timtraxanib   Click here for help

GtoPdb Ligand ID: 11673

Synonyms: AVI-3207 | AVI3207 | N2-acetyl-L-arginyl-L-leucyl-L-tyrosyl-L-glutamic acid
Comment: Timtraxanib (AVI-3207) is an angiogenesis inhibitor [2]. Structurally it is modified tetrapeptide that acts as a selective VEGF receptor-2 (VEGFR-2) inhibitor [1,3-4]. The N terminal acylation improves the peptide's stability against serum peptidase degradation [5]. Functionally, timtraxanib blocks VEGFR-2-mediated neovascularization, whilst sparing the function of VEGFR-1. Intravitreal administration of timtraxanib reduces neovascularization in animal models of age-related macular degeneration.
Bioactivity Comments
This peptide inhibits vascular endothelial growth factor (VEGF)-induced endothelial cell proliferation, migration and tube formation in vitro (IC50 0.04-0.08 nM) [2,5].