[1]林潇,唐明灯.靶向表皮生长因子受体分子探针研究进展[J].国际放射医学核医学杂志,2015,39(1):85-90,102.[doi:10.3760/cma.j.issn.1673-4114.2015.01.018]
 Lin Xiao,Tang Mingdeng.Research progresses on molecular probes targeting epidermal growth factor receptor[J].International Journal of Radiation Medicine and Nuclear Medicine,2015,39(1):85-90,102.[doi:10.3760/cma.j.issn.1673-4114.2015.01.018]
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靶向表皮生长因子受体分子探针研究进展(/HTML)
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《国际放射医学核医学杂志》[ISSN:1673-4114/CN:12-1381/R]

卷:
39
期数:
2015年第1期
页码:
85-90,102
栏目:
出版日期:
2015-01-25

文章信息/Info

Title:
Research progresses on molecular probes targeting epidermal growth factor receptor
作者:
林潇 唐明灯
福建省肿瘤医院核医学科, 福州, 350014
Author(s):
Lin Xiao Tang Mingdeng
Department of Nuclear Medicine, Fujian Provincial Cancer Hospital, Fuzhou 350014, China
关键词:
表皮生长因子受体体层摄影术发射型计算机单光子正电子发射断层显像术分子探针
Keywords:
Epidermal growth factor receptorTomography emission-computed single-photonPositron emission tomographyMolecular probes
DOI:
10.3760/cma.j.issn.1673-4114.2015.01.018
摘要:
许多恶性肿瘤细胞的增殖、转移以及不良的预后已被证实与表皮生长因子受体(EGFR)的过度表达相关。目前,针对这个靶点,美国食品和药物管理局已经批准了多个靶向EGFR药物,如吉非替尼、厄洛替尼,但治疗效率总体偏低。核医学显像能够在分子水平上评价EGFR的表达水平及其突变程度,从而为临床个性化治疗提供有力依据。笔者简述靶向EGFR分子探针及其存在的缺点,以期为进一步研究提供帮助。
Abstract:
Overexpression of epidermal growth factor receptor (EGFR) has been confirmed to be associated with cell malignancy, metastasis and poor prognosis. Against this target, several drugs have been approvaled, such as gefitinib and erlotinib. However, the therapeutic effect was not satisfied. PET/SPECT imaging can evaluate the expression and mutation of EgFR at molecular level to provide the basis for individual treat. This article is an overview of the progress of PET/SPECT molecular probes targeting EGFR and related problems in order to provide help for further research.

参考文献/References:

