GU81

GU81 is a **synthetic peptoid antagonist** targeting vascular endothelial growth factor receptor 2 (VEGFR2), developed as a derivative of the peptoid GU40C4 for enhanced binding affinity and efficacy[1][2]. Peptoids are oligomers similar to peptides but engineered for improved serum stability and cell permeability. GU81 blocks VEGF-induced VEGFR2 phosphorylation, thus inhibiting angiogenesis and endothelial cell proliferation. In animal models of breast cancer, GU81 showed limited efficacy as a single agent, but in combination with doxorubicin, it significantly reduced tumor growth and progression. GU81 reduces total vascular area and vessel size but does not reduce vessel number. As a single agent, it increases VEGF expression and macrophage infiltration in tumors, effects which are abrogated when combined with doxorubicin[1][2]. GU81 is not approved for clinical use and is at the stage of preclinical development.

Brand names

GU81GU-81GU 81

Other names

GU81GU-81GU 81