Cited by 874HER2/EGFR in Cancer ResearchLung Cancer Treatments and MutationsPI3K/AKT/mTOR signaling in cancer

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Targeting ligand-activated ErbB2 signaling inhibits breast and prostate tumor growth

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Agus, David B, Akita, Robert W, Fox, William D, Lewis, Gail D, Higgins, Brian, Pisacane, Paul I, Lofgren, Julie A, Tindell, Charles, Evans, Douglas P, Maiese, Krista, Scher, Howard I, Sliwkowski, Mark X·2002·Cancer Cell

DOI 10.1016/s1535-6108(02)00097-1

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Abstract

ErbB2 is a ligand-less member of the ErbB receptor family that functions as a coreceptor with EGFR, ErbB3, and ErbB4. Here, we describe an approach to target ErbB2's role as a coreceptor using a monoclonal antibody, 2C4, which sterically hinders ErbB2's recruitment into ErbB ligand complexes. Inhibition of ligand-dependent ErbB2 signaling by 2C4 occurs in both low- and high-ErbB2-expressing systems. Since the ErbB3 receptor contains an inactive tyrosine kinase domain, 2C4 is very effective in blocking heregulin-mediated ErbB3-ErbB2 signaling. We demonstrate that the in vitro and in vivo growth of several breast and prostate tumor models is inhibited by 2C4 treatment.

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Authors: Agus, D. B., Akita, R. W., Fox, W. D., Lewis, G. D., Higgins, B., Pisacane, P. I., Lofgren, J. A., Tindell, C., Evans, D. P., Maiese, K., Scher, H. I., & Sliwkowski, M. X.
Affiliations: Cedars-Sinai Medical Center (US)
Genentech (US)
Memorial Sloan Kettering Cancer Center (US)
Corresponding author: Sliwkowski, Mark X
ORCID: Agus, David B
Scher, Howard I
Sliwkowski, Mark X
Venue: Cancer Cell
Publisher: Elsevier BV
Published: 2002-08
Volume: 2
Issue: 2
Pages: 127-137
ISSN: 1535-6108 (ISSN-L)
DOI: 10.1016/s1535-6108(02)00097-1
OpenAlex: W2014457594
Cited by: 873
References: 83
Citations by year: 2026: 2 · 2025: 10 · 2024: 21 · 2023: 38 · 2022: 21 · 2021: 21 · 2020: 28 · 2019: 29 · 2018: 27 · 2017: 24 · 2016: 38 · 2015: 48 · 2014: 69 · 2013: 59 · 2012: 51
FWCI: 16.85
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/open-access/userlicense/1.0/ (vor, 4003 d)
Locations: Cancer Cell (publishedVersion)
PubMed (publishedVersion)
Funders: PepsiCo
Topics: Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › PI3K/AKT/mTOR signaling in cancer
Keywords: ERBB2, HER2, HER3, neuregulin-1, ErbB receptor family, breast cancer, prostate cancer, tumor growth inhibition, tyrosine kinase inhibitors
MeSH terms: Androgens, Animals, Antibodies, Monoclonal, Antineoplastic Agents, Breast Neoplasms, Cell Division, Female, Humans, Ligands, Male, Neoplasm Transplantation, Prostatic Neoplasms, Protein Binding, RNA, Messenger, Time Factors, Transplantation, Heterologous, Tumor Cells, Cultured, Signal Transduction, Gene Expression Regulation, Neoplastic, Erb-b2 Receptor Tyrosine Kinases, Neuregulin-1, Receptor, ErbB-3, Mice

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Targeting ligand-activated ErbB2 signaling inhibits breast and prostate tumor growth

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