IGF-1 receptor (IGF1R)
The IGF-1 receptor is a growth-factor receptor that many cancers use to survive; a decade of antibodies and kinase inhibitors against it failed in trials, a cautionary tale in oncology drug development.
Overview
Insulin-like growth factor 1 receptor is a receptor tyrosine kinase closely related to the insulin receptor that promotes growth and survival through PI3K-AKT and MAPK signalling. Antibodies (ganitumab, figitumumab, dalotuzumab) and small molecules (linsitinib) were tested in lung, breast, pancreatic and Ewing sarcoma without meeting their endpoints, partly because of insulin receptor compensation and hyperglycaemia. The only approved IGF1R antibody, teprotumumab, treats thyroid eye disease rather than cancer.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · The IGF-1 receptor is a growth-factor receptor that many cancers use to survive; a decade of antibodies and kinase inhibitors against it failed in trials, a cautionary tale in oncology drug development.
- 1 · What it is
The IGF-1 receptor is a growth-factor receptor that many cancers use to survive; a decade of antibodies and kinase inhibitors against it failed in trials, a cautionary tale in oncology drug development.
- 2 · What goes wrong in cancer
A heterotetrameric receptor kinase activated by IGF-1 and IGF-2; hybrid receptors with the insulin receptor complicate selective blockade.
- 3 · How drugs use it
No product in this corpus aims at IGF-1 receptor (IGF1R) yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
External identifiers
Biology
A heterotetrameric receptor kinase activated by IGF-1 and IGF-2; hybrid receptors with the insulin receptor complicate selective blockade.
- Ewing sarcoma, breast, lung and pancreatic cancers (expressed)
- Most normal tissues at lower levels
Latest papers
topQuery for this target: (TITLE:"IGF-1 receptor" OR ABSTRACT:"IGF-1 receptor" OR TITLE:"IGF1R" OR ABSTRACT:"IGF1R") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about IGF-1 receptor (IGF1R), not a curated reading list.