Therapeutic Peptides Targeting VEGF/VEGFR: Advances in Anti Angiogenic Therapy and the Role of Bioinformatics in Drug Design

Angiogenesis is a critical process in the formation of new blood vessels in both normal and pathological tissues. In cancer, angiogenesis is important to provide oxygen and nutrients to tumour sites due to oxygen deficiency during hypoxia. Vascular endothelial growth factor (VEGF) is a key regulator that activates various signalling pathways that are critical for angiogenesis by binding to the VEGF receptor (VEGFR). Targeting the VEGF/VEGFR signalling pathway, its receptor, or ligand can inhibit signalling and cause an anti-angiogenic effect. Various approaches have been developed to target the VEGF/VEGFR signalling pathway, including the most widely used monoclonal antibodies and tyrosine kinase inhibitors. Monoclonal antibodies show high target specificity, but due to their large size, they also cause high immunogenicity. Tyrosine kinase inhibitors are effective against intracellular targets but have limited capacity to target specific sites. Therapeutic peptides offer a promising alternative because of their small size, improved target selectivity, and chemical modification potential. The use of bioinformatics tools in therapeutic peptide development is time-efficient and provides a better understanding of peptide structure and activity. Bioinformatics tools help in designing therapeutic peptides, including structural and functional analysis, interaction analysis, structural prediction, and modification method testing. In this context, several anti-angiogenic peptides have been designed and developed with the help of bioinformatics tools. Here, we review the importance of the VEGF/VEGFR complex as a target for the development of anti-angiogenic drugs. We also discuss previous studies that successfully used bioinformatics techniques to design and develop effective anti-angiogenic peptides.