Structural underpinnings of oestrogen receptor mutations in endocrine therapy resistance

JA Katzenellenbogen, CG Mayne… - Nature Reviews …, 2018 - nature.com
Oestrogen receptor-α (ERα), a key driver of breast cancer, normally requires oestrogen for
activation. Mutations that constitutively activate ERα without the need for hormone binding …

Estrogen receptor mutations and functional consequences for breast cancer

C Thomas, JÅ Gustafsson - Trends in Endocrinology & Metabolism, 2015 - cell.com
A significant number of estrogen receptor α (ERα)-positive breast tumors develop resistance
to endocrine therapy and recur with metastatic disease. Several mechanisms of endocrine …

ESR1 ligand-binding domain mutations in hormone-resistant breast cancer

W Toy, Y Shen, H Won, B Green, RA Sakr, M Will, Z Li… - Nature …, 2013 - nature.com
Seventy percent of breast cancers express estrogen receptor (ER), and most of these are
sensitive to ER inhibition. However, many such tumors for unknown reasons become …

[HTML][HTML] A closer look at estrogen receptor mutations in breast cancer and their implications for estrogen and antiestrogen responses

L Clusan, P Le Goff, G Flouriot, F Pakdel - International journal of …, 2021 - mdpi.com
Breast cancer (BC) is the most common cancer among women worldwide. More than 70% of
BC cases express estrogen receptor alpha (ERα), a central transcription factor that …

Estrogen receptor mutations and changes in downstream gene expression and signaling

I Barone, L Brusco, SAW Fuqua - Clinical Cancer Research, 2010 - AACR
Estrogens play a crucial role in regulating the growth and differentiation of breast cancers,
with approximately two thirds of all breast tumors expressing the estrogen receptor alpha …

ESR1 mutations—a mechanism for acquired endocrine resistance in breast cancer

R Jeselsohn, G Buchwalter, C De Angelis… - Nature reviews Clinical …, 2015 - nature.com
Approximately 70% of breast cancers are oestrogen receptor α (ER) positive, and are,
therefore, treated with endocrine therapies. However, about 25% of patients with primary …

The changing role of ER in endocrine resistance

A Nardone, C De Angelis, MV Trivedi, CK Osborne… - The Breast, 2015 - Elsevier
Estrogen receptor (ER) is expressed in approximately 70% of newly diagnosed breast
tumors. Although endocrine therapy targeting ER is highly effective, intrinsic or acquired …

[HTML][HTML] Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding …

SW Fanning, CG Mayne, V Dharmarajan, KE Carlson… - elife, 2016 - elifesciences.org
Somatic mutations in the estrogen receptor alpha (ERα) gene (ESR1), especially Y537S and
D538G, have been linked to acquired resistance to endocrine therapies. Cell-based studies …

D538G mutation in estrogen receptor-α: A novel mechanism for acquired endocrine resistance in breast cancer

K Merenbakh-Lamin, N Ben-Baruch, A Yeheskel… - Cancer research, 2013 - AACR
Resistance to endocrine therapy occurs in virtually all patients with estrogen receptor α
(ERα)-positive metastatic breast cancer, and is attributed to various mechanisms including …

[HTML][HTML] Allele-specific chromatin recruitment and therapeutic vulnerabilities of ESR1 activating mutations

R Jeselsohn, JS Bergholz, M Pun, MI Cornwell, W Liu… - Cancer cell, 2018 - cell.com
Estrogen receptor α (ER) ligand-binding domain (LBD) mutations are found in a substantial
number of endocrine treatment-resistant metastatic ER-positive (ER+) breast cancers. We …