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Targeting the fibroblast growth factor receptors for the treatment of cancer
Steven M Lemieux1, M Kyle Hadden
1Department of Pharmaceutical Sciences, University of Connecticut, 69 N Eagleville Rd, Unit 3092, Storrs, CT 06269, USA.
Abstract:
Receptor tyrosine kinases (RTKs) are transmembrane proteins that play a critical role in stimulating signal transduction cascades to influence cell proliferation, growth, and differentiation and they have also been shown to promote angiogenesis when they are up-regulated or mutated. For this reason, their dysfunction has been implicated in the development of human cancer. Over the past decade, much attention has been devoted to developing inhibitors and antibodies against several classes of RTKs, including vascular endothelial growth factor receptors (VEGFRs), epidermal growth factor receptors (EGFRs), and platelet-derived growth factor receptors (PDGFRs). More recently, interest in the fibroblast growth factor receptor (FGFR) class of RTKs as a drug target for the treatment of cancer has emerged. Signaling through FGFRs is critical for normal cellular function and their dysregulation has been linked to various malignancies such as breast and prostate cancer. This review will focus on the current state of both small molecules and antibodies as FGFR inhibitors to provide insight into their development and future potential as anti-cancer agents.
Insights
Receptor tyrosine kinases (RTKs) are crucial for cell growth but drive cancer when mutated. This review explores fibroblast growth factor receptor (FGFR) inhibitors as potential anti-cancer agents.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Receptor tyrosine kinases (RTKs) regulate cell proliferation, growth, differentiation, and angiogenesis.
- RTK dysfunction, including upregulation or mutation, is implicated in human cancer development.
- Previous research focused on inhibitors for VEGFRs, EGFRs, and PDGFRs.
Purpose of the Study:
- To review the current development of small molecules and antibodies targeting fibroblast growth factor receptors (FGFRs).
- To provide insight into FGFR inhibitors as potential anti-cancer agents.
- To highlight the role of FGFR signaling in malignancies like breast and prostate cancer.
Main Methods:
- Literature review of small molecule and antibody-based FGFR inhibitors.
- Analysis of FGFR signaling pathways in cancer.
- Evaluation of the therapeutic potential of FGFR inhibitors.
Main Results:
- FGFRs are increasingly recognized as critical drug targets in oncology.
- Dysregulation of FGFR signaling is linked to various cancers.
- Development of both small molecule and antibody inhibitors for FGFRs is advancing.
Conclusions:
- FGFR inhibitors represent a promising therapeutic strategy for cancer treatment.
- Further research and development are needed to optimize FGFR-targeted therapies.
- Targeting FGFRs holds potential for treating malignancies including breast and prostate cancer.
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