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Updated: Aug 20, 2026

Homogeneous Time-resolved Förster Resonance Energy Transfer-based Assay for Detection of Insulin Secretion
Published on: May 10, 2018
The therapeutic potential of agents targeting the type I insulin-like growth factor receptor
1University of Minnesota Cancer Center, MMC 806, 420 Delaware Street SE, Minneapolis, MN 55455, USA.
Abstract:
The type I insulin-like growth factor receptor (IGF-1R) is a receptor tyrosine kinase that mediates insulin-like growth factor I (IGF-1) and IGF-2 signalling. Increased expression levels and/or enhanced activity of IGF-1R have been observed in many types of cancer. It is well documented that IGF-1R plays important roles in the proliferation, transformation, motility and metastasis of cancer cells. Therefore, IGF-1R has surfaced as an attractive target for cancer therapy. There are several aspects of this receptor that need to be considered when thinking about inhibitory strategies. In this review, several points relevant to targeting IGF-1R will be discussed, including the signalling pathways downstream of the receptor, the potential role for the insulin receptor in regulating IGF action and multiple cancer phenotypes regulated by this receptor. In addition, there are several strategies that could be used to inhibit IGF action. Inhibition of receptor function by lowering protein expression, decreasing kinase activity by small-molecule inhibitors, disrupting receptor function by monoclonal antibody blockade and neutralising circulating ligand all represent potential therapeutic strategies. As these strategies move forward to clinical trial, several important considerations need to be incorporated into the clinical trial design.
Insights
Targeting the type I insulin-like growth factor receptor (IGF-1R) offers a promising cancer therapy strategy. This review explores IGF-1R
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- The type I insulin-like growth factor receptor (IGF-1R) is a receptor tyrosine kinase.
- Increased IGF-1R expression/activity is linked to various cancers.
- IGF-1R regulates cancer cell proliferation, transformation, motility, and metastasis.
Purpose of the Study:
- To review therapeutic strategies targeting IGF-1R in cancer.
- To discuss downstream signaling pathways and cancer phenotypes regulated by IGF-1R.
- To consider the role of the insulin receptor in IGF action.
Main Methods:
- Review of existing literature on IGF-1R signaling and cancer.
- Analysis of various inhibitory strategies for IGF-1R.
- Discussion of clinical trial considerations for IGF-1R-targeted therapies.
Main Results:
- IGF-1R is a validated target for cancer therapy.
- Multiple therapeutic strategies exist, including small-molecule inhibitors, monoclonal antibodies, and ligand neutralization.
- Understanding downstream pathways and potential cross-talk with insulin receptors is crucial.
Conclusions:
- IGF-1R targeted therapies hold significant promise for cancer treatment.
- Careful consideration of clinical trial design is essential for successful therapeutic development.
- Inhibiting IGF-1R function through various mechanisms represents a viable approach to cancer therapy.
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