EG3287

EG3287 (also known as VEFR-Npn-1 or V-1) is a synthetic peptide antagonist of Neuropilin-1 (NRP1) originally developed by Ark Therapeutics. It is based on the heptapeptide sequence ATWLPPR, which was identified for its ability to specifically bind the b1b2 domain of NRP1 and competitively inhibit the binding of the VEGF-A165 isoform. Neuropilin-1 acts as a co-receptor that enhances the affinity of VEGF-A165 for VEGFR2, thereby potentiationg pro-angiogenic signaling. By disrupting this interaction, EG3287 inhibits VEGF-induced endothelial cell proliferation, migration, and vascular permeability. The drug was primarily investigated for the treatment of wet age-related macular degeneration (AMD) via intravitreal injection and was also explored for its potential to inhibit tumor angiogenesis in various cancers. Clinical development reached Phase 1/2 trials, but the program was discontinued following the restructuring of Ark Therapeutics.

Other names

ATWLPPRNeuropilin-1 antagonist peptideNeuropilin1 antagonist peptideNeuropilin 1 antagonist peptide