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...

Description complète

Enregistré dans:

Détails bibliographiques
Auteurs principaux:	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
Format:	article
Langue:	EN
Publié:	Nature Portfolio 2018
Sujets:	Science Q
Accès en ligne:	https://doaj.org/article/b6e95950680a407c8d0a86c8da7e1436
Tags:	Ajouter un tag Pas de tags, Soyez le premier à ajouter un tag!

id	oai:doaj.org-article:b6e95950680a407c8d0a86c8da7e1436
record_format	dspace
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
work_keys_str_mv	AT swfanning specificstereochemistryofop1074disruptsestrogenreceptoralphahelix12andconferspureantiestrogenicactivity AT lhodgesgallagher specificstereochemistryofop1074disruptsestrogenreceptoralphahelix12andconferspureantiestrogenicactivity AT dcmyles specificstereochemistryofop1074disruptsestrogenreceptoralphahelix12andconferspureantiestrogenicactivity AT rsun specificstereochemistryofop1074disruptsestrogenreceptoralphahelix12andconferspureantiestrogenicactivity AT cefowler specificstereochemistryofop1074disruptsestrogenreceptoralphahelix12andconferspureantiestrogenicactivity AT inplant specificstereochemistryofop1074disruptsestrogenreceptoralphahelix12andconferspureantiestrogenicactivity AT bdgreen specificstereochemistryofop1074disruptsestrogenreceptoralphahelix12andconferspureantiestrogenicactivity AT clharmon specificstereochemistryofop1074disruptsestrogenreceptoralphahelix12andconferspureantiestrogenicactivity AT glgreene specificstereochemistryofop1074disruptsestrogenreceptoralphahelix12andconferspureantiestrogenicactivity AT pjkushner specificstereochemistryofop1074disruptsestrogenreceptoralphahelix12andconferspureantiestrogenicactivity
_version_	1718383298819915776

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

Documents similaires