RON signalling promotes therapeutic resistance in ESR1 mutant breast cancer

Alpelisib (ALP) + fulvestrant (FUL) in patients (pts) with PIK3CA-mutated (mut) hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2–) advanced breast cancer (ABC) previously treated with cyclin-dependent kinase 4/6 inhibitor (CDKi) + aromatase inhibitor (AI): BYLieve study results.

(2020) Hope S. Rugo et al.   JOURNAL OF CLINICAL ONCOLOGY

The dysregulated pharmacology of clinically relevant ESR1 mutants is normalized by ligand-activated WT receptor

(2020) Kaitlyn J Andreano et al.   MOLECULAR CANCER THERAPEUTICS

Melphalan and exportin 1 inhibitors exert synergistic anti-tumor effects in preclinical models of human multiple myeloma

(2020) Joel G Turner et al.   CANCER RESEARCH

Combined inhibition of STAT3 and DNA repair in palbociclib-resistant ER-positive breast cancer

(2019) Nicole M. Kettner et al.   CLINICAL CANCER RESEARCH

A multicenter analysis of abemaciclib after progression on palbociclib in patients (pts) with hormone receptor-positive (HR+)/HER2- metastatic breast cancer (MBC).

(2019) Seth Andrew Wander et al.   JOURNAL OF CLINICAL ONCOLOGY

ESR1 mutations in breast cancer

(2019) Derek Dustin et al.   CANCER

Mechanisms of Resistance to CDK4/6 Inhibitors: Potential Implications and Biomarkers for Clinical Practice

(2019) Amelia McCartney et al.   Frontiers in Oncology

Practical treatment strategies and future directions after progression on CDK4/6 inhibition and endocrine therapy in advanced HR+/HER2- breast cancer

(2019) Sarah Sammons et al.   Clinical Breast Cancer

Overall Survival with Ribociclib plus Fulvestrant in Advanced Breast Cancer

(2019) Dennis J. Slamon et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

(2018) G N Hortobagyi et al.   ANNALS OF ONCOLOGY

A Living Biobank of Breast Cancer Organoids Captures Disease Heterogeneity

(2018) Norman Sachs et al.   CELL

A phase I trial to determine safety and pharmacokinetics of ASLAN002, an oral MET superfamily kinase inhibitor, in patients with advanced or metastatic solid cancers

(2018) Aflah Roohullah et al.   INVESTIGATIONAL NEW DRUGS

Phase III Randomized Study of Ribociclib and Fulvestrant in Hormone Receptor–Positive, Human Epidermal Growth Factor Receptor 2–Negative Advanced Breast Cancer: MONALEESA-3

(2018) Dennis J. Slamon et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase III study of taselisib (GDC-0032) + fulvestrant (FULV) v FULV in patients (pts) with estrogen receptor (ER)-positive, PIK3CA-mutant (MUT), locally advanced or metastatic breast cancer (MBC): Primary analysis from SANDPIPER.

(2018) Jose Baselga et al.   JOURNAL OF CLINICAL ONCOLOGY

The genetic landscape and clonal evolution of breast cancer resistance to palbociclib plus fulvestrant in the PALOMA-3 trial

(2018) Ben O'Leary et al.   Cancer Discovery

Clinical value of circulating ESR1 mutations for patients with metastatic breast cancer: a meta-analysis

(2018) Kai Zhang et al.   Cancer Management and Research

Overall Survival with Palbociclib and Fulvestrant in Advanced Breast Cancer

(2018) Nicholas C. Turner et al.   NEW ENGLAND JOURNAL OF MEDICINE

MONARCH 2: Abemaciclib in Combination With Fulvestrant in Women With HR+/HER2− Advanced Breast Cancer Who Had Progressed While Receiving Endocrine Therapy

(2017) George W. Sledge et al.   JOURNAL OF CLINICAL ONCOLOGY

CDK4/6 inhibition triggers anti-tumour immunity

(2017) Shom Goel et al.   NATURE

Discovery of naturally occurring ESR1 mutations in breast cancer cell lines modelling endocrine resistance

(2017) Lesley-Ann Martin et al.   Nature Communications

ESR1 mutations affect anti-proliferative responses to tamoxifen through enhanced cross-talk with IGF signaling

(2016) Luca Gelsomino et al.   BREAST CANCER RESEARCH AND TREATMENT

PlasmaESR1Mutations and the Treatment of Estrogen Receptor–Positive Advanced Breast Cancer

