Abstract
Much research effort has been made to understand various biological processes at levels of molecules using molecular imaging techniques. Because of great sensitivity, high resolution, and rapid detection, positron emission tomography (PET) imaging is becoming one of the most used imaging techniques for medical diagnose and pre-clinical studies. Here we provide a review on molecular imaging and PET imaging. An introduction is also provided on 18F-fluorine labeling techniques for the preparation of PET imaging probes. A summary and comparison of currently available 18F-fluorine labeling methods is provided. The perspectives for 18F-fluorine labeling techniques are also given.
Similar content being viewed by others
References
Herschman HR. Molecular imaging: Looking at problems, seeing solutions. Science, 2003, 302: 605–608
Tsien RY. Imagining imaging’s future. Nat Rev Mol Cell Biol, 2003: Ss16–Ss21
Doubrovin M, Serganova I, Mayer-Kuckuk P, Ponomarev V, Blasberg RG. Multimodality in vivo molecular-genetic imaging. Bioconjugate Chem 2004, 15: 1376–1388
Willmann JK, van Bruggen N, Dinkelborg LM, Gambhir SS. Molecular imaging in drug development. Nat Rev Drug Discovery, 2008, 7: 591–607
O’Farrell AC, Shnyder SD, Marston G, Coletta PL, Gill JH. Non-invasive molecular imaging for preclinical cancer therapeutic development. Br J Pharmacol, 2013, 169: 719–735
Alberti C. From molecular imaging in preclinical/clinical oncology to theranostic applications in targeted tumor therapy. Eur Rev Med Pharmacol Sci, 2012, 16: 1925–1933
Blankenberg FG, Strauss HW. Recent advances in the molecular imaging of programmed cell death: Part II-Non-probe-based MRI, ultrasound, and optical clinical imaging techniques. J Nucl Med, 2013, 54: 1–4
Czernin J, Weber WA, Herschman HR. Molecular imaging in the development of cancer therapeutics. Annu Rev Med, 2006, 57: 99–118
Li K, Ding D, Zhao Q, Sun J, Tang BZ, Liu B. Biocompatible organic dots with aggregation-induced emission for in vitro and in vivo fluorescence imaging. Sci China Chem, 2013, 56: 1247–1252
Wang Z. Plasmon-resonant gold nanoparticles for cancer optical imaging. Sci China Phys Mech Astron, 2013, 56: 506–513
Liu C, Han H, Ta D, Wang W. Effect of selected signals of interest on ultrasonic backscattering measurement in cancellous bones. Sci China Phys Mech Astron, 2013, 56: 1310–1316
Wang W, Zhu J-J. Optical applications of quantum dots in biological system. Sci China Chem 2011, 54: 1177–1184
Mather S. Molecular imaging with bioconjugates in mouse models of cancer. Bioconjugate Chem, 2009, 20: 631–643
Li Y, Shionhara R, Iwami K, Ohta Y, Umeda N. Observation of mitochondrial activity based on temporal and spatial pH variations measured by near-field fluorescent ratiometry. Sci China Phys Mech Astron, 2011, 54: 2225–2229
Wen J, Lu H, Wang X, Yuan K, Lue H, Zhou Y, Jin K, Yang G, Li W, Ruan K. Detection of protein microarrays by oblique-incidence reflectivity difference technique. Sci China Phys Mech Astron, 2010, 53: 306–309
Yuan K, Wang X, Lu H, Wen J, Lu H, Zhou Y, Jin K-J, Yang G, Li W, Ruan K. Label-free detection of hybridization of oligonucleotides by oblique-incidence reflectivity difference method. Sci China Phys Mech Astron, 2010, 53: 1434–1437
