ATN-161 is an integrin α5β1 binding peptide and antagonist that inhibits VEGF-induced hCECs migration and angiogenesis. ATN-161 also suppresses spike protein interaction with integrin α5β1 and may be employed against SARS-CoV-2 infection.

Compared to the control group and monotherapy, ATN-161 combined with 5-FU significantly inhibited tumor cell proliferation and markedly increased the number of apoptotic (TUNEL-positive) tumor cells. In comparison to the control group, ATN-161 reduced endothelial cell (EC) counts by 21% after 48 hours of incubation [1]. ATN-161 was able to inhibit VEGF-induced migration of Homo sapiens corneal endothelial cells (hCECs) and the formation of capillary-like tubular structures, but showed no inhibitory effect on cell proliferation. Starting from a concentration of 100 nM, ATN-161 reduced VEGF-induced cell migration in a dose-dependent manner[2].

In the α5β1-negative human colon cancer xenograft model (HT29), ATN-161 treatment significantly reduced tumor weight and vascular density [1]. Intravitreal injection of ATN-161 after laser photocoagulation effectively suppressed leakage and neovascularization of choroidal neovascularization (CNV), with efficacy comparable to that of AF564 [2].