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Preliminary evaluation of GLP-1R PET in the diagnosis and risk stratification of pheochromocytomas

In: NEOPLASMA, vol. 67, no. 1
M Li - Y Liu - Y Xu - Y Li - D Pan - L Wang - J Yan - X Wang - R Yang - M Yang
Detaily:
Rok, strany: 2020, 27 - 36
O článku:
Noninvasive imaging methods for the diagnosis and risk stratification of pheochromocytomas (PHEOs) remain a great clinical challenge. The glucagon-like peptide-1 receptor (GLP-1R) has been validated to be overexpressed in PHEOs and therefore may be a reliable target for PHEOs. In this study, we firstly synthesized a novel radiotracer 68Ga-NOTA-MAL-Cys39-exendin-4 that specifically targets GLP-1R and evaluated the performance of GLP-1R PET for the diagnosis and risk stratification of PHEOs. Cys39-exendin-4 was conjugated to NOTA-MAL and then radiolabeled with 68Ga. The reaction was completed within 20 min with a yield of 91.6 ± 2.8%. In vitro cell uptake studies validated its high specificity. PET images showed promising tumor visualization with high uptake (1.88 ± 0.10 %ID/g for PC-12 poorly differentiated tumors and 1.09 ± 0.003 %ID/g for PC-12 highly differentiated tumors at 30min after injection). There was a significant difference in the uptake of 68Ga-NOTA-MAL-Cys39-exendin-4 between PC-12 poorly and highly differentiated tumors (p < 0.001), but no significant difference could be observed by 18F-FDG PET. Biodistribution results confirmed the findings of GLP-1R PET and demonstrated that 131I-MIBG couldn’t be used for the risk stratification of PHEOs. Immunohistochemistry (IHC) staining revealed differences in GLP-1R expression between PC-12 poorly and highly differentiated tumor tissues. These results demonstrated that 68Ga-NOTA-MAL-Cys39-exendin-4 can specifically target GLP-1R with favorable pharmacokinetic properties. GLP-1R PET can be used for PHEOs detection and has potential for the risk stratification of PHEOs.
Ako citovať:
ISO 690:
Li, M., Liu, Y., Xu, Y., Li, Y., Pan, D., Wang, L., Yan, J., Wang, X., Yang, R., Yang, M. 2020. Preliminary evaluation of GLP-1R PET in the diagnosis and risk stratification of pheochromocytomas. In NEOPLASMA, vol. 67, no.1, pp. 27-36. 0028-2685.

APA:
Li, M., Liu, Y., Xu, Y., Li, Y., Pan, D., Wang, L., Yan, J., Wang, X., Yang, R., Yang, M. (2020). Preliminary evaluation of GLP-1R PET in the diagnosis and risk stratification of pheochromocytomas. NEOPLASMA, 67(1), 27-36. 0028-2685.
O vydaní:
Vydavateľ: AEPress, Ltd.