Minigastrin Explained

Minigastrin (also mini gastrin) is a form of gastrin. Its sequence is H-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2.^[1]

Minigastrin is a potential therapeutic agent for thyroid carcinoma by targeting cancer-promoting cholecystokinin receptors.^[2]

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.^[3] 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.^[4] 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.^[5] This treatment in combination with RAD001 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.^[6] 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.^[7]

Notes and References

1. Book: Oxford dictionary of biochemistry and molecular biology . 29 June 2006 . Oxford University Press . 9780198529170 . Rev..
2. von Guggenberg . Elisabeth . Rangger . Christine . Sosabowski . Jane . Laverman . Peter . Reubi . Jean-Claude . Virgolini . Irene Johanna . Decristoforo . Clemens . Preclinical Evaluation of Radiolabeled DOTA-Derivatized Cyclic Minigastrin Analogs for Targeting Cholecystokinin Receptor Expressing Malignancies . Molecular Imaging and Biology . 6 July 2011 . 14 . 3 . 366–375 . 10.1007/s11307-011-0506-2. 21732165 . 20362994 .
3. Roosenburg . S. . Laverman . P. . Joosten . L. . Cooper . M. S. . Kolenc-Peitl . P. K. . Foster . J. M. . Hudson . C. . Leyton . J. . Burnet . J. . Oyen . W. J. G. . Blower . P. J. . 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 . en . 11 . 11 . 3930–3937 . 10.1021/mp500283k . 24992368 . 1543-8384.
4. Roosenburg . S. . Laverman . P. . Joosten . L. . Cooper . M. S. . Kolenc-Peitl . P. K. . Foster . J. M. . Hudson . C. . Leyton . J. . Burnet . J. . Oyen . W. J. G. . Blower . P. J. . 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 . en . 11 . 11 . 3930–3937 . 10.1021/mp500283k . 24992368 . 1543-8384.
5. Grzmil . Michal . Imobersteg . Stefan . Blanc . Alain . Frank . Stephan . Schibli . Roger . Béhé . Martin P. . 2021-12-15 . Therapeutic Response of CCKBR-Positive Tumors to Combinatory Treatment with Everolimus and the Radiolabeled Minigastrin Analogue [177Lu]Lu-PP-F11N . Pharmaceutics . en . 13 . 12 . 2156 . 10.3390/pharmaceutics13122156 . 1999-4923 . 8708304 . 34959437. free .
6. Grzmil . Michal . Imobersteg . Stefan . Blanc . Alain . Frank . Stephan . Schibli . Roger . Béhé . Martin P. . 2021-12-15 . Therapeutic Response of CCKBR-Positive Tumors to Combinatory Treatment with Everolimus and the Radiolabeled Minigastrin Analogue [177Lu]Lu-PP-F11N . Pharmaceutics . en . 13 . 12 . 2156 . 10.3390/pharmaceutics13122156 . 1999-4923 . 8708304 . 34959437. free .
7. Grzmil . Michal . Imobersteg . Stefan . Blanc . Alain . Frank . Stephan . Schibli . Roger . Béhé . Martin P. . 2021-12-15 . Therapeutic Response of CCKBR-Positive Tumors to Combinatory Treatment with Everolimus and the Radiolabeled Minigastrin Analogue [177Lu]Lu-PP-F11N . Pharmaceutics . en . 13 . 12 . 2156 . 10.3390/pharmaceutics13122156 . 1999-4923 . 8708304 . 34959437. free .