Preclinical evaluation of gastrin derivatives labelled with 111in: Radiolabelling, affinity profile and pharmacokinetics in rats

Biomedical Papers

Volumn 158, Issue 4, 2014, Pages 544-551

  Melicharova, Ludmila ^a   Laznickova, Alice ^a   Laznicek, Milan ^a  

^a CHARLES UNIVERSITY   (Czech Republic)

Author keywords

Cholecystokinin receptors; Indium 111; Minigastrins; Peptides; Preclinical evaluation; Radiolabelling; Receptor targeting

Indexed keywords

RATTUS;

CHOLECYSTOKININ B RECEPTOR; COORDINATION COMPOUND; GASTRIN; INDIUM-111-1,4,7,10-TETRAAZACYCLODODECANE-1,4,7,10-TETRAACETIC ACID; MINIGASTRIN; PEPTIDE; RADIOPHARMACEUTICAL AGENT; SINGLE HETEROCYCLIC RINGS;

ANIMAL; MALE; METABOLISM; RAT; TISSUE DISTRIBUTION; TUMOR CELL LINE;

ANIMALS; CELL LINE, TUMOR; COORDINATION COMPLEXES; GASTRINS; HETEROCYCLIC COMPOUNDS, 1-RING; MALE; PEPTIDES; RADIOPHARMACEUTICALS; RATS; RECEPTOR, CHOLECYSTOKININ B; TISSUE DISTRIBUTION;

EID: 84916225874     PISSN: 12138118     EISSN: 18047521     Source Type: Journal    
DOI: 10.5507/bp.2013.064     Document Type: Article

References (15)

1. Nanda PK, Lane SR, Retzloff LB, Pandey US, Smith CJ. Radiolabeled regulatory peptides for imaging and therapy. Curr Opin Endocrinol Diabetes Obes 2010;17:69-76.
2. Fani M, Maecke HR, Okarvi S. Radiolabeled peptides: Valuable tools for the detection and treatment of cancer. Theranostics 2012;2:481-501.
3. Reubi JC, Schaer JC, Waser B. Cholecystokinin (CCK)-A and CCK-B/ gastrin receptors in human tumors. Cancer Res 1997;57:1377-86.
4. Tornesello AL, Aurilio M, Accardo A, Tarallo L, Barbieri A, Arra C, Tesauro D, Morell G, Aloj L. Gastrin and cholecystokinin peptidebased radiopharmaceuticals: an in vivo and in vitro comparison. J Pept Sci 2011;17:405-12.
5. Von Guggenberg E, Rangger C, Sosabowski J, Laverman P, Reubi JC, Virgolini IJ, Decristoforo R. Preclinical Evaluation of Radiolabeled DOTA-Derivatized Cyclic Minigastrin Analogs for Targeting Cholecystokinin Receptor Expressing Malignancies. Mol Imag Biol 2012;14:366–75.
6. Aloj L, Aurilio M, Rinaldi V, Dámbrosio L, Tesauro D, Kolenc Peitl P, Maina T, Mansi R, von Guggenberg E, Joosten L, Sosabowski JK, Breeman WAP, De Blois E, Koelewijn S, Melis M, Waser B, Beetschen K, Reubi JC, de Jong M. Comparison of the binding and internalization properties of 12 DOTA- coupled and 111In- labelled CCK2/ gastrin receptor binding peptides: a collaborative project under COST Action BM0607 Eur J Nucl Med Mol Imaging 2011;38:1417-25.
7. Behr TM, Jenner N, Behe M, Angerstein C, Gratz S, Raue F, Becker W. Radiolabeled Peptides for Targeting Cholecystokinin-B/ Gastrin Receptor-Expressing Tumors. J Nucl Med 1999;40:1029-44.
8. Behr TM, Behe MP. Cholecystokinin-B/Gastrin Receptor-Targeting Peptides for Staging and Therapy of Medullary Thyroid Cancer and Other Cholecystokinin-B Receptor-Expressing Malignancies. Semin Nucl Med 2002;32:97-109.
9. Melis M, Krenning EP, Bernard BF, de Visser M, Rolleman E, de Jong M. Renal uptake and retention of radiolabeled somatostatin; bombesin; neurotensin; minigastrin and CCK analogs: species and gender differences. Nucl Med Biol 2007;34:633-41.
10. Laverman P, Joosten L, Eek A, Rosenburg S, Kolenc Peitl P, Maina T, Macke H, Aloj L, von Guggenberg E, Sosabowski JK, de Jong M, Reubi JC, Oyen WJG, Boerman OC. Comparative biodistribution of 12 111In-labelled gastrin/CCK2 receptor-targeting peptides. Eur J Nucl Med Mol Imaging 2011;38:1410-6.
11. Ocak M, Helbok A, Rangger C, Peitl PK, Nock BA, Morelli G, Eek A, Sosabowski JK, Breeman WAP, Reubi JC, Decristoforo C. Comparison of biological stability and metabolism of CCK2 receptor targeting peptides, a collaborative project under COST BM0607. Eur J Nucl Med Mol Imaging 2011;38:1426–36.
12. Kulaksiz H, Arnold R, Goke B, Maronde E, Meyer M, Fahrenholz F, Forssmann W-G, Eissele R. Expression and cell-specific localization of the cholecystokinin B/gastrin receptor in the human stomach. Cell Tissue Res 2000:289-98.
13. Vegt E, de Jong M, Wetzels JFM, Masereeuw R, Melis M, Oyen WJG, Gotthardt M, Boerman OC. Renal toxicity of radiolabeled peptides and antibody fragments: mechanisms, impact on radionuclide therapy, and strategies for prevention. J Nucl Med 2010;51:1049-58.
14. Behe M, Kluge G, Becker W, Gotthardt M, Behr TM. Use of polyglutamic acids to reduce uptake of radiometal-labeled minigastrin in the kidneys. J Nucl Med 2005;46:1012-15.
15. Schrenck T, Weerth A, Bechtel S, Eschenhagen T, Weil J, Wolf G, Schulz M, Greten H. Evidence for CCKB receptors in the guinea-pig kidney: localization and characterization by 125I gastrin binding studies and by RT-PCR. Naunyn-Schmiedebergs Arch Pharmacol 1998:287-92.