PMID- 22450794
OWN - NLM
STAT- MEDLINE
DCOM- 20120716
LR  - 20190923
IS  - 1738-8872 (Electronic)
IS  - 1017-7825 (Linking)
VI  - 22
IP  - 3
DP  - 2012 Mar
TI  - Organotin compounds act as inhibitor of transcriptional activation with human 
      estrogen receptor.
PG  - 378-84
AB  - In aquatic invertebrates, particularly marine gastropods, organotin compounds 
      induce irreversible sexual abnormality in females, which is termed imposex, at 
      very low concentrations. Organotin compounds are agonists for nuclear receptors 
      such as RXRs and PPARgamma. However, the imposex phenomenon has not been reported 
      to act as an antagonist on estrogen receptors in other species, including 
      vertebrates and invertebrates. In order to gain insights into the antagonistic 
      activity of organotin compounds on estrogen receptors (ERs), we examined the 
      inhibitive effect of these compounds on estradiol-dependent beta-galactosidase 
      activity using the yeast two-hybrid detection system consisting of a combination 
      of the human estrogen receptor (hERbeta) ligand-binding domain and the 
      co-activator steroid receptor co-activator-1 (SRC1). Tributyltin-hydroxide 
      (TBT-OH) and triphenyltin-chlorine (TPT-Cl) exhibited an inhibitive effect on 
      E(2)-dependent transcriptional activity, similar to antagonistic chemicals such as 
      4-hydroxytamoxifen (OHT) or ICI 182,780, at a very low concentration of 10(-)(1)(4) M 
      TBT or 10(-)(1)(0) M TPT, respectively. The yeast growth and transcriptional activity 
      with transcriptional factor GAL4 did not exhibit any effect at the tested 
      concentration of TBT or TPT. Moreover, the yeast two-hybrid system using the 
      interaction between p53 and the T antigen of SV40 large did not describe any 
      effect at the tested concentration of OHT or ICI 182,780. However, the 
      interaction between p53 and T antigen was inhibited at a TBT or TPT concentration 
      of 10(-)(9) M, respectively. These results indicate that TBT and TPT act as 
      inhibitors of ER-dependent reporter gene transcriptional activation and of the 
      interaction between hERbeta LBD and the co-activator SRC1 in the yeast two-hybrid 
      system. Consequently, our data could partly explain the occurrence of organotin 
      compound-induced imposex on the endocrine system of mammals, including humans.
FAU - Cho, Eun-Min
AU  - Cho EM
AD  - New and Renewable Energy Company, North of Gyeonggi Venture Center, Uijongbu, 
      Gyeonggi-do 480-020, Korea.
FAU - Lee, Haeng-Seog
AU  - Lee HS
FAU - Moon, Jeong-Suk
AU  - Moon JS
FAU - Kim, Im-Soon
AU  - Kim IS
FAU - Sim, Sanghyo
AU  - Sim S
FAU - Ohta, Akinori
AU  - Ohta A
LA  - eng
PT  - Journal Article
PL  - Korea (South)
TA  - J Microbiol Biotechnol
JT  - Journal of microbiology and biotechnology
JID - 9431852
RN  - 0 (Endocrine Disruptors)
RN  - 0 (Organotin Compounds)
RN  - 0 (Receptors, Estrogen)
RN  - 0 (Trialkyltin Compounds)
RN  - 4TI98Z838E (Estradiol)
RN  - 4XDX163P3D (tributyltin)
RN  - EC 3.2.1.23 (beta-Galactosidase)
RN  - I1L80IDY27 (triphenyltin chloride)
SB  - IM
MH  - Down-Regulation/*drug effects
MH  - Endocrine Disruptors/pharmacology
MH  - Estradiol/metabolism
MH  - Female
MH  - Humans
MH  - Models, Biological
MH  - Organotin Compounds/*pharmacology
MH  - Ovotesticular Disorders of Sex Development/*etiology/genetics/metabolism
MH  - Receptors, Estrogen/*genetics/metabolism
MH  - Saccharomyces cerevisiae/genetics/metabolism
MH  - Transcriptional Activation/*drug effects
MH  - Trialkyltin Compounds/*pharmacology
MH  - Two-Hybrid System Techniques
MH  - beta-Galactosidase/antagonists & inhibitors/genetics/metabolism
EDAT- 2012/03/28 06:00
MHDA- 2012/07/17 06:00
CRDT- 2012/03/28 06:00
PHST- 2012/03/28 06:00 [entrez]
PHST- 2012/03/28 06:00 [pubmed]
PHST- 2012/07/17 06:00 [medline]
AID - JMB022-03-13 [pii]
AID - 10.4014/jmb.1105.05033 [doi]
PST - ppublish
SO  - J Microbiol Biotechnol. 2012 Mar;22(3):378-84. doi: 10.4014/jmb.1105.05033.