(2016) Charlotte Fribbens et al.   JOURNAL OF CLINICAL ONCOLOGY

Palbociclib and Letrozole in Advanced Breast Cancer

(2016) Richard S. Finn et al.   NEW ENGLAND JOURNAL OF MEDICINE

Heterogeneity and clinical significance of ESR1 mutations in ER-positive metastatic breast cancer patients receiving fulvestrant

(2016) Jill M. Spoerke et al.   Nature Communications

ActivatingESR1Mutations Differentially Affect the Efficacy of ER Antagonists

(2016) Weiyi Toy et al.   Cancer Discovery

Kinetics, prognostic and predictive values of ESR1 circulating mutations in metastatic breast cancer patients progressing on aromatase inhibitor

(2016) Florian Clatot et al.   Oncotarget

Prevalence of ESR1 Mutations in Cell-Free DNA and Outcomes in Metastatic Breast Cancer

(2016) Sarat Chandarlapaty et al.   JAMA Oncology

Preclinical Efficacy of Ron Kinase Inhibitors Alone and in Combination with PI3K Inhibitors for Treatment of sfRon-Expressing Breast Cancer Patient-Derived Xenografts

(2015) M. Bieniasz et al.   CLINICAL CANCER RESEARCH

Palbociclib in Hormone-Receptor–Positive Advanced Breast Cancer

(2015) Nicholas C. Turner et al.   NEW ENGLAND JOURNAL OF MEDICINE

Analysis of ESR1 mutation in circulating tumor DNA demonstrates evolution during therapy for metastatic breast cancer

(2015) Gaia Schiavon et al.   Science Translational Medicine

Ron Receptor Tyrosine Kinase Activation Confers Resistance to Tamoxifen in Breast Cancer Cell Lines

(2015) Rebecca J. McClaine et al.   NEOPLASIA

AR collaborates with ERα in aromatase inhibitor-resistant breast cancer

(2014) Yassine Rechoum et al.   BREAST CANCER RESEARCH AND TREATMENT

Invasive Lobular Carcinoma Cell Lines Are Characterized by Unique Estrogen-Mediated Gene Expression Patterns and Altered Tamoxifen Response

(2014) M. J. Sikora et al.   CANCER RESEARCH

Ganitumab with either exemestane or fulvestrant for postmenopausal women with advanced, hormone-receptor-positive breast cancer: a randomised, controlled, double-blind, phase 2 trial

(2013) John FR Robertson et al.   LANCET ONCOLOGY

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

(2013) Weiyi Toy et al.   NATURE GENETICS

Endocrine-Therapy-Resistant ESR1 Variants Revealed by Genomic Characterization of Breast-Cancer-Derived Xenografts

(2013) Shunqiang Li et al.   Cell Reports

Dynamic Reprogramming of the Kinome in Response to Targeted MEK Inhibition in Triple-Negative Breast Cancer

(2012) James S. Duncan et al.   CELL

Crystal Structure of the Sema-PSI Extracellular Domain of Human RON Receptor Tyrosine Kinase

(2012) Kinlin L. Chao et al.   PLoS One

AKT Inhibition Relieves Feedback Suppression of Receptor Tyrosine Kinase Expression and Activity

(2011) Sarat Chandarlapaty et al.   CANCER CELL

IGF1-R signals through the RON receptor to mediate pancreatic cancer cell migration

(2011) Dawn V. Jaquish et al.   CARCINOGENESIS

Tumor grafts derived from women with breast cancer authentically reflect tumor pathology, growth, metastasis and disease outcomes

(2011) Yoko S DeRose et al.   NATURE MEDICINE

Everolimus in Postmenopausal Hormone-Receptor–Positive Advanced Breast Cancer

(2011) José Baselga et al.   NEW ENGLAND JOURNAL OF MEDICINE

Gab2-Mediated Signaling Promotes Melanoma Metastasis

(2009) Basil Horst et al.   AMERICAN JOURNAL OF PATHOLOGY

Emerging role of insulin-like growth factor receptor inhibitors in oncology: early clinical trial results and future directions

(2009) A Gualberto et al.   ONCOGENE

Kinase-Selective Enrichment Enables Quantitative Phosphoproteomics of the Kinome across the Cell Cycle

(2008) Henrik Daub et al.   MOLECULAR CELL