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- Estrogen receptor signaling mechanisms.Adv Protein Chem Struct Biol. 2019; 116: 135-170
- ESR1 mutations-a mechanism for acquired endocrine resistance in breast cancer.Nat Rev Clin Oncol. 2015; 12: 573-583
- Alpelisib plus fulvestrant or letrozole demonstrates sustained benefits across subgroups of patients with PIK3CA-mutated HR+/HER2- advanced breast cancer.Oncologist. 2022; 27: S13-S14
- Overcoming endocrine resistance in breast cancer.Cancer Cell. 2020; 37: 496-513
- The genomic landscape of endocrine-resistant advanced breast cancers.Cancer Cell. 2018; 34: 427-438 e6
- Molecular changes in tamoxifen-resistant breast cancer: relationship between estrogen receptor, HER-2, and p38 mitogen-activated protein kinase.J Clin Oncol. 2005; 23: 2469-2476
- Luminal B breast cancer: molecular characterization, clinical management, and future perspectives.J Clin Oncol. 2014; 32: 2794-2803
- Inactivating NF1 mutations are enriched in advanced breast cancer and contribute to endocrine therapy resistance.Clin Cancer Res. 2020; 26: 608-622
- The prognostic effects of somatic mutations in ER-positive breast cancer.Nat Commun. 2018; 9: 3476
- Comprehensive profiling of DNA repair defects in breast cancer identifies a novel class of endocrine therapy resistance drivers.Clin Cancer Res. 2018; 24: 4887-4899
- Genomic profiling of ER(+) breast cancers after short-term estrogen suppression reveals alterations associated with endocrine resistance.Sci Transl Med. 2017; 9https://doi.org/10.1126/scitranslmed.aai7993
- Comprehensive molecular portraits of human breast tumours.Nature. 2012; 490: 61-70
- An estrogen receptor mutant with strong hormone-independent activity from a metastatic breast cancer.Cancer Res. 1997; 57: 1244-1249
- Emergence of constitutively active estrogen receptor-alpha mutations in pretreated advanced estrogen receptor-positive breast cancer.Clin Cancer Res. 2014; 20: 1757-1767
- ESR1 ligand-binding domain mutations in hormone-resistant breast cancer.Nat Genet Dec. 2013; 45: 1439-1445
- Primary endocrine resistance of ER+ breast cancer with ESR1 mutations interrogated by droplet digital PCR.NPJ Breast Cancer. 2022; 8: 58
- Early enrichment of ESR1 mutations and the impact on gene expression in presurgical primary breast cancer treated with aromatase inhibitors.Clin Cancer Res. 2019; 25: 7485-7496
- Circulating ESR1 mutations at the end of aromatase inhibitor adjuvant treatment and after relapse in breast cancer patients.Breast Cancer Res. 2018; 20: 40
- Updated results from MONALEESA-2, a phase III trial of first-line ribociclib plus letrozole versus placebo plus letrozole in hormone receptor-positive, HER2-negative advanced breast cancer.Ann Oncol. 2018; 29: 1541-1547
- Characterization of ESR1 mutations at metastatic relapse and outcome under first line aromatase inhibitor and palbociclib in the PADA-1 trial.Cancer Res. 2021; 81: CT189
- Analysis of ESR1 mutation in circulating tumor DNA demonstrates evolution during therapy for metastatic breast cancer.Sci Transl Med. 2015; 7: 313ra182
- ESR1 mutations are not a common mechanism of endocrine resistance in patients with estrogen receptor-positive breast cancer treated with neoadjuvant aromatase inhibitor therapy.Front Oncol. 2020; 10: 342
- ESR1 mutations are frequent in newly diagnosed metastatic and loco-regional recurrence of endocrine-treated breast cancer and carry worse prognosis.Breast Cancer Res. 2020; 22: 16
- Heterogeneity and clinical significance of ESR1 mutations in ER-positive metastatic breast cancer patients receiving fulvestrant.Nat Commun. 2016; 7: 11579
