The Structure-Function Relationship of Angular Estrogens and Estrogen Receptor Alpha to Initiate Estrogen-Induced Apoptosis in Breast Cancer Cells.
Breast Neoplasms
/ drug therapy
Cell Line, Tumor
Cell Survival
/ drug effects
Drug Resistance, Neoplasm
/ drug effects
Estradiol
/ chemistry
Estrogen Antagonists
/ chemical synthesis
Estrogen Receptor alpha
/ chemistry
Female
Humans
MCF-7 Cells
Models, Molecular
Molecular Dynamics Simulation
Molecular Structure
Stilbenes
/ chemical synthesis
Structure-Activity Relationship
Journal
Molecular pharmacology
ISSN: 1521-0111
Titre abrégé: Mol Pharmacol
Pays: United States
ID NLM: 0035623
Informations de publication
Date de publication:
07 2020
07 2020
Historique:
received:
10
02
2020
accepted:
16
04
2020
pubmed:
5
5
2020
medline:
31
7
2020
entrez:
5
5
2020
Statut:
ppublish
Résumé
High-dose synthetic estrogen therapy was the standard treatment of advanced breast cancer for three decades until the discovery of tamoxifen. A range of substituted triphenylethylene synthetic estrogens and diethylstilbestrol were used. It is now known that low doses of estrogens can cause apoptosis in long-term estrogen deprived (LTED) breast cancer cells resistant to antiestrogens. This action of estrogen can explain the reduced breast cancer incidence in postmenopausal women over 60 who are taking conjugated equine estrogens and the beneficial effect of low-dose estrogen treatment of patients with acquired aromatase inhibitor resistance in clinical trials. To decipher the molecular mechanism of estrogens at the estrogen receptor (ER) complex by different types of estrogens-planar [17
Identifiants
pubmed: 32362585
pii: mol.120.119776
doi: 10.1124/mol.120.119776
pmc: PMC7294906
doi:
Substances chimiques
ESR1 protein, human
0
Estrogen Antagonists
0
Estrogen Receptor alpha
0
Stilbenes
0
Estradiol
4TI98Z838E
triphenylethylene
S4ZLZ1K74B
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, Non-P.H.S.
Research Support, U.S. Gov't, P.H.S.
Langues
eng
Sous-ensembles de citation
IM
Pagination
24-37Subventions
Organisme : Department of Defense
ID : W81XWH-06-1-0590
Pays : International
Organisme : NCI NIH HHS
ID : CA016672
Pays : United States
Organisme : NCI NIH HHS
ID : U24 CA199461
Pays : United States
Organisme : Department of Defense
ID : W81XWH-14-1-0360
Pays : International
Organisme : NCI NIH HHS
ID : P30 CA125123
Pays : United States
Organisme : US Department of Energy
ID : DE-AC02-06CH11357
Pays : International
Informations de copyright
Copyright © 2020 The Author(s).
Références
Br J Pharmacol. 2014 Sep;171(17):4062-72
pubmed: 24819221
Cancer Res. 1989 Sep 1;49(17):4765-9
pubmed: 2758410
Cancer Res. 1988 Sep 15;48(18):5183-7
pubmed: 3409244
CA Cancer J Clin. 2015 Jan-Feb;65(1):5-29
pubmed: 25559415
Mol Pharmacol. 2014 May;85(5):789-99
pubmed: 24608856
J Natl Cancer Inst. 2011 Sep 21;103(18):1397-402
pubmed: 21753181
JAMA. 2004 Apr 14;291(14):1701-12
pubmed: 15082697
Proc Natl Acad Sci U S A. 2011 Nov 22;108(47):18879-86
pubmed: 22011582
Cancer. 1970 Oct;26(4):737-54
pubmed: 4918638
J Natl Cancer Inst. 2001 Nov 21;93(22):1714-23
pubmed: 11717332
Acta Crystallogr D Biol Crystallogr. 2010 Feb;66(Pt 2):213-21
pubmed: 20124702
Mol Endocrinol. 2002 Aug;16(8):1778-92
pubmed: 12145334
Ann N Y Acad Sci. 2004 Dec;1038:80-7
pubmed: 15838100
Mol Cell Proteomics. 2018 Nov;17(11):2270-2283
pubmed: 30093420
Recent Results Cancer Res. 1993;127:23-33
pubmed: 8502820
Cancer Res. 2017 Nov 1;77(21):e23-e26
pubmed: 29092932
Mol Cell. 2013 Jul 25;51(2):185-99
pubmed: 23850489
Angew Chem Int Ed Engl. 2016 Mar 18;55(13):4252-5
pubmed: 26928945
J Biol Chem. 2011 Jul 29;286(30):26267-76
pubmed: 21652716
Mol Endocrinol. 1993 Oct;7(10):1266-74
pubmed: 8264659
Cancer Res. 2001 Sep 15;61(18):6619-23
pubmed: 11559523
Nature. 1997 Jun 12;387(6634):733-6
pubmed: 9192902
JAMA. 2009 Aug 19;302(7):774-80
pubmed: 19690310
Br J Pharmacol. 2013 May;169(1):167-78
pubmed: 23373633
Oncogene. 2018 Aug;37(33):4581-4598
pubmed: 29748621
Nat Rev Drug Discov. 2003 Mar;2(3):205-13
pubmed: 12612646
J Med Chem. 2010 Apr 22;53(8):3273-83
pubmed: 20334368
Mol Pharmacol. 2018 Aug;94(2):812-822
pubmed: 29739819
J Med Chem. 2014 Jun 12;57(11):4569-83
pubmed: 24805199
Clin Cancer Res. 2000 May;6(5):2028-36
pubmed: 10815929
Br Med J. 1944 Sep 23;2(4368):393-8
pubmed: 20785660
Acta Crystallogr D Biol Crystallogr. 2010 Apr;66(Pt 4):486-501
pubmed: 20383002
J Biol Chem. 2001 Sep 21;276(38):35684-92
pubmed: 11473106
Acta Crystallogr D Biol Crystallogr. 2006 Aug;62(Pt 8):859-66
pubmed: 16855301
Cancer. 1965 Dec;18(12):1551-7
pubmed: 5845796
J Natl Cancer Inst. 2005 Dec 7;97(23):1746-59
pubmed: 16333030
J Natl Cancer Inst. 2014 Sep 30;106(11):
pubmed: 25269699
Mol Cell Biol. 1999 Dec;19(12):8226-39
pubmed: 10567548
Breast Cancer Res Treat. 2001 May;67(2):111-6
pubmed: 11519859
Horm Mol Biol Clin Investig. 2011 Mar 1;5(1):27-34
pubmed: 21660224
Science. 1997 Aug 15;277(5328):965-8
pubmed: 9252329
J Steroid Biochem Mol Biol. 2005 Feb;94(1-3):131-41
pubmed: 15862958
Maturitas. 2017 Jan;95:11-23
pubmed: 27889048
Nat Chem Biol. 2008 Apr;4(4):241-7
pubmed: 18344977
JAMA. 2011 Apr 6;305(13):1305-14
pubmed: 21467283