Yang W, Lin Y, Zhang X, Zhang J, Wang X. Synthesis of several MPP derivatives for Tc-99m-labelling and evaluated as potential 5-HT1A receptor imaging agents. Sci China Chem, 2011, 54: 1148–1154
Zhu Z, Zhao X, Qin W, Chen G, Qian J, Xu Z. Fluorescent AIE dots encapsulated organically modified silica (ORMOSIL) nanoparticles for two-photon cellular imaging. Sci China Chem, 2012, 56: 1247–1252
Yang H, Zhao B, Yan Q, Liu Y, Hu H. Decoding algorithms of single photon counting imager based on two-dimensional Vernier anodes. Sci China Phys Mech Astron, 2011, 54: 1943–1947
Dobrucki LW, Sinusas AJ. Imaging angiogenesis. Curr Opin Biotechnol 2007, 18: 90–96
Ametamey SM, Honer M, Schubiger PA. Molecular imaging with PET. Chem Rev, 2008, 108: 1501–1516
Le Bars D. Fluorine-18 and medical imaging: Radiopharmaceuticals for positron emission tomography. J Fluorine Chem, 2006, 127: 1488–1493
Sun W, Ma W, Zhang R, Guo L, Jiang Y, Han L. Effects of the littlest Higgs model on the process e+e− → µ+µ− at a Z 0-factory. Sci China Phys Mech Astron, 2010, 53: 1961–1967
Chang C, Wang J, Wu X. Production of a heavy quarkonium with a photon or via ISR at Z peak in e+e− collider. Sci China Phys Mech Astron, 2010, 53: 2031–2036
Budinger TF, Brennan KM, Moses WW, Derenzo SE. Advances in positron tomography for oncology. Nucl Med Biol, 1996, 23: 659–667
Saha GB, Performance characteristics of PET Scanners. In: Basics of PET Imaging: Physics, Chemistry, and Regulations. Springer: New York, 2010. 97–113
Vallabhajosula S. F-18-Labeled positron emission tomographic radiopharmaceuticals in oncology: An overview of radiochemistry and mechanisms of tumor localization. Semin Nucl Med, 2007, 37: 400–419
Delacrois D, Guerre JP, Leblanc P, Hickman C. Radionuclide and Radiation Protection Data Handbook 2002. Nuclear Technology Publishing, 2002
Schlyer DJ. PET tracers and radiochemistry. Ann Acad Med Singap, 2004, 33: 146–154
Lodi F, Malizia C, Castellucci P, Cicoria G, Fanti S, Boschi S. Synthesis of oncological C-11 radiopharmaceuticals for clinical PET. Nucl Med Biol, 2012, 39: 447–460
Tu Z, Mach RH. C-11 radiochemistry in cancer imaging applications. Curr Top Med Chem, 2010, 10: 1060–1095
Toyohara J, Sakata M, Wu J, Ishikawa M, Oda K, Ishii, K, Iyo M, Hashimoto K, Ishiwata K. Preclinical and the first clinical studies on [(11)C]CHIBA-1001 for mapping alpha 7 nicotinic receptors by positron emission tomography. Ann Nucl Med, 2009, 23: 301–309
Ishiwata K, Tsukada H, Kubota K, Nariai T, Harada N, Kawamura K, Kimura Y, Oda K, Iwata R, Ishii K. Preclinical and clinical evaluation of O-[C-11]methyl-L-tyrosine for tumor imaging by positron emission tomography. Nucl Med Biol, 2005, 32: 253–262
Anderson CJ, Ferdani R. Copper-64 radiopharmaceuticals for PET imaging of cancer: Advances in preclinical and clinical research. Cancer Biother Radiopharm, 2009, 24: 379–393
Smith SV. Molecular imaging with copper-64 in the drug discovery and development arena. Expert Opin Drug Discov, 2007, 2: 659–672
Smith SV. Molecular imaging with copper-64. J Inorg Biochem 2004, 98: 1874–1901