- D538G mutation in estrogen receptor-alpha: a novel mechanism for acquired endocrine resistance in breast cancer.Cancer Res. 2013; 73: 6856-6864
- Understanding the organ tropism of metastatic breast cancer through the combination of liquid biopsy tools.Eur J Cancer. 2021; 143: 147-157
- Prevalence of ESR1 mutations in cell-free DNA and outcomes in metastatic breast cancer: a secondary analysis of the BOLERO-2 clinical trial.JAMA Oncol. 2016; 2: 1310-1315
- Kinetics, prognostic and predictive values of ESR1 circulating mutations in metastatic breast cancer patients progressing on aromatase inhibitor.Oncotarget. 2016; 7: 74448-74459
- Activating ESR1 mutations in hormone-resistant metastatic breast cancer.Nat Genet. 2013; 45: 1446-1451
- Allele-specific chromatin recruitment and therapeutic vulnerabilities of ESR1 activating mutations.Cancer Cell. 2018; 33: 173-186 e5
- Estrogen receptor alpha mutations in breast cancer cells cause gene expression changes through constant activity and secondary effects.Cancer Res. 2021; 81: 539-551
- ESR1 mutant breast cancers show elevated basal cytokeratins and immune activation.Nat Commun. 2022; 13: 2011
- Mutation site and context dependent effects of ESR1 mutation in genome-edited breast cancer cell models.Breast Cancer Res. 2017; 19: 60
- The genetic landscape and clonal evolution of breast cancer resistance to palbociclib plus fulvestrant in the PALOMA-3 trial.Cancer Discov. 2018; 8: 1390-1403
- Unraveling the clinicopathological features driving the emergence of ESR1 mutations in metastatic breast cancer.NPJ Breast Cancer. 2018; 4: 22
- Clinical implications of monitoring ESR1 mutations by circulating tumor DNA in estrogen receptor positive metastatic breast cancer: a pilot study.Transl Oncol. 2020; 13: 321-328
- Acquired genomic alterations in circulating tumor DNA from patients receiving abemaciclib alone or in combination with endocrine therapy.J Clin Oncol. 2020; 38: 3519
- Plasma ESR1 mutations and the treatment of estrogen receptor-positive advanced breast cancer.J Clin Oncol. 2016; 34: 2961-2968
- Early circulating tumor DNA dynamics and clonal selection with palbociclib and fulvestrant for breast cancer.Nat Commun. 2018; 9: 896
- Clinical significance of PIK3CA and ESR1 mutations in circulating tumor DNA: analysis from the MONARCH 2 study of abemaciclib plus fulvestrant.Clin Cancer Res. 2022; 28: 1500-1506
- Phase I/II trial of exemestane, ribociclib, and everolimus in women with HR(+)/HER2(-) advanced breast cancer after progression on CDK4/6 inhibitors (TRINITI-1).Clin Cancer Res. 2021; 27: 4177-4185
- Impact of ESR1 mutations on endocrine therapy (ET) plus alpelisib benefit in patients with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-), PIK3CA-mutated, advanced breast cancer (ABC) who progressed on or after prior cyclin-dependent kinase inhibitor (CDK4/6i) therapy in the BYLieve trial.Cancer Res. 2022; 82: PD15-01
- Elacestrant (oral selective estrogen receptor degrader) versus standard endocrine therapy for estrogen receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer: results from the randomized phase III EMERALD trial.J Clin Oncol. 2022; : JCO2200338https://doi.org/10.1200/JCO.22.00338
- Rintodestrant (G1T48), an oral selective estrogen receptor degrader, in ER+/HER2– locally advanced or metastatic breast cancer: updated phase 1 results and dose selection.Cancer Res. 2021; 81: PS12-04
- Updated data from SERENA-1: a Phase 1 dose escalation and expansion study of the next generation oral SERD AZD9833 as a monotherapy and in combination with palbociclib, in women with ER-positive, HER2-negative advanced breast cancer.Cancer Res. 2021; 81: PS11-05
