Development and evaluation of 18F-TTCO-Cys40-exendin- 4: A PET probe for imaging transplanted islets

Journal of Nuclear Medicine

Volumn 54, Issue 2, 2013, Pages 244-251

  Wu, Zhanhong ^a   Liu, Shuanglong ^b   Hassink, Matthew ^c   Nair, Indu ^a   Park, Ryan ^b   Li, Lin ^a   Todorov, Ivan ^a   Fox, Joseph M ^c   Li, Zibo ^b,e   Shively, John E ^a   Conti, Peter S ^b   Kandeel, Fouad ^a,d  

^a CITY OF HOPE NATIONAL MEDICAL CENTER   (United States)

^b UNIVERSITY OF SOUTHERN CALIFORNIA   (United States)

^c UNIVERSITY OF DELAWARE   (United States)

^d City of Hope ^*  (United States)

^e UNIVERSITY OF SOUTHERN CALIFORNIA   (United States)

Author keywords

18F labeled exendin 4; GLP 1R; Islet imaging

Indexed keywords

FLUORINE TETRAZINE CYCLOOCTENE CYSTEINE EXENDIN 4 F 18; GLUCAGON LIKE PEPTIDE 1 RECEPTOR; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG; CYCLOOCTANE DERIVATIVE; DIAGNOSTIC AGENT; EXENDIN 4; FLUORINE; GLUCAGON RECEPTOR; GLUCAGON-LIKE PEPTIDE-1 RECEPTOR; PEPTIDE; VENOM;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BINDING AFFINITY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; HUMAN; HUMAN TISSUE; IMMUNOHISTOCHEMISTRY; IN VITRO STUDY; IN VIVO STUDY; ISOTOPE LABELING; MALE; MOLECULAR IMAGING; MOUSE; NON INVASIVE PROCEDURE; NONHUMAN; PANCREAS ISLET TRANSPLANTATION; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PROCESS DEVELOPMENT; PROTEIN TARGETING; RADIATION EXPOSURE; RADIOCHEMISTRY; RADIOISOTOPE DISTRIBUTION; RAT; ANIMAL; BINDING COMPETITION; CYTOLOGY; DIAGNOSTIC IMAGING; GENE EXPRESSION REGULATION; INSULINOMA; LIVER; METABOLISM; METHODOLOGY; MOUSE MUTANT; NONOBESE DIABETIC MOUSE; NUCLEAR MEDICINE; PANCREAS ISLET BETA CELL;

ANIMALS; BINDING, COMPETITIVE; CYCLOOCTANES; DIAGNOSTIC IMAGING; FLUORINE RADIOISOTOPES; GENE EXPRESSION REGULATION; HUMANS; INSULIN-SECRETING CELLS; INSULINOMA; ISLETS OF LANGERHANS TRANSPLANTATION; LIVER; MALE; MICE; MICE, INBRED NOD; MICE, SCID; NUCLEAR MEDICINE; PEPTIDES; POSITRON-EMISSION TOMOGRAPHY; RATS; RECEPTORS, GLUCAGON; VENOMS;

MLCS; MLOWN;

EID: 84873551370     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: 10.2967/jnumed.112.109694     Document Type: Article

References (32)

