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Mol Imaging Biol. 2011 Feb;13(1):112-20. doi: 10.1007/s11307-010-0302-4.

Specific targeting of human integrin α(v)β (3) with (111)In-labeled Abegrin™ in nude mouse models.

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Medical Isotopes Research Center and Department of Radiation Medicine, School of Basic Medical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China.



The cell adhesion molecule integrin α(v)β(3) is an important player in the process of tumor angiogenesis and metastasis. Abegrin™, a fully humanized anti-integrin α(v)β(3) monoclonal antibody, was currently in clinical trials for cancer therapy. Herein, we labeled Abegrin™ with (111)In, evaluated the in vitro and in vivo characteristics, and investigated whether the expression of integrin α(v)β(3) in tumors could be imaged with (111)In-labeled Abegrin™.


The binding affinity and specificity of Abegrin™ was analyzed using U87MG glioblastoma cells. Abegrin™ was coupled with 1,4,7,10-tetraazadodecane-N,N',N",N'″-tetraacetic acid (DOTA) for (111)In radiolabeling. γ Imaging of (111)In-DOTA-Abegrin™ was carried out in nude mice bearing both integrin α(v)β(3)-positive U87MG and integrin α(v)β(3)-negative HT-29 tumors. Biodistribution and blocking studies of (111)In-DOTA-Abegrin™ were investigated in U87MG tumor-bearing nude mice.


Abegrin™ exhibited high-binding affinity to human integrin α(v)β(3) expressed on U87MG cells (K (d) of 0.35 ± 0.06 nM). The antibody retained antigen-binding affinity/specificity after DOTA conjugation. γ Imaging showed that the tumor uptake of (111)In-DOTA-Abegrin™ in integrin α(v)β(3)-positive U87MG tumors was much higher than that in integrin α(v)β(3)-negative HT-29 tumors. In the HT-29 tumors, Abegrin™ was mainly nonspecifically accumulated around the blood vessels, while in the U87MG tumors, besides the nonspecific tumor retention, Abegrin™ also specifically bound the human integrin α(v)β(3) expressed on the tumor cells. Biodistribution and blocking studies exhibited that the U87MG tumor uptake of (111)In-DOTA-Abegrin™ decreased from 14.12 ± 0.44 to 6.93 ± 0.94 percentage of injected dose per gram of tissue after coinjection of excess dose of cold Abegrin™, which confirmed the in vivo integrin α(v)β(3) binding specificity of (111)In-DOTA-Abegrin™.


Abegrin™ showed specific binding to human integrin α(v)β(3) expressed on the tumor cells. (111)In-DOTA-Abegrin™ can specifically target the human integrin α(v)β(3) expression in the nude mouse model. (111)In-DOTA-Abegrin™ has a potential for clinical translation as an agent for integrin α(v)β(3)-positive tumor imaging, evaluating tumor angiogenic status and monitoring the therapeutic efficacy of Abegrin™-based cancer therapy.

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