- AMEERA-1: Subgroup analyses of phase I/II study of amcenestrant (SAR439859), an oral selective estrogen receptor (ER) degrader (SERD), with palbociclib in postmenopausal women with ER+/human epidermal growth factor receptor 2-negative (HER2–) advanced breast cancer (aBC).Ann Oncol. 2021; 32: S457-S515
- A phase I study of LSZ102, an oral selective estrogen receptor degrader, with or without ribociclib or alpelisib, in patients with estrogen receptor-positive breast cancer.Clin Cancer Res. 2021; 27: 5760-5770
- A first-in-human phase 1a/b trial of LY3484356, an oral selective estrogen receptor (ER) degrader (SERD) in ER+ advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC): results from the EMBER study.J Clin Oncol. 2021; 39: 1050
- Activity and biomarker analyses from a phase Ia/b study of giredestrant (GDC-9545; G) with or without palbociclib (palbo) in patients with estrogen receptor-positive, HER2-negative locally advanced/metastatic breast cancer (ER+/HER2- LA/mBC).Cancer Res. 2022; 82 (Abstract nr PD13-07)https://doi.org/10.1158/1538-7445.SABCS21-PD13-07
- PROTAC: an effective targeted protein degradation strategy for cancer therapy.Front Pharmacol. 2021; 12: 692574
- Discovery of selective estrogen receptor covalent antagonists for the treatment of ERalpha(WT) and ERalpha(MUT) breast cancer.Cancer Discov. 2018; 8: 1176-1193
Hodges-Gallagher L, Sun R, Myles DC, Harmon CL, Kushner PJ. OP-1250 is a Complete Estrogen Receptor Antagonist (CERAN) that Lacks Agonist Activity on Cell Signaling and Proliferation in Breast Cancer Cells. presented at EORTC-NCI-AACR 2020.
- Phase I/II study of H3B-6545, a novel selective estrogen receptor covalent antagonist (SERCA), in estrogen receptor positive (ER+), human epidermal growth factor receptor 2 negative (HER2-) advanced breast cancer.J Clin Oncol. 2021; 39: 1018
- Preliminary Data From a Phase 1/2, Multicenter, Dose Escalation Study of OP-1250, an Oral CERAN/SERD, in Patients With Advanced and/or Metastatic Estrogen Receptor (ER)-Positive, HER2-Negative Breast Cancer.Cancer Res. 2022; 82: P1-17-12
- Open-label, phase 2, multicenter study of lasofoxifene (LAS) combined with abemaciclib (Abema) for treating pre- and postmenopausal women with locally advanced or metastatic ER+/HER2− breast cancer and an ESR1 mutation after progression on prior therapies.J Clin Oncol. 2022; 40 (abstr 1022))
- Longitudinal circulating tumor DNA (ctDNA) whole-exome sequencing (WES) in the phase Ib/II trial of palbociclib and bazedoxifene reveals genomic dynamics and clonal evolution with the acquisition of treatment resistance in hormone receptor-positive, HER2-negative (HR+ HER2-), advanced breast cancer (ABC).J Clin Oncol. 2022; 40: 1058
- Fulvestrant-palbociclib vs continuing aromatase inhibitor-palbociclib upon detection of circulating ESR1 mutation in HR+ HER2- metastatic breast cancer patients: Results of PADA-1, a UCBG-GINECO randomized phase 3 trial.Cancer Res. 2022; 82: GS3-05
- Randomised, open-label, multicentric phase III trial to evaluate the safety and efficacy of palbociclib in combination with endocrine therapy, guided by ESR1 mutation monitoring in oestrogen receptor-positive, HER2-negative metastatic breast cancer patients: study design of PADA-1.BMJ Open. 2022; 12: e055821
- Circulating ESR1 mutation detection rate and early decrease under first line aromatase inhibitor and palbociclib in the PADA-1 trial (UCBG-GINECO).Cancer Res. 2019; 79: PD2-PD06
- Steroid hormone receptor and infiltrating immune cell status reveals therapeutic vulnerabilities of ESR1-mutant breast cancer.Cancer Res. 2021; 81: 732-746