Target intelligence / Profile preview

Angiopoietin-1; Angiopoietin-2 (Ang-1; Ang-2)

Target
Ang-1; Ang-2
Molecular classification
Growth factor, Ligand, Cytokine
01

Overview

Angiopoietin-1 and Angiopoietin-2 are secreted glycoproteins that bind to and modulate the activity of the Tie2 receptor on endothelial cells, controlling blood vessel formation, stabilization (by Angiopoietin-1) and destabilization (by Angiopoietin-2). Angiopoietin-1 promotes vessel maturation, endothelial survival, and integrity. Angiopoietin-2 acts as a context-dependent antagonist or partial agonist, promoting vascular permeability and regression particularly under pathological conditions such as cancer and inflammation. The Angiopoietins interact with VEGF signaling, and their balance is critical in maintaining vascular homeostasis. Both are prominent therapeutic targets in cancer, retinal/vascular disease, and chronic inflammatory settings. Measuring their circulating levels provides prognostic information in oncology and cardiovascular disease.

Other names
Angiopoietin 1 (Angpt1)Angiopoietin 2 (Angpt2)ANGPT1ANGPT2Ang-1Ang-2
02

Mechanism of action

Antagonism or blockade of Ang-2 (restores vascular stability, limits tumor growth and inflammation) Tie2 agonism/activation by Ang-1 (promotes vessel maturation and stabilization) Dual inhibition of Ang-2 and VEGF (synergistic antiangiogenic effect)

03

Biological functions

Regulation of angiogenesis (formation of new blood vessels)Vascular stability and maturation (Ang-1)Vascular destabilization and regression (Ang-2)Endothelial cell survival (Ang-1)Endothelial cell death/proliferation (Ang-2)Inflammation regulation
04

Disease associations

Cancer (regulates tumor angiogenesis and immune cell infiltration)Cardiovascular disease (critical for vessel maintenance, implicated in atherosclerosis, ischemia)Retinal/choroidal vascular diseases, diabetic retinopathyInflammationOther: Sepsis, nephropathy, liver diseases
05

Safety considerations

Vascular regression and increased permeability with Ang-2 antagonism (may destabilize normal vasculature)Immune-related adverse events when combining with immunotherapiesPotential impact on wound healing, hypertension, edema
06

Interacting drugs

Anti-Angiopoietin-2 antibodies (experimental/clinical)

4 more in the full profile.

07

Biomarkers

Plasma levels of Ang-1 and Ang-2 (diagnostic and prognostic in cancer, e.g., hepatocellular carcinoma)Vascular/endothelial markers (retinal diseases, cardiovascular risk)

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