T De Marchi, JA Foekens, A Umar, JWM Martens - Drug discovery today, 2016 - Elsevier
Highlights•Endocrine treatment resistance in estrogen receptor positive breast cancer.•Technological advancements for the discovery of biomarkers of endocrine …
M Fan, A Park, KP Nephew - Molecular endocrinology, 2005 - academic.oup.com
In estrogen target cells, estrogen receptor-α (ERα) protein levels are strictly regulated. Although receptor turnover is a continuous process, dynamic fluctuations in receptor levels …
HS Seo, DG DeNardo, Y Jacquot, I Laïos… - Breast cancer research …, 2006 - Springer
Genistein and apigenin are phytoestrogens present in commercial preparations used for the treatment of postmenopausal symptoms. In this study, we assessed the influence of these …
NB Berry, M Fan, KP Nephew - Molecular endocrinology, 2008 - academic.oup.com
Cellular levels of estrogen receptor-α (ERα) protein are regulated primarily by the ubiquitin- proteasome pathway. Dynamic interactions between ERα and the protein degradation …
Y Demizu, K Okuhira, H Motoi, A Ohno, T Shoda… - Bioorganic & medicinal …, 2012 - Elsevier
We designed and synthesized estrogen receptor (ER) degradation inducers 5, 6, and 7, which crosslink the ER and the cellular inhibitor of apoptosis protein 1 (cIAP1). Compounds …
AL Portbury, SM Ronnebaum, M Zungu… - Journal of molecular and …, 2012 - Elsevier
Awareness of the regulation of cell signaling by post-translational ubiquitination has emerged over the past 2 decades. Like phosphorylation, post-translational modification of …
Tamoxifen remains a cornerstone of adjuvant therapy for patients with early stage breast cancer and oestrogen-receptor-positive tumours. Accurate markers of tamoxifen resistance …
G Leclercq, M Lacroix, I Laïos… - Current cancer drug …, 2006 - ingentaconnect.com
Estrogen receptors (α and ß) are members of the steroid/thyroid nuclear receptors superfamily of ligand-dependent transcription factors. Impact of the? isoform of estrogen …
Targeting selective estrogen subtype receptors through typical medicinal chemistry approaches is based on occupancy-driven pharmacology. In occupancy-driven …