Receptor Tyrosine Kinase-Targeted Cancer Therapy
Open accessAbstract
In the past two decades, several molecular targeted inhibitors have been developed and evaluated clinically to improve the survival of patients with cancer. Molecular targeted inhibitors inhibit the activities of pathogenic tyrosine kinases. Particularly, aberrant receptor tyrosine kinase (RTK) activation is a potential therapeutic target. An increased understanding of genetics, cellular biology and structural biology has led to the development of numerous important therapeutics. Pathogenic RTK mutations, deletions, translocations and amplification/over-expressions have been identified and are currently being examined for their roles in cancers. Therapies targeting RTKs are categorized as small-molecule inhibitors and monoclonal antibodies. Studies are underway to explore abnormalities in 20 types of RTK subfamilies in patients with cancer or other diseases. In this review, we describe representative RTKs important for developing cancer therapeutics and predicting or evaluated resistance mechanisms.
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“Genetic alterations in components of RTK signaling pathways are frequently found in cancer and can lead to constitutive activation of downstream pathways such as RAS/ RAF/MAPK, PI3K/AKT, and JAK/STAT [68, 69].”
- Authors
- Yamaoka, T., Kusumoto, S., Ando, K., Ohba, M., & Ohmori, T.
- Affiliations
- SHOWA Medical University (JP)
- Division of Allergology and Respiratory Medicine, Department of Medicine, Showa University School of Medicine, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, Japan
- Corresponding author
- Yamaoka, Toshimitsu
- Venue
- International Journal of Molecular Sciences
- Publisher
- MDPI AG
- Published
- 2018-11-06
- Volume
- 19
- Issue
- 11
- Pages
- 3491
- ISSN
- 1422-0067 (ISSN-L)
- PMC
- PMC6274851
- OpenAlex
- W2900390128
- Cited by
- 297
- References
- 24
- Citations by year
- 2026: 19 · 2025: 35 · 2024: 49 · 2023: 44 · 2022: 52 · 2021: 40 · 2020: 43 · 2019: 14 · 2018: 1
- FWCI
- 4.38
- Type
- journal article
- Language
- en
- Open access
- gold
- dx.doi.org
- Licence
- Locations
- International Journal of Molecular Sciences (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Funders
- Japan Society for the Promotion of Science (16K09590)
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
- Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
- Health Sciences › Medicine › Pathology and Forensic Medicine › Cancer Mechanisms and Therapy
- Keywords
- receptor tyrosine kinase, targeted cancer therapy, tyrosine kinase inhibitors, small molecule inhibitors, monoclonal antibodies, drug resistance mechanisms, cancer therapeutics
- MeSH terms
- Animals, Antineoplastic Agents, Antineoplastic Combined Chemotherapy Protocols, Clinical Trials as Topic, Humans, Neoplasms, Biomarkers, Tumor, Signal Transduction, Gene Expression Regulation, Neoplastic, Treatment Outcome, Drug Resistance, Neoplasm, Receptor Protein-Tyrosine Kinases, Protein Kinase Inhibitors, Molecular Targeted Therapy, ErbB Receptors
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