In vivo responses of human A375M melanoma to a σ ligand: 18F-FDG PET imaging

Journal of Nuclear Medicine

Volumn 54, Issue 9, 2013, Pages 1613-1620

  Rybczynska, Anna A ^a   De Bruyn, Marco ^a   Ramakrishnan, Nisha K ^a   De Jong, Johan R ^a   Elsinga, Philip H ^a   Helfrich, Wijnand ^a   Dierckx, Rudi A J O ^a,b   Van Waarde, Aren ^a  

^a UNIVERSITY MEDICAL CENTER GRONINGEN   (Netherlands)

^b GHENT UNIVERSITY HOSPITAL   (Belgium)

Author keywords

Antitumor effect; FDG PET; Melanoma; Receptors; Rimcazole;

Indexed keywords

FLUORODEOXYGLUCOSE F 18; LIGAND; RIMCAZOLE; ANTINEOPLASTIC AGENT; CARBAZOLE DERIVATIVE; DIAGNOSTIC AGENT; RADIOPHARMACEUTICAL AGENT; SIGMA OPIATE RECEPTOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CELL DEATH; CONTROLLED STUDY; DIAGNOSTIC IMAGING; DIARRHEA; DRUG TOXICITY; IN VITRO STUDY; IN VIVO STUDY; LIVER; MELANOMA; MOUSE; NONHUMAN; NUDE MOUSE; PANCREAS; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; TUMOR GROWTH; TUMOR XENOGRAFT; Σ RECEPTORS; ANIMAL; ANTIBODY SPECIFICITY; ANTITUMOR EFFECT; DRUG EFFECT; FDG PET; HUMAN; METABOLIC CLEARANCE RATE; METABOLISM; METHODOLOGY; REPRODUCIBILITY; SCINTISCANNING; SENSITIVITY AND SPECIFICITY; TISSUE DISTRIBUTION; TREATMENT OUTCOME; TUMOR CELL LINE;

Σ RECEPTORS; ANTITUMOR EFFECT; FDG PET; MELANOMA; RIMCAZOLE;

ANIMALS; ANTINEOPLASTIC AGENTS; CARBAZOLES; CELL LINE, TUMOR; FLUORODEOXYGLUCOSE F18; HUMANS; MELANOMA; METABOLIC CLEARANCE RATE; MICE; MICE, NUDE; ORGAN SPECIFICITY; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; RECEPTORS, SIGMA; REPRODUCIBILITY OF RESULTS; SENSITIVITY AND SPECIFICITY; TISSUE DISTRIBUTION; TREATMENT OUTCOME;

EID: 84887375187     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: 10.2967/jnumed.113.122655     Document Type: Article

References (39)

