Research resource: Transcriptional profiling in a cellular model of breast cancer reveals functional and mechanistic differences between clinically relevant SERM and between SERM/estrogen complexes.

Molecular Endocrinology
Suzanne E WardellDonald P McDonnell

Abstract

Exploitation of the relationship between estrogen receptor (ER) structure and activity has led to the development of 1) selective ER modulators (SERM), compounds whose relative agonist/antagonist activities differ between target tissues; 2) selective ER degraders (SERD), compounds that induce a conformational change in the receptor that targets it for proteasomal degradation; and 3) tissue-selective estrogen complexes (TSEC), drugs in which a SERM and an ER agonist are combined to yield a blended activity that results in distinct clinical profiles. In this study, we have performed a comprehensive head-to-head analysis of the transcriptional activity of these different classes of ERM in a cellular model of breast cancer. Not surprisingly, these studies highlighted important functional differences and similarities among the existing SERM, selective ER degraders, and TSEC. Of particular importance was the identification of genes that were regulated by various TSEC combinations but not by an estrogen or SERM alone. Cumulatively, the findings of this analysis are informative with respect to the mechanisms by which ER is engaged by different enhancers/promoters and highlights how promoter context influences the pharmacological activi...Continue Reading

References

Mar 26, 1992·The New England Journal of Medicine·R R LoveD L DeMets
Dec 1, 1991·Annals of Internal Medicine·R R LoveD L DeMets
Jun 1, 1995·The Journal of Steroid Biochemistry and Molecular Biology·D L ClemmD P McDonnell
May 26, 1998·JAMA : the Journal of the American Medical Association·B W WalshP W Anderson
Mar 31, 1999·Proceedings of the National Academy of Sciences of the United States of America·L A PaigeD M Fowlkes
Jul 31, 1999·Science·J D NorrisD P McDonnell
Feb 16, 2002·Methods : a Companion to Methods in Enzymology·K J Livak, T D Schmittgen
Mar 30, 2002·Science·Yongfeng Shang, Myles Brown
Oct 10, 2002·Journal of Molecular Endocrinology·A InoueS Hayashi
May 10, 2003·The Journal of Biological Chemistry·Tetsuo FujitaJunn Yanagisawa
Dec 25, 2003·Bioinformatics·Monica BenitoJ S Marron
Mar 9, 2006·Best Practice & Research. Clinical Endocrinology & Metabolism·Ashley C W Pike
Jun 7, 2006·JAMA : the Journal of the American Medical Association·Victor G VogelUNKNOWN National Surgical Adjuvant Breast and Bowel Project (NSABP)
Feb 23, 2007·Menopause : the Journal of the North American Menopause Society·Dale W StovallLeo Plouffe
Apr 9, 2008·Journal of Cellular Biochemistry·Irene M WolfDonald B DeFranco
Dec 25, 2008·Expert Review of Anticancer Therapy·Victor G Vogel
Nov 11, 2009·The Journal of Steroid Biochemistry and Molecular Biology·Eric P SmithKenneth S Korach
May 29, 2010·Current Vascular Pharmacology·Genovefa KolovouHelen Bilianou
Jul 7, 2010·Current Osteoporosis Reports·Stuart L Silverman
Oct 7, 2010·Nature Chemical Biology·John B BruningKendall W Nettles
Feb 15, 2011·Trends in Biochemical Sciences·Shigeaki KatoRyoji Fujiki
May 4, 2011·Gender Medicine·Jeffrey P Levine

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Citations

Aug 24, 2012·Epigenetics & Chromatin·Tanja PrenzelSteven A Johnsen
Nov 29, 2013·Toxicological Sciences : an Official Journal of the Society of Toxicology·Anne KatchyCecilia Williams
Mar 4, 2014·Expert Review of Clinical Pharmacology·Maryam Sharifi, E Michael Lewiecki
Jun 29, 2013·Climacteric : the Journal of the International Menopause Society·J V PinkertonS Mirkin
Dec 23, 2015·The Journal of Steroid Biochemistry and Molecular Biology·Zeynep Madak-ErdoganBenita S Katzenellenbogen
Jan 30, 2013·Journal of Cellular Physiology·Barry S Komm, Sebastian Mirkin
Jul 15, 2015·Endocrine-related Cancer·Suzanne E WardellDonald P McDonnell
Jul 26, 2015·Cancer Letters·Govindasamy-Muralidharan KarthikJohan Hartman
Mar 29, 2014·The Journal of Steroid Biochemistry and Molecular Biology·Barry S Komm, Sebastian Mirkin
Jul 16, 2013·Maturitas·Sebastian Mirkin, Barry S Komm
Jun 26, 2013·Molecular and Cellular Endocrinology·S Stoney Simons, Raj Kumar
Aug 21, 2016·Molecular and Cellular Endocrinology·Ping GongBenita S Katzenellenbogen
Aug 16, 2013·Reproductive Sciences·Sarah L Berga
Feb 13, 2014·Menopause : the Journal of the North American Menopause Society·Sebastian MirkinBarry S Komm
Mar 27, 2018·International Journal of Cancer. Journal International Du Cancer·Wei YueRichard J Santen
Feb 24, 2015·Cancer Informatics·Magdalena A CichonDerek C Radisky
Oct 6, 2018·Annals of the New York Academy of Sciences·Shira Rebecca Saul, Nathan Kase
May 26, 2018·Scientific Reports·David J SchultzCarolyn M Klinge
Aug 8, 2017·The Journal of Clinical Investigation·Hideyuki OguroSean J Morrison
Jul 14, 2017·The Biochemical Journal·Lasse StabyKaren Skriver
Jan 16, 2014·The Journal of Clinical Endocrinology and Metabolism·Richard J SantenHugh S Taylor
Jan 1, 2014·Breast Cancer Research : BCR·Carolyn L SmithSebastian Mirkin
Apr 20, 2019·Frontiers in Endocrinology·Hideyuki Oguro
Aug 8, 2014·Molecular Cancer Research : MCR·Tricia M WrightDonald P McDonnell
Mar 29, 2013·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Suzanne E WardellDonald P McDonnell
Jan 11, 2021·Hormones and Behavior·Ha Na ChoeErich D Jarvis
May 28, 2021·Biochemical Pharmacology·Liqian MaErik R Nelson
Aug 21, 2021·Journal of Medicinal Chemistry·Leah L LowderSridhar Varadarajan

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