1. van Belle TL, Coppieters KT, von Herrath MG. Type 1 diabetes: etiology, immunology, and therapeutic strategies. Physiol Rev. 2011;91:79-118.
2. Langer RM. Islet transplantation: lessons learned since the Edmonton breakthrough. Transplant Proc. 2010;42:1421-1424.
3. Shapiro AM, Hao EG, Lakey JR, et al. Novel approaches toward early diagnosis of islet allograft rejection. Transplantation. 2001;71:1709-1718.
4. Shapiro AM, Lakey JR, Ryan EA, et al. Islet transplantation in seven patients with type 1 diabetes mellitus using a glucocorticoid-free immunosuppressive regimen. N Engl J Med. 2000;343:230-238.
5. Holst JJ. The physiology of glucagon-like peptide 1. Physiol Rev. 2007;87:1409-1439.
6. Baggio LL, Drucker DJ. Biology of incretins: GLP-1 and GIP. Gastroenterology. 2007;132:2131-2157.
7. Körner M, Stockli M, Waser B, Reubi JC. GLP-1 receptor expression in human tumors and human normal tissues: potential for in vivo targeting. J Nucl Med. 2007;48:736-743.
8. Moens K, Heimberg H, Flamez D, et al. Expression and functional activity of glucagon, glucagon-like peptide I, and glucose-dependent insulinotropic peptide receptors in rat pancreatic islet cells. Diabetes. 1996;45:257-261.
9. Tornehave D, Kristensen P, Romer J, Knudsen LB, Heller RS. Expression of the GLP-1 receptor in mouse, rat, and human pancreas. J Histochem Cytochem. 2008; 56:841-851.
10. Eng J, Kleinman WA, Singh L, Singh G, Raufman JP. Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom: further evidence for an exendin receptor on dispersed acini from guinea pig pancreas. J Biol Chem. 1992;267:7402-7405.
11. Edwards CM, Stanley SA, Davis R, et al. Exendin-4 reduces fasting and postprandial glucose and decreases energy intake in healthy volunteers. Am J Physiol Endocrinol Metab. 2001;281:E155-E161.
12. Malhotra R, Singh L, Eng J, Raufman JP. Exendin-4, a new peptide from Heloderma suspectum venom, potentiates cholecystokinin-induced amylase release from rat pancreatic acini. Regul Pept. 1992;41:149-156.
13. Göke R, Fehmann HC, Linn T, et al. Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)- amide receptor of insulin-secreting beta-cells. J Biol Chem. 1993;268:19650-19655.
14. 64Cu-DO3A-VS-Cys40-exendin-4 by targeting GLP-1 receptor. Bioconjug Chem. 2011;22:1587-1594.
15. Connolly BM, Vanko A, McQuade P, et al. Ex vivo imaging of pancreatic beta cells using a radiolabeled GLP-1 receptor agonist. Mol Imaging Biol. 2012;14:79-87.
16. Pattou F, Kerr-Conte J, Wild D. GLP-1-receptor scanning for imaging of human beta cells transplanted in muscle. N Engl J Med. 2010;363:1289-1290.
17. 18F-FBEM- EM3106B, a new GLP-1 analogue. Mol Pharm. 2011;8:1775-1782.
18. 18F-radiolabeled analogs of exendin-4 for PET imaging of GLP-1 in insulinoma. Eur J Nucl Med Mol Imaging. 2012;39:463-473.
19. 18F]exendin (9-39) as a potential biomarker to measure pancreatic beta-cell mass. Nucl Med Biol. 2012;39:167-176.
20. 18F labeled probes. Chem Commun (Camb). 2010;46:8043-8045.
21. 18F labeling of cysteine containing peptides and proteins. Mol Imaging. In press.
22. Ricordi C, Lacy PE, Scharp DW. Automated islet isolation from human pancreas. Diabetes. 1989;38(suppl 1):140-142.
23. Blackman ML, Royzen M, Fox JM. Tetrazine ligation: fast bioconjugation based on inverse-electron-demand Diels-Alder reactivity. J Am Chem Soc. 2008;130:13518-13519.
24. Gallwitz B, Witt M, Folsch UR, Creutzfeldt W, Schmidt WE. Binding specificity and signal transduction of receptors for glucagon-like peptide-1(7-36)amide and gastric inhibitory polypeptide on RINm5F insulinoma cells. J Mol Endocrinol. 1993;10:259-268.
25. Todorov I, Nair I, Avakian-Mansoorian A, et al. Quantitative assessment of betacell apoptosis and cell composition of isolated, undisrupted human islets by laser scanning cytometry. Transplantation. 2010;90:836-842.
26. Zhang C, Todorov I, Lin CL, et al. Elimination of insulitis and augmentation of islet beta cell regeneration via induction of chimerism in overtly diabetic NOD mice. Proc Natl Acad Sci U S A. 2007;104:2337-2342.
27. Montaña E, Bonner-Weir S, Weir GC. Beta cell mass and growth after syngeneic islet cell transplantation in normal and streptozocin diabetic C57BL/6 mice. J Clin Invest. 1993;91:780-787.
28. Behnam Azad B, Rota VA, Breadner D, Dhanvantari S, Luyt LG. Design, synthesis and in vitro characterization of glucagon-like peptide-1 derivatives for pancreatic beta cell imaging by SPECT. Bioorg Med Chem. 2010;18:1265-1272.
29. 68Ga- labelled exendin-3, a new agent for the detection of insulinomas with PET. Eur J Nucl Med Mol Imaging. 2010;37:1345-1355.
30. Wild D, Wicki A, Mansi R, et al. Exendin-4-based radiopharmaceuticals for glucagonlike peptide-1 receptor PET/CT and SPECT/CT. J Nucle Md. 2010;51:1059-1067.
31. 2]exendin-4, a very promising ligand for glucagon-like peptide-1 (GLP-1) receptor targeting. J Nucl Med. 2006;47:2025-2033.
32. Li L, Olafsen T, Anderson AL, et al. Reduction of kidney uptake in radiometal labeled peptide linkers conjugated to recombinant antibody fragments: site-specific conjugation of DOTA-peptides to a Cys-diabody. Bioconjug Chem. 2002;13:985-995.