1. Miller AJ, Mihm MC. Melanoma. N Engl J Med. 2006;355:51-65.
2. Waterhouse RN, Collier TL. In vivo evaluation of [18F]1-(3-fluoropropyl)- 4-(4- cyanophenoxymethyl)piperidine: a selective sigma-1 receptor radioligand for PET. Nucl Med Biol. 1997;24:127-134.
3. Michelot JM, Moreau MF, Labarre PG, et al. Synthesis and evaluation of new iodine-125 radiopharmaceuticals as potential tracers for malignant melanoma. J Nucl Med. 1991;32:1573-1580.
4. John CS, Bowen WD, Saga T, et al. A malignant melanoma imaging agent: synthesis, characterization, in vitro binding and biodistribution of iodine-125- (2-piperidinylaminoethyl)4-iodobenzamide. J Nucl Med. 1993;34:2169-2175.
5. Hirata M, Mori T, Umeda T, Abe T, Yamamoto T, Ohmomo Y. Evaluation of radioiodinated 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(2-iodophenylpropyl)piperazine as a tumor diagnostic agent with functional sigma receptor imaging by single photon emission computed tomography. Biol Pharm Bull. 2008;31:879-883.
6. Hayashi T, Su T-P. Sigma-1 receptor chaperones at the ER-mitochondrion interface regulate Ca(21) signaling and cell survival. Cell. 2007;131:596-610.
7. Zeng C, Vangveravong S, Xu J, et al. Subcellular localization of sigma-2 receptors in breast cancer cells using two-photon and confocal microscopy. Cancer Res. 2007;67:6708-6716.
8. Hellewell SB, Bowen WD. A sigma-like binding site in rat pheochromocytoma (PC12) cells: decreased affinity for (1)-benzomorphans and lower molecular weight suggest a different sigma receptor form from that of guinea pig brain. Brain Res. 1990;527:244-253.
9. Quirion R, Bowen WD, Itzhak Y, et al. A proposal for the classification of sigma binding sites. Trends Pharmacol Sci. 1992;13:85-86.
10. Xu J, Zeng C, Chu W, et al. Identification of the PGRMC1 protein complex as the putative sigma-2 receptor binding site. Nat Commun. 2011;2:380.
11. Rybczynska AA, Elsinga PH, Sijbesma JW, et al. Steroid hormones affect binding of the sigma ligand 11C-SA4503 in tumour cells and tumour-bearing rats. Eur J Nucl Med Mol Imaging. 2009;36:1167-1175.
12. Zamora PO, Moody TW, John CS. Increased binding to sigma sites of N-[19(2- piperidinyl)ethyl)-4-[I-125]-iodobenzamide (I-125-PAB) with onset of tumor cell proliferation. Life Sci. 1998;63:1611-1618.
13. Mach RH, Smith CR, Al-Nabulsi I, Whirrett BR, Childers SR, Wheeler KT. Sigma 2 receptors as potential biomarkers of proliferation in breast cancer. Cancer Res. 1997;57:156-161.
14. Roperto S, Colabufo NA, Inglese C, et al. Sigma-2 receptor expression in bovine papillomavirus-associated urinary bladder tumours. J Comp Pathol. 2010;142: 19-26.
15. Spruce BA, Campbell LA, McTavish N, et al. Small molecule antagonists of the sigma-1 receptor cause selective release of the death program in tumor and selfreliant cells and inhibit tumor growth in vitro and in vivo. Cancer Res. 2004; 64:4875-4886.
16. van Waarde A, Rybczynska AA, Ramakrishnan N, Ishiwata K, Elsinga PH, Dierckx RAJO. Sigma receptors in oncology: therapeutic and diagnostic applications of sigma ligands. Curr Pharm Des. 2010;16:3519-3537.
17. Crawford KW, Bowen WD. Sigma-2 receptor agonists activate a novel apoptotic pathway and potentiate antineoplastic drugs in breast tumor cell lines. Cancer Res. 2002;62:313-322.
18. Nordenberg J, Perlmutter I, Lavie G, et al. Anti-proliferative activity of haloperidol in B16 mouse and human SK-MEL-28 melanoma cell lines. Int J Oncol. 2005;27:1097-1103.
19. Azzariti A, Colabufo NA, Berardi F, et al. Cyclohexylpiperazine derivative PB28, a sigma2 agonist and sigma1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer. Mol Cancer Ther. 2006;5:1807-1816.
20. Brent PJ, Pang G, Little G, Dosen PJ, Van Helden DF. The sigma receptor ligand, reduced haloperidol, induces apoptosis and increases intracellular-free calcium levels [Ca21]i in colon and mammary adenocarcinoma cells. Biochem Biophys Res Commun. 1996;219:219-226.