Cutler PD, Schwarz SW, Anderson CJ, Connett JM, Welch MJ, Philpott GW, Siegel BA. Dosimetry of copper-64-labeled monoclonal-antibody 1a3 as determined by pet imaging of the torso. J Nucl Med, 1995, 36: 2363–2371
Fani M, Andre JP, Maecke HR. Ga-68-PET: A powerful generator-based alternative to cyclotron-based PET radiopharmaceuticals. Contrast Media Mol Imaging, 2008, 3: 53–63
Morgat C, Hindie E, Mishra AK, Allard M, Fernandez P. Gallium-68: Chemistry and radiolabeled peptides exploring different oncogenic pathways. Cancer Biother Radiopharm, 2013, 28: 85–97
Deri MA, Zeglis BM, Francesconi LC, Lewis JS. PET imaging with Zr-89: From radiochemistry to the clinic. Nucl Med Biol, 2013, 40: 3–14
Varagnolo L, Stokkel MPM, Mazzi U, Pauwels EKJ. F-18-labeled radiopharmaceuticals for PET in oncology, excluding FDG. Nucl Med Biol, 2000, 27: 103–112
Huang C, McConathy J. Fluorine-18 labeled amino acids for oncologic imaging with positron emission tomography. Curr Top Med Chem, 2013, 13: 871–891
Zeng F, Goodman MM. Fluorine-18 radiolabeled heterocycles as pet tracers for imaging beta-amyloid plaques in Alzheimer’s disease. Curr Top Med Chem, 2013, 13: 909–919
Helus F, Maierborst W, Sahm U, Wiebe LI. F-18 cyclotron production methods. Radiochem Radioanal Lett, 1979, 38: 395–410
Snell AH. In: Minutes of the Pasadena Meeting. Proceedings of the American Physical Society, Pasadena, December 18 and 19. Phys Rev: Pasadena, 1936. 142–150
Nickles RJ, Hichwa RD, Daube ME, Hutchins GD, Congdon DD. An O-18(2)-target for the high-yield production of F-18-fluoride. Int J Appl Radiat Is, 1983, 34: 625–629
Ruth TJ, Wolf AP. Absolute cross-sections for the production of F-18 via the O-18 (P, N) F-18 reaction. Radiochim Acta, 1979, 26: 21–24
Kilbourn MR, Hood JT, Welch MJ. A simple O-18 water target for F-18 production. Int J Appl Radiat Is, 1984, 35: 599–602
Peeples JL, Stokely MH, Doster JM. Thermal performance of batch boiling water targets for F-18 production. Appl Radiat Isot, 2011, 69: 1349–1354
Ido T, Wan CN, Fowler JS, Wolf AP. Fluorination with F2 — Convenient synthesis of 2-deoxy-2-fluoro-D-glucose. J Org Chem 1977, 42: 2341–2342
Fowler JS, MacGregor RR, Wolf AP, Farrell AA, Karlstrom KI, Ruth, TJ. A shielded synthesis system for production of 2-deoxy-2-[F-18]fluoro-D-glucose. J Nucl Med, 1981, 22: 376–380
Bida GT, Satyamurthy N, Barrio JR. The synthesis of 2-[F-18] fluoro-2-deoxy-D-glucose using glycals — A reexamination. J Nucl Med, 1984, 25: 1327–1334
Korytnyk W, Valentekovic-Horvat S. Reactions of glycals with xenon fluoride — An improved synthesis of 2-deoxy-2-fluorosaccharides. Tetrahedron Lett, 1980, 21: 1493–1496
Shiue CY, To KC, Wolf AP. A rapid synthesis of 2-deoxy-2-fluorodeuterium-glucose from xenon difluoride suitable for labeling with F-18. J Labelled Compd Radiopharm, 1983, 20: 157–162
Sood S, Firnau G, Garnett ES. Radiofluorination with xenon difluoride — A new high-yield synthesis of [F-18]2-fluoro-2-deoxydeuterium-glucose. Int J Appl Radiat Is, 1983, 34: 743–745
Firnau G, Chirakal R, Sood S, Garnett ES. Radiofluorination with xenon difluoride-l-6[F-18]fluoro-dopa. J Labelled Compd Radiopharm, 1981, 18: 7–8
