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by | Mar 21, 2018 | Azalea

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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]

References

  1. ^ Oxford dictionary of biochemistry and molecular biology (Rev. ed.). Oxford University Press. 29 June 2006. ISBN 9780198529170.
  2. ^ von Guggenberg, Elisabeth; Rangger, Christine; Sosabowski, Jane; Laverman, Peter; Reubi, Jean-Claude; Virgolini, Irene Johanna; Decristoforo, Clemens (6 July 2011). "Preclinical Evaluation of Radiolabeled DOTA-Derivatized Cyclic Minigastrin Analogs for Targeting Cholecystokinin Receptor Expressing Malignancies". Molecular Imaging and Biology. 14 (3): 366–375. doi:10.1007/s11307-011-0506-2. PMID 21732165. S2CID 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. 11 (11): 3930–3937. doi:10.1021/mp500283k. ISSN 1543-8384. PMID 24992368.
  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. 11 (11): 3930–3937. doi:10.1021/mp500283k. ISSN 1543-8384. PMID 24992368.
  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. 13 (12): 2156. doi:10.3390/pharmaceutics13122156. ISSN 1999-4923. PMC 8708304. PMID 34959437.
  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. 13 (12): 2156. doi:10.3390/pharmaceutics13122156. ISSN 1999-4923. PMC 8708304. PMID 34959437.
  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. 13 (12): 2156. doi:10.3390/pharmaceutics13122156. ISSN 1999-4923. PMC 8708304. PMID 34959437.


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