Wikipedia

Minigastrin

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
Identifiers
3D model (JSmol)
ChemSpider
UNII
  • InChI=1S/C74H99N15O26S/c1-37(2)30-44(75)65(106)81-47(19-24-58(94)95)68(109)83-49(21-26-60(98)99)70(111)85-50(22-27-61(100)101)71(112)84-48(20-25-59(96)97)69(110)82-46(18-23-57(92)93)67(108)79-38(3)64(105)88-53(32-40-14-16-42(90)17-15-40)66(107)78-36-56(91)80-54(33-41-35-77-45-13-9-8-12-43(41)45)73(114)86-51(28-29-116-4)72(113)89-55(34-62(102)103)74(115)87-52(63(76)104)31-39-10-6-5-7-11-39/h5-17,35,37-38,44,46-55,77,90H,18-34,36,75H2,1-4H3,(H2,76,104)(H,78,107)(H,79,108)(H,80,91)(H,81,106)(H,82,110)(H,83,109)(H,84,112)(H,85,111)(H,86,114)(H,87,115)(H,88,105)(H,89,113)(H,92,93)(H,94,95)(H,96,97)(H,98,99)(H,100,101)(H,102,103)/t38-,44-,46-,47-,48-,49-,50-,51-,52-,53-,54-,55-/m0/s1 ☒N
    Key: HRSUIUNCTPSRLR-SOLHVGTRSA-N ☒N
  • C[C@@H](C(=O)N[C@@H](Cc1ccc(cc1)O)C(=O)NCC(=O)N[C@@H](Cc2c[nH]c3c2cccc3)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc4ccccc4)C(=O)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)N
Properties
C70H91N15O26
Molar mass 1558.56 g/mol
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Minigastrin is a potential therapeutic agent for thyroid carcinoma by targeting cancer-promoting cholecystokinin receptors.[2]

Applications

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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

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  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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