21. Cassano G, Gasparre G, Niso M, Contino M, Scalera V, Colabufo NA. F281, synthetic agonist of the sigma-2 receptor, induces Ca21 efflux from the endoplasmic reticulum and mitochondria in SK-N-SH cells. Cell Calcium. 2009;45:340-345.
22. Crawford KW, Coop A, Bowen WD. Sigma(2) receptors regulate changes in sphingolipid levels in breast tumor cells. Eur J Pharmacol. 2002;443:207-209.
23. Wang L, Prescott AR, Spruce BA, Sanderson J, Duncan G. Sigma receptor antagonists inhibit human lens cell growth and induce pigmentation. Invest Ophthalmol Vis Sci. 2005;46:1403-1408.
24. Dai Y, Wei Z, Sephton CF, Zhang D, Anderson DH, Mousseau DD. Haloperidol induces the nuclear translocation of phosphatidylinositol 39-kinase to disrupt Akt phosphorylation in PC12 cells. J Psychiatry Neurosci. 2007;32:323-330.
25. Wei Z, Mousseau DD, Dai Y, Cao X, Li X-M. Haloperidol induces apoptosis via the sigma2 receptor system and Bcl-XS. Pharmacogenomics J. 2006;6:279-288.
26. Wei Z, Qi J, Dai Y, Bowen WD, Mousseau DD. Haloperidol disrupts Akt signalling to reveal a phosphorylation-dependent regulation of pro-apoptotic Bcl-XS function. Cell Signal. 2009;21:161-168.
27. de Bruyn M, Rybczynska AA, Wei Y, et al. Melanoma-associated chondroitin sulfate proteoglycan (MCSP)-targeted delivery of soluble TRAIL potently inhibits melanoma outgrowth in vitro and in vivo. Mol Cancer. 2010;9:301.
28. Rybczynska AA, Dierckx RA, Ishiwata K, Elsinga PH, van Waarde A. Cytotoxicity of sigma-receptor ligands is associated with major changes of cellular metabolism and complete occupancy of the sigma-2 subpopulation. J Nucl Med. 2008;49:2049-2056.
29. Achison M, Boylan MT, Hupp TR, Spruce BA. HIF-1alpha contributes to tumour- selective killing by the sigma receptor antagonist rimcazole. Oncogene. 2007;26:1137-1146.
30. Hamacher K, Coenen HH, Stöcklin G. Efficient stereospecific synthesis of nocarrier- added 2-[18F]-fluoro-2-deoxy-D-glucose using aminopolyether supported nucleophilic substitution. J Nucl Med. 1986;27:235-238.
31. Vilner BJ, John CS, Bowen WD. Sigma-1 and sigma-2 receptors are expressed in a wide variety of human and rodent tumor cell lines. Cancer Res. 1995;55:408-413.
32. Inoue A, Sugita S, Shoji H, Ichimoto H, Hide I, Nakata Y. Repeated haloperidol treatment decreases sigma(1) receptor binding but does not affect its mRNA levels in the guinea pig or rat brain. Eur J Pharmacol. 2000;401:307-316.
33. vanWaarde A, Shiba K, De Jong JR, Ishiwata K, Dierckx RA, Elsinga PH. Rapid reduction of sigma1-receptor binding and 18F-FDG uptake in rat gliomas after in vivo treatment with doxorubicin. J Nucl Med. 2007;48:1320-1326.
34. Mortimer JE, Dehdashti F, Siegel BA, Trinkaus K, Katzenellenbogen JA, Welch MJ. Metabolic flare: indicator of hormone responsiveness in advanced breast cancer. J Clin Oncol. 2001;19:2797-2803.
35. Dehdashti F, Mortimer JE, Trinkaus K, et al. PET-based estradiol challenge as a predictive biomarker of response to endocrine therapy in women with estrogenreceptor- positive breast cancer. Breast Cancer Res Treat. 2009;113:509-517.
36. Rybczynska AA. Sigma Receptor Ligands: Novel Applications in Cancer Imaging and Treatment [Ph.D.thesis]. Groningen, The Netherlands: University of Groningen 2012.
37. Tang D, Okada H, Ruland J, et al. Akt is activated in response to an apoptotic signal. J Biol Chem. 2001;276:30461-30466.
38. Klouz A, Sapena R, Liu J, et al. Evidence for sigma-1-like receptors in isolated rat liver mitochondrial membranes. Br J Pharmacol. 2002;135:1607-1615.
39. Chan SL, Morgan NG. Sigma receptor ligands and imidazoline secretagogues mediate their insulin secretory effects by activating distinct receptor systems in isolated islets. Eur J Pharmacol. 1998;350:267-272.