Firnau G, Chirakal R, Sood S, Garnett S. Aromatic fluorination with xenon difluoride — l-3,4-Dihydroxy-6-fluoro-phenylalanine. Can J Chem, 1980, 58: 1449–1450
Hiller A, Fischer C, Jordanova A, Patt JT, Steinbach J. Investigations to the synthesis of n.c.a. F-18 FClO3 as electrophilic fluorinating agent. Appl Radiat Isot, 2008, 66: 152–157
Shiue CY, Salvadori PA, Wolf AP, Fowler JS, Macgregor RR. A new improved synthesis of 2-deoxy-2-(F-18)fluoro-D-glucose from F-18-labeled acetyl hypofluorite. J Nucl Med, 1982, 23: 899–903
Ehrenkaufer RE, Potocki JF, Jewett DM. Simple synthesis of F-18-labeled 2-fluoro-2-deoxy-D-glucose — Concise communication. J Nucl Med, 1984, 25: 333–337
Bishop A, Satyamurthy N, Bida G, Barrio JR. Chemical reactivity of the F-18 electrophilic reagents from the O-18(p,n)F-18 gas target systems. Nucl Med Biol, 1996, 23: 559–565
Lerman O, Tor Y, Hebel D, Rozen S. A novel electrophilic fluorination of activated aromatic rings using acetyl hypofluorite, suitable also for introducing F-18 into benzene nuclei. J Org Chem, 1984, 49: 806–813
Hess E, Sichler S, Kluge A, Coenen HH. Synthesis of 2-[(18)F] fluoro-L-tyrosine via regiospecific fluoro-de-stannylation. Appl Radiat Isot 2002, 57: 185–191
Dolle F, Demphel S, Hinnen F, Fournier D, Vaufrey F, Crouzel C. 6-[F-18]fluoro-L-DOPA by radiofluorodestannylation: A short and simple synthesis of a new labelling precursor. J Labell Compd Radiopharm, 1998, 41: 105–114
Forsback S, Eskola O, Haaparanta M, Bergman J, Solin O. Electrophilic synthesis of 6-F-18 fluoro-L-DOPA using post-target produced F-18 F-2. Radiochim Acta, 2008, 96: 845–848
Hamacher K, Coenen HH, Stocklin G. Efficient stereospecific synthesis of no-carrier-added 2-[F-18]-fluoro-2-deoxy-D-glucose using aminopolyether supported nucleophilic-substitution. J Nucl Med, 1986, 27: 235–238
Fuchtner F, Preusche S, Mading P, Zessin J, Steinbach J. Factors affecting the specific activity of [F-18]fluoride from a [O-18] water target. Nuklearmed Nucl Med, 2008, 47: 116–119
Schirrmacher R, Wangler C, Schirrmacher E. Recent developments and trends in F-18-radiochemistry: Syntheses and applications. Mini-Rev Org Chem, 2007, 4: 317–329
Liu C, Jiang S. Preparation of two triflate precursors for O-(2-[18F] fluoroethyl)-L-tyrosine used in positron emission tomography (PET). Sci China Chem, 2009, 52: 2195–2199
Alauddin MM, Fissekis JD, Conti PS. Synthesis of [F-18]-labeled adenosine analogues as potential PET imaging agents. J Labelled Compd Radiopharm, 2003, 46: 805–814
Fookes CJR, Pham TQ, Mattner F, Loc’h C, Liu X, Berghofer P, Shepherd R, Gregoire MC, Katsifis A, Greguric I. Synthesis and biological evaluation of substituted [F-18]imidazo[1,2-a]pyridines and [F-18]pyrazolo [1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positron emission tomography. J Med Chem, 2008, 51: 3700–3712
Gill HS, Tinianow JN, Ogasawara A, Flores JE, Vanderbilt AN, Raab H, Scheer JM, Vandlen R, Williains SP, Marik J. A modular platform for the rapid site-specific radiolabeling of proteins with (18)F exemplified by quantitative positron emission tomography of human epidermal growth factor receptor 2. J Med Chem, 2009, 52: 5816–5825
