ATN-161 is a novel small peptide inhibitor of integrin α5β1; a beta integrin antagonist with antitumor activity. ATN-161 inhibited VEGF-induced migration and capillary tube formation in hCECs. In vivo, injection of ATN-161 after laser photocoagulation inhibited CNV leakage and neovascularization to an extent similar to AF564. Furthermore, SD-OCT and histologic examinations indicated that ATN-161 significantly decreased the size of laser-induced lesions. Treatment with the α5β1 signaling inhibitor ATN-161 significantly blunts atherosclerotic plaque development in apolipoprotein E-deficient mice, characterized by reduced vascular cell adhesion molecule-1 expression and macrophage accumulation without affecting fibrous cap size.
|Source||Graefes Arch Clin Exp Ophthalmol (2018). Figure 2. ATN-161|
|Method||western blot assay|
|Cell Lines||Tet/opsin/VEGF mice|
|Concentrations||0.1, 1, and 10 μg/μL|
|Incubation Time||24 h|
|Results||The analysis of western blot results revealed that ATN-161 significantly reduced the expression of integrin 5β1 at concentrations of 1 and 10 μg/μL, and this seemed to present a dose-independent manner|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
α5β1 integrin signaling mediates oxidized low-density lipoprotein-induced inflammation and early atherosclerosis.
Yurdagul A Jr, et al. Arterioscler Thromb Vasc Biol. 2014 Jul;34(7):1362-73. PMID: 24833794.
The antiangiogenic effects of integrin alpha5beta1 inhibitor (ATN-161) in vitro and in vivo.
Wang W, et al. Invest Ophthalmol Vis Sci. 2011 Sep 14;52(10):7213-20. PMID: 21813636.
Inhibition of integrin alpha5beta1 function with a small peptide (ATN-161) plus continuous 5-FU infusion reduces colorectal liver metastases and improves survival in mice.
Stoeltzing O, et al. Int J Cancer. 2003 Apr 20;104(4):496-503. PMID: 12584749.
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