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Insulin-like growth factor 1; Insulin-like growth factor 2 (IGF-1; IGF-2)

Target
IGF-1; IGF-2
Molecular classification
Polypeptide hormone, Growth factor, Ligand for receptor tyrosine kinases (IGF1R, IR-A)
01

Overview

Insulin-like growth factor 1 (IGF-1) and insulin-like growth factor 2 (IGF-2) are peptide hormones structurally similar to proinsulin, consisting of a single polypeptide chain (IGF-1: 70 amino acids; IGF-2: 67 amino acids)[4][6]. IGF-1 is produced mainly in the liver under growth hormone regulation and mediates most of its growth-promoting effects, whereas IGF-2 plays a dominant role in fetal development and tissue growth[7][3][5]. Both IGF-1 and IGF-2 bind to the IGF1R (a receptor tyrosine kinase) and to IR-A with high affinity, activating downstream signaling pathways (especially the PI3K/Akt pathway) to stimulate cell proliferation, inhibit apoptosis, and regulate metabolic homeostasis[4][3][2]. Aberrant IGF signaling is implicated in cancer progression, resistance to therapy, and other diseases, making both IGFs—and their receptor IGF1R—important drug targets and clinical biomarkers[9][4][3][7].

Other names
Somatomedin C (IGF-1)IGF-IIGF-II
02

Mechanism of action

Ligand blockade (preventing IGF1/IGF2 from binding IGF1R) - Receptor downregulation or inhibition of kinase activity - Induction of apoptosis in cancer cells by suppressing survival signaling pathways

03

Biological functions

Cell growthCell proliferationInhibition of apoptosis (cell death)Signal transductionFetal development (IGF-2)Metabolic regulationTissue repair and regeneration
04

Disease associations

Cancer (tumor growth, drug resistance)Growth disorders (short stature, acromegaly)Cardiovascular diseaseNeurodegenerative disease (neural development, neuroprotection)Other (metabolic syndrome, diabetes, aging)
05

Safety considerations

Growth-promoting and anti-apoptotic activity can cause or worsen malignancySystemic effects due to endocrine and paracrine signalingRisk of hypoglycemia (cross-reactivity with insulin signaling)
06

Interacting drugs

Anti-IGF1R monoclonal antibodies (e.g., figitumumab, ganitumab)

2 more in the full profile.

07

Biomarkers

Serum IGF-1 and IGF-2 levels (used in growth disorders, cancer prognosis)IGF1R expression (immunohistochemistry, gene expression)

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