Sachin K, Kim EM, Cheong SJ, Jeong HJ, Lim ST, Sohn MH, Kim DW. Synthesis of N(4)′-[(18)F]fluoroalkylated ciprofloxacin as a potential bacterial infection imaging agent for PET study. Bioconjugate Chem, 2010, 21: 2282–2288
Gao MZ, Wang M, Miller KD, Sledge GW, Hutchins GD, Zheng QH. Synthesis of radiolabeled stilbene derivatives as new potential PET probes for aryl hydrocarbon receptor in cancers. Bioorg Med Chem Lett, 2006, 16: 5767–5772
Viel T, Kuhnast B, Hinnen F, Boisgard R, Tavitian B, Dolle F. Fluorine-18 labelling of small interfering RNAs (siRNAs) for PET imaging. J Labelled Compd Radiopharm, 2007, 50: 1159–1168
Kapur S, Jones C, DaSilva J, Wilson A, Houle S. Reliability of a simple non-invasive method for the evaluation of 5-HT2 receptors using [F-18]-setoperone PET imaging. Nucl Med Commun, 1997, 18: 395–399
Flavell RR, Kothari P, Bar-Dagan M, Synan M, Vallabhajosula S, Friedman JM, Muir TW, Ceccarini G. Site-specific F-18-labeling of the protein hormone leptin using a general two-step ligation procedure. J Am Chem Soc, 2008, 130: 9106–9112
Schottelius M, Berger S, Poethko T, Schwaiger M, Wester HJ. Development of novel Ga-68- and F-18-labeled GnRH-I analogues with high GnRHR-targeting efficiency. Bioconjugate Chem, 2008, 19: 1256–1268
Pike VW, Aigbirhio FI. Reactions of cyclotron-produced [F-18] fluoride with diaryliodonium-salts — A novel single-step route to nocarrier-added [(18)]fluoroarenes. J Chem Soc Chem Commun, 1995: 2215-2216
Chun J, Lu S, Lee YS, Pike VW. Radiofluorination of unsymmetrical diaryliodonium salt complies with the Curtin-Hammett principle. J Labelled Compd Radiopharm, 2009, 52: S159–S159
Chun JH, Lu SY, Lee YS, Pike VW. Fast and high-yield microreactor syntheses of ortho-substituted [(18)f]fluoroarenes from reactions of [(18)f]fluoride ion with diaryliodonium salts. J Org Chem, 2010, 75: 3332–3338
Mu, L, Fischer, CR, Holland, JP, Becaud, J, Schubiger, PA, Schibli, R, Ametamey, SM, Graham, K, Stellfeld, T, Dinkelborg, LM, Lehmann L. 18F-Radiolabeling of aromatic compounds using triarylsulfonium salts. Eur J Org Chem, 2012: 889-892
Chun J-H, Morse CL, Chinz FT, Pike VW. No-carrier-added F-18 fluoroarenes from the radiofluorination of diaryl sulfoxides. Chem Commun, 2013, (49): 2151–2153
Studenov AR, Adam MJ, Wilson JS, Ruth TJ. New radiolabelling chemistry: Synthesis of phosphorus-[F-18]fluorine compounds. J Labelled Compd Radiopharm, 2005, 48: 497–500
McBride WJ, Sharkey RM, Karacay H, D’Souza CA, Rossi EA, Laverman P, Chang CH, Boerman OC, Goldenberg DM. A novel method of (18)F radiolabeling for PET. J Nucl Med, 2009, 50: 991–998
McBride WJ, D’Souza CA, Sharkey RM, Karacay H, Rossi EA, Chang CH, Goldenberg DM. Improved (18)F labeling of peptides with a fluoride-aluminum-chelate complex. Bioconjugate Chem, 2010, 21: 1331–1340
Laverman P, McBride WJ, Sharkey RM, Eek A, Joosten L, Oyen WJG, Goldenberg DM, Boerman OC. A novel facile method of labeling octreotide with (18)F-fluorine. J Nucl Med, 2010, 51: 454–461
D’Souza CA, McBride WJ, Sharkey RM, Todaro LJ, Goldenberg DM. High-yielding aqueous 18F-labeling of peptides via Al18F chelation. Bioconjugate Chem, 2011, 22: 1793–1803
