Characterization of the estrogen receptor and its dynamics in MCF-7 human breast cancer cells using a covalently attaching antiestrogen

Endocrinology
F J MonsmaJ A Katzenellenbogen

Abstract

We have used a covalently attaching antiestrogen, tamoxifen aziridine [TA; (Z)-(1-[4-(2-[N-aziridinyl] ethoxy)phenyl])1,2-diphenyl-1-butene], to analyze the structure and dynamics of the estrogen receptor in MCF-7 human breast cancer cells. The labeling of receptor with [3H]TA is specific, being blocked only by estrogens and antiestrogens, and the labeling is very efficient in that TA labels covalently the same number of receptors that are labeled reversibly by estradiol. In cells exposed to [3H]TA for 1 h, most of the covalently associated radioactivity is found in the 0.6 M KCl extract of the nuclear fraction; this receptor has an apparent mol wt of 63,000 +/- 2000 by sodium dodecyl sulfate-polyacrylamide gel electrophoresis and a pI of 5.7 by gel isoelectric focusing in the presence of 8 M urea. The mol wt and pI of cytosol receptor labeled with [3H] TA are identical. In cells labeled with [3H]TA (20 nM) for 1 h and then exposed to a chase of 10(-6) M estradiol, [3H]TA-labeled nuclear receptor disappears with a half-life of 4 h. Analysis of nuclear receptor by sodium dodecyl sulfate-gels during the chase period reveals that this loss reflects a decrease in the 63,000 mol wt species; no significant quantities of lower mol wt ...Continue Reading

Citations

Jan 1, 1994·Breast Cancer Research and Treatment·M B MartinM M Gottardis
Jan 1, 1988·Journal of Steroid Biochemistry·B N Díaz-ChicoW L McGuire
Dec 1, 1988·Journal of Steroid Biochemistry·T RatajczakR Hähnel
Aug 1, 1989·Journal of Steroid Biochemistry·J G LewisP A Elder
Sep 1, 1989·Journal of Steroid Biochemistry·M TetsuoJ Sjövall
Apr 1, 1989·Journal of Steroid Biochemistry·C H Van AswegenJ L Wittliff
May 1, 1989·Journal of Steroid Biochemistry·L DufreneE E Baulieu
Jan 1, 1985·Pharmacology & Therapeutics·E Milgrom
Jun 1, 1986·Molecular and Cellular Endocrinology·H Gronemeyer, M V Govindan
Nov 12, 1990·Molecular and Cellular Endocrinology·H LahootiA Aakvaag
Aug 1, 1993·Molecular and Cellular Endocrinology·W V WelshonsD E Preziosi
Jan 1, 1992·The Journal of Steroid Biochemistry and Molecular Biology·C M Silva, J A Cidlowski
Dec 1, 1993·The Journal of Steroid Biochemistry and Molecular Biology·F PakdelB S Katzenellenbogen
Feb 1, 1996·The Journal of Steroid Biochemistry and Molecular Biology·M BorrásG Leclercq
Apr 16, 2004·The Journal of Steroid Biochemistry and Molecular Biology·Larry N PetzAnn M Nardulli
Feb 27, 2001·Molecular and Cellular Endocrinology·M S CotroneoC A Lamartiniere
Jan 7, 1999·The Journal of Steroid Biochemistry and Molecular Biology·Y MaaroufiG Leclercq
Aug 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·G A PucaA M Molinari
Jan 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·T S Golding, K S Korach
Jul 20, 2007·Nucleic Acids Research·Jennifer R Schultz-NortonAnn M Nardulli
Apr 5, 2008·Molecular Endocrinology·Nicholas B BerryKenneth P Nephew
Jun 1, 1987·Journal of Steroid Biochemistry·M HayashidaK Matsumoto
Jan 1, 1988·Journal of Cancer Research and Clinical Oncology·R HackenbergK D Schulz
Jan 1, 1985·Journal of Cancer Research and Clinical Oncology·R W HartmannG Kranzfelder
Jan 1, 1988·Critical Reviews in Clinical Laboratory Sciences·V C JordanW V Welshons
Jun 26, 2008·Molecular and Cellular Endocrinology·Amy L CreekmoreAnn M Nardulli
Oct 1, 1991·General and Comparative Endocrinology·J C Reese, I P Callard

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.