Minigastrin

Applications

Peptide Receptor Radionuclide Therapy (PRRT)

A radioactively labeled analogue of minigastrin, PP-F11, conjugated with NOTA, DOTA, or NODAGA, was studied to view the effects they have on peptide receptor radionuclide therapy (PRRT) and cancer cell tracing. When mice with CCK2 tumors were injected with 64Cu-labeled DOTA-PP-F11, NOTA-PP-F11, and NODAGA-PP-F11, the mice labeled with NOTA displayed a tumor uptake of 7.20 ± 0.44% ID/g and a high tumor-to-blood ratio. Further studies are being investigated on how to reduce the background levels to obtain clearer images.

The inhibition of rapamycin complex 1 improves the tumor uptake of radioactively labeled minigastrin. Treatment of A431/CCKBR tumor cells were assessed with DOTA-PP-F11N. This treatment in combination with everolimus in mice, resulted in an average size tumor reduction of about 0.3 cm³ in comparison to the control group which had an average tumor size of 0.97 cm³. The treatment group also had a higher survival rate where the control group median life span was 19.5 days and the group that received treatment had an average life span of 43 days.

References

References

1. (29 June 2006). "Oxford dictionary of biochemistry and molecular biology". Oxford University Press.
2. (6 July 2011). "Preclinical Evaluation of Radiolabeled DOTA-Derivatized Cyclic Minigastrin Analogs for Targeting Cholecystokinin Receptor Expressing Malignancies". Molecular Imaging and Biology.
3. (2014-11-03). "PET and SPECT Imaging of a Radiolabeled Minigastrin Analogue Conjugated with DOTA, NOTA, and NODAGA and Labeled with 64 Cu, 68 Ga, and 111 In". Molecular Pharmaceutics.
4. (2021-12-15). "Therapeutic Response of CCKBR-Positive Tumors to Combinatory Treatment with Everolimus and the Radiolabeled Minigastrin Analogue [177Lu]Lu-PP-F11N". Pharmaceutics.