Endoglin-Targeted Therapeutics in Vascular Biology

Summary

Endoglin (CD105) is a transmembrane glycoprotein and auxiliary receptor for transforming growth factor-β (TGF-β) family ligands, highly expressed on proliferating endothelial cells. It modulates signalling through TGF-β1, TGF-β3 and bone morphogenetic proteins such as BMP9, thereby influencing angiogenesis, vascular remodelling and endothelial homeostasis. Dysregulated endoglin expression or function underlies a spectrum of vascular disorders, from hereditary haemorrhagic telangiectasia to tumour hypervascularisation and metabolic-associated steatohepatitis. Therapeutic strategies have focused on monoclonal antibodies that bind endoglin to block pathogenic angiogenesis, on soluble endoglin as a biomarker and ligand trap, and on small-molecule or antibody-based modulation of endoglin–BMP9 interactions. Preclinical and early clinical studies demonstrate that endoglin-targeted agents can restore endothelial quiescence, reduce fibrosis and impede tumour neovascular networks while highlighting challenges related to receptor heterogeneity, off-target effects and the dynamic balance of pro- and anti-angiogenic signalling.

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Endoglin-Targeted Therapeutics in Vascular Biology publication trend

The graph below shows the total number of articles in endoglin-targeted therapeutics in vascular biology across all publications each year (not limited to Nature Index journals).

Technical terms

Endoglin (CD105): A TGF-β co-receptor on endothelial cells that regulates angiogenesis and vascular remodelling.

Monoclonal antibody (mAb): A homogenous antibody engineered to bind a specific molecular target.

Soluble endoglin (sEng): The extracellular fragment of endoglin released into circulation that can modulate ligand availability.

BMP9: A member of the TGF-β superfamily critical for vascular quiescence and endothelial integrity.

Hepatocellular carcinoma (HCC): The most common primary liver malignancy, often characterised by aberrant angiogenesis.

References

  1. Anti-Endoglin monoclonal antibody prevents the progression of liver sinusoidal endothelial inflammation and fibrosis in MASH. Life Sciences (2025).
  2. Endoglin Requirement for BMP9 Signaling in Endothelial Cells Reveals New Mechanism of Action for Selective Anti-Endoglin Antibodies. PLOS ONE (2012).
  3. Role of Endoglin (CD105) in the Progression of Hepatocellular Carcinoma and Anti-Angiogenic Therapy. International Journal of Molecular Sciences (2018).
  4. Endoglin Is an Accessory Protein That Interacts with the Signaling Receptor Complex of Multiple Members of the Transforming Growth Factor-β Superfamily*. Journal of Biological Chemistry (1999).
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