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Design, Synthesis, and Evaluation of a Neurokinin-1 Receptor-Targeted Near-IR Dye for Fluorescence-Guided Surgery of Neuroendocrine Cancers.

Bioconjug. Chem.. 2016-09; 
KanduluruAnanda Kumar,SrinivasaraoMadduri,LowPhil
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Biochemicals NHS-Rhodamine ester was purchased from Thermo Fisher Scientific Inc., Chicago, Illinois. (Benzotriazol-1-yloxy)tripyrrolidinophosphonium hexafluoro-phosphate (PyBOP) was obtained from Genscript Inc. (Piscataway, New Jersey). Get A Quote

摘要

The neurokinin-1 receptor (NK1R) is implicated in the growth and metastasis of many tumors, including cancers of the brain (e.g., gliomas, glioblastomas, and astrocytomas), skin (e.g., melanomas), and neuroendocrine tissues (cancers of the breast, stomach, pancreas, larynx, and colon). Because overexpression of NK1R has been reported in most of these malignancies, we have undertaken designing an NK1R-targeted near-infrared (NIR) fluorescent dye for fluorescence-guided surgeries of these cancers. We demonstrate here that an NK1R-binding ligand linked to the NIR dye LS288 selectively accumulates in NK1R-expressing tumor xenografts with high affinity (Kd = 13 nM), allowing intraoperative ... More

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