Peptide Inhibitors of Vascular Endothelial Growth Factor A: Current Situation and Perspectives

Vascular endothelial growth factors (VEGFs) are the family of extracellular signaling proteins involved in the processes of angiogenesis. VEGFA overexpression and altered regulation of VEGFA signaling pathways lead to pathological angiogenesis, which contributes to the progression of various diseases, such as age-related macular degeneration and cancer. Monoclonal antibodies and decoy receptors have been extensively used in the anti-angiogenic therapies for the neutralization of VEGFA. However, multiple side effects, solubility and aggregation issues, and the involvement of compensatory VEGFA-independent pro-angiogenic mechanisms limit the use of the existing VEGFA inhibitors. Short chemically synthesized VEGFA binding peptides are a promising alternative to these full-length proteins. In this review, we summarize anti-VEGFA peptides identified so far and discuss the molecular basis of their inhibitory activity to highlight their pharmacological potential as anti-angiogenic drugs.

Automated summary

VEGFs play crucial roles in angiogenesis, but dysregulation can lead to pathological angiogenesis in various diseases. Monoclonal antibodies and decoy receptors are commonly used to neutralize VEGFA in anti-angiogenic therapies. Short peptides are promising alternatives to full-length VEGFA inhibitors, overcoming some limitations of existing therapies.