Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity

Estrogen receptor alpha (ERα) plays critical roles in the etiology and treatment of breast cancer. Here the authors synthesize benzopyrans with variable side chains to identify antiestrogenic compounds and characterize OP-1074, a compound that exhibits pure antiestrogenic activity by inducing the de...

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Autores principales:	S. W. Fanning, L. Hodges-Gallagher, D. C. Myles, R. Sun, C. E. Fowler, I. N. Plant, B. D. Green, C. L. Harmon, G. L. Greene, P. J. Kushner
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2018
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/b6e95950680a407c8d0a86c8da7e1436
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spelling	oai:doaj.org-article:b6e95950680a407c8d0a86c8da7e14362021-12-02T16:49:32ZSpecific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity10.1038/s41467-018-04413-32041-1723https://doaj.org/article/b6e95950680a407c8d0a86c8da7e14362018-06-01T00:00:00Zhttps://doi.org/10.1038/s41467-018-04413-3https://doaj.org/toc/2041-1723Estrogen receptor alpha (ERα) plays critical roles in the etiology and treatment of breast cancer. Here the authors synthesize benzopyrans with variable side chains to identify antiestrogenic compounds and characterize OP-1074, a compound that exhibits pure antiestrogenic activity by inducing the degradation of ERα and possesses greater potency than tamoxifen or fulvestrant in a xenograft model.S. W. FanningL. Hodges-GallagherD. C. MylesR. SunC. E. FowlerI. N. PlantB. D. GreenC. L. HarmonG. L. GreeneP. J. KushnerNature PortfolioarticleScienceQENNature Communications, Vol 9, Iss 1, Pp 1-12 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q S. W. Fanning L. Hodges-Gallagher D. C. Myles R. Sun C. E. Fowler I. N. Plant B. D. Green C. L. Harmon G. L. Greene P. J. Kushner Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity
description	Estrogen receptor alpha (ERα) plays critical roles in the etiology and treatment of breast cancer. Here the authors synthesize benzopyrans with variable side chains to identify antiestrogenic compounds and characterize OP-1074, a compound that exhibits pure antiestrogenic activity by inducing the degradation of ERα and possesses greater potency than tamoxifen or fulvestrant in a xenograft model.
format	article
author	S. W. Fanning L. Hodges-Gallagher D. C. Myles R. Sun C. E. Fowler I. N. Plant B. D. Green C. L. Harmon G. L. Greene P. J. Kushner
author_facet	S. W. Fanning L. Hodges-Gallagher D. C. Myles R. Sun C. E. Fowler I. N. Plant B. D. Green C. L. Harmon G. L. Greene P. J. Kushner
author_sort	S. W. Fanning
title	Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity
title_short	Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity
title_full	Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity
title_fullStr	Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity
title_full_unstemmed	Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity
title_sort	specific stereochemistry of op-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity
publisher	Nature Portfolio
publishDate	2018
url	https://doaj.org/article/b6e95950680a407c8d0a86c8da7e1436
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Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity

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