Schirrmacher R, Bradtmoller G, Schirrmacher E, Thews O, Tillmanns J, Siessmeier T, Buchholz HG, Bartenstein P, Waengler B, Niemeyer CM, Jurkschat K. F-18-labeling of peptides by means of an organosilicon-based fluoride acceptor. Angew Chem Int Ed, 2006, 45: 6047–6050
Hoehne A, Mu L, Honer M, Schubiger PA, Ametamey SM, Graham K, Stellfeld T, Borkowski S, Berndorff D, Klar U, Voigtmann U, Cyr JE, Friebe M, Dinkelborg L, Srinivasan A. Synthesis, F-18-labeling, and in vitro and in vivo studies of bombesin peptides modified with silicon-based building blocks. Bioconjugate Chem, 2008, 19: 1871–1879
Mu LJ, Hohne A, Schubiger RA, Ametamey SM, Graham K, Cyr JE, Dinkelborg L, Stellfeld T, Srinivasan A, Voigtmann U, Klar U. Silicon-based building blocks for one-step F-18-radiolabeling of peptides for PET imaging. Angew Chem Int Ed, 2008, 47: 4922–4925
Iovkova L, Konning D, Wangler B, Schirrmacher R, Schoof S, Arndt HD, Jurkschat K. SiFA-modified phenylalanine: A key compound for the efficient synthesis of (18)F-labelled peptides. Eur J Inorg Chem, 2011: 2238-2246
Kostikov AP, Iovkova L, Chin J, Schirrmacher E, Wangler B, Wangler C, Jurkschat K, Cosa G, Schirrmacher R. N-(4-(di-tert-butyl[(18)F]fluorosilyl)benzyl)-2-hydroxy-N,N-dimethylethylammonium bromide ([(18)F]SiFAN(+)Br(-)): A novel lead compound for the development of hydrophilic SiFA-based prosthetic groups for (18)F-labeling. J Fluorine Chem, 2011, 132: 27–34
Wangler C, Waser B, Alke A, Iovkova L, Buchholz HG, Niedermoser S, Jurkschat K, Fottner C, Bartenstein P, Schirrmacher R, Reubi JC, Weste HJ, Wangler B. One-step (18)F-labeling of carbohydrate-conjugated octreotate-derivatives containing a siliconfluoride-acceptor (SiFA): In vitro and in vivo evaluation as tumor imaging agents for positron emission tomography (PET). Bioconjugate Chem, 2010, 21: 2289–2296
Iovkova L, Wangler B, Schirrmacher E, Schirrmacher R, Quandt G, Boening G, Schurmann M, Jurkschat K. para-Functionalized aryldi-tert-butylfluorosilanes as potential labeling synthons for (18)F radiopharmaceuticals. Chem Eur J, 2009, 15: 2140–2147
Ting R, Adam MJ, Ruth TJ, Perrin DM. Arylfluoroborates and alkylfluorosilicates as potential PET imaging agents: High-yielding aqueous biomolecular F-18-labeling. J Am Chem Soc, 2005, 127: 13094–13095
Ting R, Harwig C, auf dem Keller U, McCormick S, Austin P, Overall CM, Adam MJ, Ruth TJ, Perrin DM. Toward [F-18]-labeled aryltrifluoroborate radiotracers: In vivo positron emission tomography imaging of stable aryltrifluoroborate clearance in mice. J Am Chem Soc, 2008, 130: 12045–12055
Ting R, Lo J, Adam MJ, Ruth TJ, Perrin, DM. Capturing aqueous [F-18]-fluoride with an arylboronic ester for PET: Synthesis and aqueous stability of a fluorescent [F-18]-labeled aryltrifluoroborate. J Fluorine Chem, 2008, 129: 349–358
Ting R, Aguilera TA, Crisp JL, Hall DJ, Eckelman WC, Vera DR, Tsien RY. Fast (18)F labeling of a near-infrared fluorophore enables positron emission tomography and optical imaging of sentinel Lymph nodes. Bioconjugate Chem, 2010, 21: 1811–1819
