Ontology highlight
ABSTRACT:
SUBMITTER: Joseph JD
PROVIDER: S-EPMC4961458 | biostudies-literature | 2016 Jul
REPOSITORIES: biostudies-literature
Joseph James D JD Darimont Beatrice B Zhou Wei W Arrazate Alfonso A Young Amy A Ingalla Ellen E Walter Kimberly K Blake Robert A RA Nonomiya Jim J Guan Zhengyu Z Kategaya Lorna L Govek Steven P SP Lai Andiliy G AG Kahraman Mehmet M Brigham Dan D Sensintaffar John J Lu Nhin N Shao Gang G Qian Jing J Grillot Kate K Moon Michael M Prudente Rene R Bischoff Eric E Lee Kyoung-Jin KJ Bonnefous Celine C Douglas Karensa L KL Julien Jackaline D JD Nagasawa Johnny Y JY Aparicio Anna A Kaufman Josh J Haley Benjamin B Giltnane Jennifer M JM Wertz Ingrid E IE Lackner Mark R MR Nannini Michelle A MA Sampath Deepak D Schwarz Luis L Manning Henry Charles HC Tantawy Mohammed Noor MN Arteaga Carlos L CL Heyman Richard A RA Rix Peter J PJ Friedman Lori L Smith Nicholas D ND Metcalfe Ciara C Hager Jeffrey H JH
eLife 20160713
ER-targeted therapeutics provide valuable treatment options for patients with ER+ breast cancer, however, current relapse and mortality rates emphasize the need for improved therapeutic strategies. The recent discovery of prevalent ESR1 mutations in relapsed tumors underscores a sustained reliance of advanced tumors on ERα signaling, and provides a strong rationale for continued targeting of ERα. Here we describe GDC-0810, a novel, non-steroidal, orally bioavailable selective ER downregulator (S ...[more]