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Updated: Mar 19, 2026

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
Published on: September 19, 2018
Emerging Receptor Tyrosine Kinase Drug Targets: Implications for Antibody-Based Therapies for Oncology and
Theresa M LaVallee1, Diego Alvarado1, Andrew J Garton1
1Kolltan Pharmaceuticals, Inc., New Haven, CT.
Abstract:
Protein kinases play a critical regulatory role in essentially every aspect of cell biology. Of the 518 known kinases, the most successful class for drug targeting is the receptor tyrosine kinase (RTK) family consisting of 58 distinct and diverse members. RTKs regulate a broad range of cellular functions, including proliferation, differentiation, survival, and apoptosis and have been intensively studied in development and cancer. Targeting of RTKs has resulted in many marketed small molecule and antibody-based drugs in a number of different solid tumors and hematological malignancies, and more recently in inflammatory diseases such as idiopathic pulmonary fibrosis. In this review, we discuss some of the RTKs in cancer in which drugs targeting the ErbB family (EGFR, HER2, and ErbB3) and KIT have had meaningful clinical benefit to cancer patients, RTKs' emerging role in regulating innate immunity, and the potential to explore targeting RTKs outside of oncology.
Insights
Receptor tyrosine kinases (RTKs) are crucial for cell biology and successful drug targets in cancer and inflammatory diseases. This review highlights RTKs in cancer therapy, immunity, and potential non-oncology applications.
Area of Science:
- Cell Biology
- Molecular Biology
- Pharmacology
Background:
- Protein kinases regulate fundamental cellular processes.
- Receptor tyrosine kinases (RTKs) are a key class of protein kinases, with 58 members, extensively studied in development and cancer.
- Targeting RTKs has yielded numerous drugs for various cancers and inflammatory conditions.
Purpose of the Study:
- To review the clinical benefits of targeting specific RTKs in cancer, focusing on the ErbB family (EGFR, HER2, ErbB3) and KIT.
- To discuss the emerging role of RTKs in regulating innate immunity.
- To explore the potential of targeting RTKs beyond oncology.
Main Methods:
- Literature review of RTKs in cancer therapy.
- Analysis of RTK involvement in innate immunity.
- Exploration of non-oncology therapeutic applications of RTKs.
Main Results:
- Drugs targeting ErbB family members (EGFR, HER2, ErbB3) and KIT have shown significant clinical efficacy in various cancers.
- RTKs play an increasingly recognized role in the regulation of innate immune responses.
- There is potential for developing RTK-targeted therapies for diseases outside of cancer.
Conclusions:
- RTK-targeting therapies have transformed cancer treatment and show promise in other diseases.
- Understanding RTK roles in immunity opens new therapeutic avenues.
- Further research into non-oncology RTK targets is warranted.
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