Jauregui-Osoro M, Sunassee K, Weeks AJ, Berry DJ, Paul RL, Cleij M, Banga J, O’Doherty MJ, Marsden PK, Clarke SEM, Ballinger JR, Szanda I, Cheng SY, Blower PJ. Synthesis and biological evaluation of [(18)F]tetrafluoroborate: A PET imaging agent for thyroid disease and reporter gene imaging of the sodium/iodide symporter. Eur J Nucl Med Mol Imaging, 2010, 37: 2108–2116
Gao H, Lang L, Guo N, Cao F, Quan Q, Hu S, Kiesewetter DO, Niu G, Chen X. PET imaging of angiogenesis after myocardial infarction/reperfusion using a one-step labeled integrin-targeted tracer F-18-AlF-NOTA-PRGD2. Eur J Nucl Med Mol Imaging, 2012, 39: 683–692
Guo N, Lang L, Li W, Kiesewetter DO, Gao H, Niu G, Xie Q, Chen X. Quantitative analysis and comparison study of F-18 AlF-NOTA-PRGD2, 18F FPPRGD2 and Ga-68 Ga-NOTA-PRGD2 using a reference tissue model. PLoS One, 2012, 7: 103
McBride WJ, D’Souza CA, Sharkey RM, Goldenberg DM. The radiolabeling of proteins by the F-18 AlF method. Appl Radiat Isot, 2012, 70: 200–204
Crouch RD. Selective monodeprotection of bis-silyl ethers. Tetrahedron, 2004, 60: 5833–5871
Rosenthal MS, Bosch AL, Nickles RJ, Gatley SJ. Synthesis and some characteristics of no-carrier added [F-18] fluorotrimethylsilane. Int J Appl Radiat Is, 1985, 36: 318–319
Amigues E, Schulz J, Szlosek-Pinaud M, Fernandez P, Silvente-Poirot S, Brillouet S, Courbon F, Fouquet E. F-18 Si-RiboRGD: From design and synthesis to the imaging of alpha(v)beta(3) integrins in melanoma tumors. Chempluschem, 2012, 77: 345–349
Kostikov AP, Chin J, Orchowski K, Niedermoser S, Kovacevic MM, Aliaga A, Jurkschat K, Waengler B, Waengler C, Wester H-J, Schirrmacher R. Oxalic acid supported Si-F-18-radiofluorination: One-step radiosynthesis of N-succinimidyl 3-(di-tert-butyl F-18 fluorosilyl) benzoate ( F-18 SiFB) for protein labeling. Bioconjugate Chem, 2012, 23: 106–114
Joyard Y, Azzouz R, Bischoff L, Papamicael C, Labar D, Bol A, Bol V, Vera P, Gregoire V, Levacher V, Bohn P. Synthesis of new F-18-radiolabeled silicon-based nitroimidazole compounds. Bioorg Med Chem, 2013, 21: 3680–3688
Ting R, Harwig CW, Lo J, Li Y, Adam MJ, Ruth TJ, Perrin DM. Substituent effects on aryltrifluoroborate solvolysis in water: Implications for Suzuki-Miyaura coupling and the design of stable F-18-labeled aryltrifluoroborates for use in PET imaging. J Org Chem, 2008, 73: 4662–4670
Keller UAD, Bellac CL, Li Y, Lou YM, Lange PF, Ting R, Harwig C, Kappelhoff R, Dedhar S, Adam MJ, Ruth TJ, Benard F, Perrin DM, Overall CM. Novel matrix metalloproteinase inhibitor [F-18] marimastat-aryltrifluoroborate as a probe for in vivo positron emission tomography imaging in cancer. Cancer, Res 2010, 70: 7562–7569
Li Y, Ting R, Harwig CW, Keller UAD, Bellac CL, Lange PF, Inkster JAH, Schaffer P, Adam MJ, Ruth TJ, Overall CM, Perrin DM. Towards kit-like F-18-labeling of marimastat, a noncovalent inhibitor drug for in vivo PET imaging cancer associated matrix metalloproteases. Medchemcomm, 2011, 2: 942–949
Li Y, Guo J, Tang S, Lang L, Chen X, Perrin DM. One-step and one-pot-two-step radiosynthesis of cyclo-RGD-(18)F-aryltrifluoroborate conjugates for functional imaging. Am J Nucl Med Mol Imaging, 2013, 3: 44–56
Li Y, Liu Z, Lozada J, Wong MQ, Lin K-S, Yapp D, Perrin DM. Single step 18F-labeling of dimeric cycloRGD for functional PET imaging of tumors in mice. Nucl Med Biol, 2013, 40: 959–966
