PMID- 3383172
OWN - NLM
STAT- MEDLINE
DCOM- 19880811
LR  - 20190720
IS  - 0304-3835 (Print)
IS  - 0304-3835 (Linking)
VI  - 40
IP  - 2
DP  - 1988 Jun 15
TI  - Effect of tamoxifen and tamoxifen derivatives on the conversion of estrone 
      sulfate to estradiol in the MCF-7 mammary cancer cell line.
PG  - 115-21
AB  - The human mammary cancer cell line MCF-7 in culture was used to study the effect 
      of tamoxifen and its derivatives: 4-hydroxytamoxifen (4-OH-Tam), 
      N-desmethyltamoxifen (Dem-Tam) and cis-tamoxifen (cis-Tam) on the uptake and 
      conversion of [3H]estrone sulfate (3H-E1S) to estradiol (E2). When [3H]-E1S (4 X 
      10(-9) M) was incubated by itself (control) a great proportion of the 
      radioactivity was found as [3H]E2, predominantly in the nuclear fraction. All of 
      the anti-estrogens (10(-6) M - 10(-5) M) studied decreased the total uptake of 
      radioactivity by the cells by 50-60% and the quantity of E2 formed. The 
      calculated concentrations (in pg/mg DNA +/- S.E.M.) of E2 (cytosol + 0.6 M KCl 
      nuclear extract) with the anti-estrogens at 10(-5) M were as follows: control 56 
      +/- 3; Tam treated cells 4 +/- 1; + 4-OH-Tam 2 +/- 1; + Dem-Tam 5 +/- 2; + 
      cis-Tam 8 +/- 4. A significant decrease in the concentrations of E2 was also 
      observed in the mitochondria-microsomal fractions after the different treatments. 
      It is suggested that the MCF-7 cells can use estrone-3-sulfate as a source of E2 
      and that the inhibitory effect of tamoxifen and its derivatives on the conversion 
      of this sulfate to E2 could be involved in the anti-estrogenic process of these 
      triphenylethylene derivatives.
FAU - Pasqualini, J R
AU  - Pasqualini JR
AD  - C.N.R.S. Steroid Hormone Research Unit, Foundation for Hormone Research, Paris, 
      France.
FAU - Gelly, C
AU  - Gelly C
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Ireland
TA  - Cancer Lett
JT  - Cancer letters
JID - 7600053
RN  - 094ZI81Y45 (Tamoxifen)
RN  - 2DI9HA706A (Estrone)
RN  - 4TI98Z838E (Estradiol)
RN  - QTL48N278K (estrone sulfate)
SB  - IM
MH  - Breast Neoplasms/*metabolism
MH  - Cell Line
MH  - Estradiol/*metabolism
MH  - Estrone/*analogs & derivatives/metabolism
MH  - Female
MH  - Humans
MH  - Tamoxifen/analogs & derivatives/*pharmacology
MH  - Tumor Cells, Cultured
EDAT- 1988/06/15 00:00
MHDA- 1988/06/15 00:01
CRDT- 1988/06/15 00:00
PHST- 1988/06/15 00:00 [pubmed]
PHST- 1988/06/15 00:01 [medline]
PHST- 1988/06/15 00:00 [entrez]
AID - 0304-3835(88)90001-8 [pii]
AID - 10.1016/0304-3835(88)90001-8 [doi]
PST - ppublish
SO  - Cancer Lett. 1988 Jun 15;40(2):115-21. doi: 10.1016/0304-3835(88)90001-8.