Rapid and selective targeting of heterogeneous pancreatic neuroendocrine tumors

Citation:

G. K. Park, J. H. Lee, E. Soriano, M. Choi, K. Bao, W. Katagiri, D. Y. Kim, J. H. Paik, S. H. Yun, J. V. Frangioni, T. E. Clancy, S. Kashiwagi, M. Henary, and H. S. Choi. 2020. “Rapid and selective targeting of heterogeneous pancreatic neuroendocrine tumors.” iScience, 23, Pp. 101006.

Abstract:

Design of tissue-specific contrast agents to delineate tumors from background tissues is a major unmet clinical need for ultimate surgical interventions. Bioconjugation of fluorophore(s) to a ligand has been mainly used to target overexpressed receptors on tumors. However, the size of the final targeted ligand can be large, >20 kDa, and cannot readily cross the microvasculature to meet the specific tissue, resulting in low targetability with a high background. Here, we report a small and hydrophilic phenoxazine with high targetability and retention to pancreatic neuroendocrine tumor. This bioengineered fluorophore permits sensitive detection of ultrasmall (<0.5 mm) ectopic tumors within a few seconds after a single bolus injection, highlighting every tumor in the pancreas from the surrounding healthy tissues with reasonable half-life. The knowledge-based approach and validation used to develop structure-inherent tumor-targeted fluorophores have a tremendous potential to improve treatment outcome by providing definite tumor margins for image-guided surgery.

Notes:

Park, G KateLee, Jeong HeonSoriano, EduardoChoi, MyunghwanBao, KaiKatagiri, WataruKim, Do-YeonPaik, Ji-HyeYun, Seok-HyunFrangioni, John VClancy, Thomas EKashiwagi, SatoshiHenary, MagedChoi, Hak SooengiScience. 2020 Mar 25;23(4):101006. doi: 10.1016/j.isci.2020.101006.