Li Y, Liu Z, Harwig CW, Pourghiasian M, Lau J, Lin K-S, Schaffer P, Benard F, Perrin DM. (18)F-click labeling of a bombesin antagonist with an alkyne-(18)F-ArBF(3) (-): In vivo PET imaging of tumors expressing the GRP-receptor. Am J Nucl Med Mol Imaging, 2013, 3: 57–70
Weeks AJ, Jauregui-Osoro M, Cleij M, Blower JE, Ballinger JR, Blower PJ. Evaluation of [(18)F]-tetrafluoroborate as a potential PET imaging agent for the human sodium/iodide symporter in a new colon carcinoma cell line, HCT116, expressing hNIS. Nucl Med Commun, 2011, 32: 98–105
Liu Z, Li Y, Lozada J, Wang M, Lin K-S, Yepp D, Perrin D. Novel F-18-radiolabeling of RGD at super high specific activity by isotope exchange. J Labelled Compd Radiopharm, 2013, 56: S167–S167
Liu Z, Li Y, Lozada J, Wong MQ, Greene J, Lin K-S, Yapp D, Perrin DM. Kit-like (18)F-labeling of RGD-(19)F-Arytrifluroborate in high yield and at extraordinarily high specific activity with preliminary in vivo tumor imaging. Nucl Med Biol, 2013, 40: 841-9
Liu Z, Li Y, Lozada J, Schaffer P, Adam MJ, Ruth TJ, Perrin DM. Stoichiometric leverage: Rapid 18F-aryltrifluoroborate radiosynthesis at high specific activity for click conjugation. Angew Chem Int Ed, 2013, 52: 2303–2307
Inkster JAH, Liu K, Ait-Mohand S, Schaffer P, Guerin B, Ruth TJ, Storr T. Sulfonyl fluoride-based prosthetic compounds as potential 18F labelling agents. Chem Eur J, 2012, 18: 11079–11087
Zhang S, Yang K, Liu Z. Carbon nanotubes for in vivo cancer nanotechnology. Sci China Chem, 2010, 53: 2217–2225
Bu H, Gao Y, Li Y. Overcoming multidrug resistance (MDR) in cancer by nanotechnology. Sci China Chem, 2010, 53: 2226–2232
Xu X, Li C, Li H, Liu R, Jiang C, Wu Y, He B, Gu Z. Polypeptide dendrimers: Self-assembly and drug delivery. Sci China Chem, 2011, 54: 326–333
Lee Y, Deng P. Review of micro/nano technologies and theories for electroporation of biological cells. Sci China Phys Mech Astron, 2012, 55: 996–1003
Romero G, Murray RA, Qiu Y, Sanz D, Moya SE. Layer by layer surface engineering of poly(lactide-co-glycolide) nanoparticles: A versatile tool for nanoparticle engineering for targeted drug delivery. Sci China Chem, 2013, 56: 1029–1039
Orbay H, Hong H, Zhang Y, Cai W. PET/SPECT imaging of hindlimb ischemia: focusing on angiogenesis and blood flow. Angiogenesis, 2013, 16: 279–287
Bai J, Liu F, Liu X. Progress on multi-modality molecular imaging. Curr Med Imag Rev 2012, 8: 295–301
Yankeelov TE, Peterson TE, Abramson RG, Garcia-Izquierdo D, Arlinghaus LR, Li X, Atuegwu NC, Catana C, Manning HC, Fayad ZA, Gore JC. Simultaneous PET-MRI m oncology: A solution looking for a problem? Magn Reson Imag, 2012, 30: 1342–1356
Tomasi G, Rosso L. PET imaging: implications for the future of therapy monitoring with PET/CT in oncology. Curr Opin Pharmacol, 2012, 12: 569–575
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Li, Y. 18F-labeling techniques for positron emission tomography. Sci. China Chem. 56, 1682–1692 (2013). https://doi.org/10.1007/s11426-013-5004-8
Received:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1007/s11426-013-5004-8