EGFR family: Structure physiology signalling and therapeutic targets †
Abstract
There are four members of the EGFR family: EGFR, erbB2, erbB3 and erbB4. These receptors form ligand-activated oligomers which regulate intracellular processes via an oligomeric tyrosine kinase scaffold. The receptors are activated when the extracellular domain undergoes a conformational change which facilitates either homo- or hetero-oligomerization with other family members. The absence of one EGFR family member leads to embryonic or early post-natal death due to implantation, central nervous system or cardiac defects. Many mouse models of defective or deficient EGFR family members are available for studying physiology and/or pathology of EGFR family members. Sophisticated antibody and kinase inhibitors which target different family members have been designed, produced. EGFR and erbB2 are frequently activated, over expressed or mutated in many common cancers and the antagonists and/or inhibitors of EGFR and/or erbB2 signalling have already been shown to have therapeutic benefits for cancer patients.
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EGFR is implicated in cell proliferation, mitosis, and cancer development.
“and is implicated in cell proliferation, mitosis, and cancer development.99,103,104”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [104]
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Epidermal growth factor receptor targeting in cancer: a review of trends and strategies
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- Authors
- Burgess, A. W.
- Affiliations
- Ludwig Cancer Research (AU)
- Corresponding author
- Burgess, Antony W.
- ORCID
- Burgess, Antony W.
- Venue
- Growth Factors
- Publisher
- Informa UK Limited
- Published
- 2008-01
- Volume
- 26
- Issue
- 5
- Pages
- 263-274
- ISSN
- 0897-7194 (ISSN-L)
- 1029-2292
- OpenAlex
- W2161879730
- Cited by
- 288
- References
- 152
- Citations by year
- 2026: 14 · 2025: 16 · 2024: 24 · 2023: 17 · 2022: 9 · 2021: 11 · 2020: 15 · 2019: 6 · 2018: 13 · 2017: 15 · 2016: 13 · 2015: 17 · 2014: 16 · 2013: 24 · 2012: 18
- FWCI
- 10.56
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Growth Factors (publishedVersion)
- PubMed (publishedVersion)
- 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 › Metabolism, Diabetes, and Cancer
- Keywords
- ErbB receptors, epidermal growth factor receptor, ERBB2, HER3, ErbB4, receptor oligomerization, tyrosine kinase signaling, receptor conformational change, hetero-oligomerization, embryonic lethality, mouse model, kinase inhibitors, cancer therapy
- MeSH terms
- Animals, Humans, Models, Genetic, Models, Molecular, Protein Conformation, Structure-Activity Relationship, Signal Transduction, Protein Structure, Tertiary, Erb-b2 Receptor Tyrosine Kinases, Genes, erbB, Dimerization, Receptor, ErbB-3, Mice, ErbB Receptors
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