An antiestrogen-binding protein in human tissues - PubMed (original) (raw)
. 1983 Mar 10;258(5):3173-7.
- PMID: 6826555
Free article
An antiestrogen-binding protein in human tissues
O L Kon. J Biol Chem. 1983.
Free article
Abstract
Although nonsteroidal antiestrogens of the triphenylethylene type are generally considered to act through the estrogen receptor, some observations suggest that estrogen target tissues may also contain a binding protein specific for these compounds. The data so far reported, however, are also consistent with ligand-induced changes in conformation or in the state of aggregation of the estrogen receptor. The studies reported here demonstrate the existence of a protein in human myometrial cytosol which binds 1-[4-(2-dimethylaminoethoxy)phenyl]1,2-diphenylbut-1(Z)-ene ([3H]tamoxifen) with high affinity (Kd = 2.3 X 10(-9) M). This protein exhibits striking specificity for nonsteroidal antiestrogens. Estradiol competes weakly for bound [3H]tamoxifen, while other estrogens and nonestrogenic steroid hormones do not compete at all. Sedimentation analysis and molecular sieve chromatography indicate that the antiestrogen-binding protein is a larger species than the estrogen receptor and elutes from DEAE-Sephacel at a lower KCl concentration (0.03 M) than the estrogen receptor (0.15 M). Differential thermal stability of the estrogen receptor and the antiestrogen-binding protein was demonstrable in the absence of added ligand. The antiestrogen-binding protein was ubiquitous, being present in many tissues where estrogen receptor was undetectable. These findings support the separate existence of an antiestrogen-binding protein.
Similar articles
- Characterization of an antiestrogen-binding protein in high salt extracts of human breast cancer tissue.
Kon OL. Kon OL. J Steroid Biochem. 1985 Feb;22(2):177-86. doi: 10.1016/0022-4731(85)90110-4. J Steroid Biochem. 1985. PMID: 3982029 - Differential inhibition of estrogen and antiestrogen binding to the estrogen receptor by diethylpyrocarbonate.
Borgna JL, Scali J. Borgna JL, et al. J Steroid Biochem. 1988 Oct;31(4A):427-36. doi: 10.1016/0022-4731(88)90311-1. J Steroid Biochem. 1988. PMID: 3050278 - Antiestrogen binding in antiestrogen growth-resistant estrogen-responsive clonal variants of MCF-7 human breast cancer cells.
Miller MA, Lippman ME, Katzenellenbogen BS. Miller MA, et al. Cancer Res. 1984 Nov;44(11):5038-45. Cancer Res. 1984. PMID: 6488162 - Triphenylethylene antiestrogen-binding sites in cockerel liver nuclei: evidence for an endogenous ligand.
Murphy PR, Butts C, Lazier CB. Murphy PR, et al. Endocrinology. 1984 Jul;115(1):420-6. doi: 10.1210/endo-115-1-420. Endocrinology. 1984. PMID: 6734522 - Interactions of tamoxifen in the chicken.
Lazier CB. Lazier CB. J Steroid Biochem. 1987;27(4-6):877-82. doi: 10.1016/0022-4731(87)90163-4. J Steroid Biochem. 1987. PMID: 3320566 Review.
Cited by
- Advance in metabolism and target therapy in breast cancer stem cells.
Gao X, Dong QZ. Gao X, et al. World J Stem Cells. 2020 Nov 26;12(11):1295-1306. doi: 10.4252/wjsc.v12.i11.1295. World J Stem Cells. 2020. PMID: 33312399 Free PMC article. Review. - Microsomal epoxide hydrolase expression in the endometrial uterine corpus is regulated by progesterone during the menstrual cycle.
Popp SL, Abele IS, Buck MB, Stope MB, Blok LJ, Hanifi-Moghaddam P, Burger CW, Fritz P, Knabbe C. Popp SL, et al. J Mol Histol. 2010 Apr;41(2-3):111-9. doi: 10.1007/s10735-010-9266-6. Epub 2010 Apr 13. J Mol Histol. 2010. PMID: 20383792 - Microsomal epoxide hydrolase of rat liver is a subunit of theanti-oestrogen-binding site.
Mésange F, Sebbar M, Kedjouar B, Capdevielle J, Guillemot JC, Ferrara P, Bayard F, Delarue F, Faye JC, Poirot M. Mésange F, et al. Biochem J. 1998 Aug 15;334 ( Pt 1)(Pt 1):107-12. doi: 10.1042/bj3340107. Biochem J. 1998. PMID: 9693109 Free PMC article. - Tamoxifen inhibits nitrobenzylthioinosine-sensitive equilibrative uridine transport in human MCF-7 breast cancer cells.
Cai J, Lee CW. Cai J, et al. Biochem J. 1996 Dec 15;320 ( Pt 3)(Pt 3):991-5. doi: 10.1042/bj3200991. Biochem J. 1996. PMID: 9003390 Free PMC article. - Binding sites of droloxifene in the cytosol of 7,12-dimethylbenz[a]anthracene-induced rat mammary tumor cells.
Kawamura I, Lacey E, Tanaka Y, Nishigaki F, Manda T, Shimomura K. Kawamura I, et al. Jpn J Cancer Res. 1994 Jun;85(6):639-44. doi: 10.1111/j.1349-7006.1994.tb02407.x. Jpn J Cancer Res. 1994. PMID: 8063618 Free PMC article.
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources