and ERss to associate with specific 
      DNA sequences (EREs). The direct binding of human recombinant estrogen receptors 
      to fluorescein-labeled EREs indicates that phytoestrogens can cause 
      conformational changes in both human ERs, which results in altered affinities of 
      the complexes for the ERE from the Xenopus vitellogenin A2 gene and an ERE from 
      the human pS2 gene.
FAU - Nikov, G N
AU  - Nikov GN
AD  - Department of Chemistry, Tulane University, New Orleans, Louisiana 07118, USA.
FAU - Hopkins, N E
AU  - Hopkins NE
FAU - Boue, S
AU  - Boue S
FAU - Alworth, W L
AU  - Alworth WL
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Research Support, U.S. Gov't, Non-P.H.S.
PL  - United States
TA  - Environ Health Perspect
JT  - Environmental health perspectives
JID - 0330411
RN  - 0 (Estrogens)
RN  - 0 (Ligands)
RN  - 0 (Plant Growth Regulators)
RN  - 0 (Receptors, Estrogen)
RN  - 9007-49-2 (DNA)
SB  - IM
CIN - Environ Health Perspect. 2000 Sep;108(9):A416. PMID: 11185385
MH  - Animals
MH  - Binding Sites
MH  - Chemoprevention
MH  - DNA/physiology
MH  - Diet
MH  - Estrogens/*pharmacology
MH  - Humans
MH  - Ligands
MH  - Plant Growth Regulators/*pharmacology
MH  - Protein Conformation
MH  - Receptors, Estrogen/*drug effects/physiology
MH  - Xenopus/physiology
PMC - PMC2556928
EDAT- 2000/10/06 11:00
MHDA- 2001/02/28 10:01
PMCR- 2000/09/01
CRDT- 2000/10/06 11:00
PHST- 2000/10/06 11:00 [pubmed]
PHST- 2001/02/28 10:01 [medline]
PHST- 2000/10/06 11:00 [entrez]
PHST- 2000/09/01 00:00 [pmc-release]
AID - sc271_5_1835 [pii]
AID - 10.1289/ehp.00108867 [doi]
PST - ppublish
SO  - Environ Health Perspect. 2000 Sep;108(9):867-72. doi: 10.1289/ehp.00108867.