Novel positron emission tomography imaging targeting cell surface glycans for pancreatic cancer: 18 F ‐labeled rBC2LCN lectin

Advancement in early detection modalities will greatly improve the overall prognoses of pancreatic ductal adenocarcinoma (PDAC). For this purpose, we report a novel class of tumor‐specific probes for positron emission tomography (PET) based on targeting cell surface glycans. The PDAC‐targeting abili...

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Bibliographic Details
Published in:Cancer science Vol. 114; no. 8; pp. 3364 - 3373
Main Authors: Kuroda, Yukihito, Oda, Tatsuya, Shimomura, Osamu, Louphrasitthiphol, Pakavarin, Mathis, Bryan J., Tateno, Hiroaki, Hatano, Kentaro
Format: Journal Article
Language:English
Published: England 01.08.2023
Subjects:
Animals
Carcinoma, Pancreatic Ductal
Cell Line, Tumor
Humans
Mice
Mice, Nude
Pancreatic Neoplasms
Pancreatic Neoplasms - diagnostic imaging
Positron-Emission Tomography - methods
Radiopharmaceuticals
fluorine-18
pancreatic cancer
molecular imaging
lectin
PET
ISSN:1347-9032, 1349-7006, 1349-7006
Online Access:Get full text
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Summary:Advancement in early detection modalities will greatly improve the overall prognoses of pancreatic ductal adenocarcinoma (PDAC). For this purpose, we report a novel class of tumor‐specific probes for positron emission tomography (PET) based on targeting cell surface glycans. The PDAC‐targeting ability of rBC2LCN lectin, combined with fluorine‐18 ( 18 F) ([ 18 F]FB‐rBC2LCN), resulted in reproducible, high‐contrast PET imaging of tumors in a PDAC xenograft mouse model. [ 18 F] N ‐succinimidyl‐4‐fluorobenzoate ([ 18 F]SFB) was conjugated to rBC2LCN, and [ 18 F]FB‐rBC2LCN was successfully prepared with a radiochemical purity >95%. Cell binding and uptake revealed that [ 18 F]FB‐rBC2LCN binds to H‐type‐3‐positive Capan‐1 pancreatic cancer cells. As early as 60 min after [ 18 F]FB‐rBC2LCN (0.34 ± 0.15 MBq) injection into the tail vein of nude mice subcutaneously bearing Capan‐1 tumors, tumor uptake was high (6.6 ± 1.8 %ID/g), and the uptake increased over time (8.8 ± 1.9 %ID/g and 11 ± 3.2 %ID/g at 150 and 240 min after injection, respectively). Tumor‐to‐muscle ratios increased over time, up to 19 ± 1.8 at 360 min. High‐contrast PET imaging of tumors relative to background muscle was also achieved as early as 60 min after injection of [ 18 F]FB‐rBC2LCN (0.66 ± 0.12 MBq) and continued to increase up to 240 min. Our 18 F‐labeled rBC2LCN lectin warrants further clinical development to improve the accuracy and sensitivity of early‐stage pancreatic cancer detection.
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ISSN:1347-9032
1349-7006
1349-7006
DOI:10.1111/cas.15846