[1] 孙莹莹,孙夕林,王凯,等.EGFR靶向的PET/SPECT分子成像研究进展[J].现代生物医学进展,2014,14(10):1980-1986.
[2] Laskin JJ,sandier AB.Eoidermal growth factor receotor:a promising target in solid tumours[J/OL].Cancer Treat Rev,2004,30(1):1-17[2014-11-09].http://www.sciencedirect.com/sci-ence/article/pii/S0305737203002020.
[3] Eccles SA.Cell biology of lymphatic metastasis.The potential role of c-erbB oncogene signalling[J].Recent Results Cancer Res,2000,157:41-54.
[4] Shepherd FA,Pereira JR,Ciuleanu T,et al.Erlotinib in previously treated non-small-cell lung cancer[J].N Engl J Med,2005,353(2):123-132.
[5] Madhusudan S,Ganesan TS.Tyrosine kinase inhibitors in cancer therapy[J/OL].Clin Biochem,2004,37(7):618-635[2014-11-01],http://www.sciencedirect.com/science/article/pii/S0009912004001298.
[6] Schiller JH.Noninvasive monitoring of tumors[J/OL].N Engl J Med,2008,359(4):418-420[2014-11-01].http://connec-tion.ebscohost.com/c/editorials/33291815/noninvasive-monitoring-tumors.
[7] Levitzki A.Protein kinase inhibitors as a therapeutic modality[J].Acc Chem Res,2003,36(6):462-469.
[8] Reilly RM,Kiarash R,Cameron RG,et al.111In-labeled EGF is se-lectively radiotoxic to human breast cancer cells overexpressing EGFR[J].J Nucl Med,2000,41(3):429-438.
[9] Reilly RM,Kiarash R,Cameron RG,et al.A comparison of EGF and Mab 528 labeled with 111In for imaging human breast cancer[J].J Nucl Med,2000,41(5):903-911.
[10] Jung KH,Park J W,Paik JY,et al.EGF receptor targeted tumorimaging with biotin-PEG-EGF linked to 99mTc-HYNIC labeledavidin and streptavidin[J].Nucl Med Biol,2012,39(8):1122-1127.
[11] Jung KH,Choe YS,Paik JY,et al.99mTc-Hydrazinonicotinamide epidermal growth factor-polyethylene glycol-quantum dot imagingallows quantification of breast cancer epidermal growth factor re-ceptor expression and monitors receptor downregulation in response to cetuximab therapy[J].J Nucl Med,2011,52(9):1457-1464.
[12] 戴春岭,符立梧.靶点药物Cetuximab(C225)研究新进展[J].生物化学与生物物理进展,2007,34(3):246-254.
[13] Schechter NR,Yang DJ,Azhdarinia A,et al.Assessment of epider-mal growth factor receptor with 99mTc-ethylenedicysteine-C225 monoclonal antibody[J].Anticancer Drugs,2003,14(1):49-56.
[14] Liu Z,Ma T,Liu H,et al.177Lu-labeled antibodies for EGFR-target-ed SPECT/CT imaging and radioimmunotherapy in a preclinical head and neck carcinoma model[J].Mol Pharm,2014,11(3):800-807.
[15] Xu N,Cai G,Ye W,et al.Molecular imaging application of radioio-dinated anti-EGFR human Fab to EGFR-overexpressing tumor xenografts[J].Anticancer Res,2009,29(10):4005-4011.
[16] Wang X,Zhu J,Zhao P,et al.In vitro efficacy of immuno-chemotherapy with anti-EGFR human fab-taxol conjugate on A431 epidermoid carcinoma cells[J].Cancer Biol Ther,2007,6(6):980-986.
[17] 董强刚,李建璋,黎飒,等.上皮生长因子受体外显子21基因突变L858R的实时定量PCR检测[J].肿瘤,2007,27(2):150-154.
[18] Pal A,Balatoni JA,Mukhopadhyay U,et al.Radiosynthesis and ini-tial in vitro evaluation of[18F] F-PEG6-IPQA——a novel PET radio-tracer for imaging E GFR expression-activity in lung carcinomas[J].Mol Imaging Biol,2011,13(5):853-861.
[19] Yeh HH,Ogawa K,Balatoni J,et al.Molecular imaging of active mutant L858R EG F receptor (EgFR) kinase-expressing nonsmall cell lung carcinomas using PET/CT[J].Proc Natl Acad Sci USA.2011,108(4):1603-1608.
[20] Pal A,Glekas A,Doubrovin M,et al.Molecular imaging of EGFR kinase activity in tumors with 124I-labeled small molecular tracer and positron emission tomography[J].Mol Imaging Biol,2006,8(5):262-277.
[21] Wong SF.Cetuximab:an epidermal growth factor receptor mono-clonal antibody for the treatment of colorectal cancer[J].Clin Ther,2005,27(6):684-694.
[22] Cai W,Chen K,He L,et al.Quantitative PET of EGFR expression in xenograft-bearing mice using 64Cu-labeled cetuximab,a chimeric anti-EGFR monoclonal antibody[J].Eur J Nucl Med Mol Imaging,2007,34(6):850-858.
[23] Sadri K,Ren Q,Zhang K,et al.PET imaging of EGFR expression in nude mice bearing MDA-MB-468,a human breast adenocarcino-ma[J].Nucl Med Commun,2011,32(7):563-569.
[24] Eiblmaier M,Meyer LA,Watson MA,et al.Correlating E GFR ex-pression with receptor-binding properties and internalization of 64Cu-DOTA-cetuximab in 5 cervical cancer cell lines[J].J Nucl Med,2008,49(9):1472-1479.
[25] Niu G,Sun XL,Cao QZ,et al.Cetuximab-Based immunotherapy and radioimmunotherapy of head and neck squamous cell carcinoma[J].Clin Cancer Res,2010,16(7):2095-2105.
[26] Perk LR,Visser GW,Vosjan MJ,et al.89Zr as a PET surrogate ra-dioisotope for scouting biodistribution of the therapeutic radiometals and 177Lu in tumor-bearing nude mice after coupling to the internalizing antibody cetuximab[J].J Nucl Med,2005,46(11):1898-1906.
[27] Aerts HJ,Dubois L,Perk L,et al.Disparity between in vivo EGFR expression and 89Zr-labeled cetuximab uptake assessed with PET[J].JNucl Med,2009,50(1):123-131.
[28] Miao Z,Ren G,Liu H,et al.PET of E GFR expression with an 18F-labeled affibody molecule[J].J Nucl Med,2012,53(7):1110-1118.
[29] Fredriksson A,Johnstrom P,Thorell JO,et al.In vivo evaluation of the biodistribution of 11C-labeled PD153035 in rats without and with neuroblastoma implants[J].Life Sci,1999,65(2):165-174.
[30] Meng X,Loo BW,Ma L,et al.Molecular imaging with 11C-PD153035 PET/CT predicts survival in non-small cell lung cancer treated with EGFR-TKI:a pilot study[J].J Nucl Med,2011,52(10):1573-1579.
[31] Memon AA,Jakobsen S,Dagnaes-Hansen F,et al.Positron emis-sion tomography (PET) imaging with[11C]-labeled erlotinib:a micro-PET study on mice with lung tumor xenografts[J].Cancer Res,2009,69(3):873-878.
[32] Memon AA,Weber B,Winterdahl M,et al.PET imaging of patients with non-small cell lung cancer employing an EGF receptor target-ing drug as tracer[J].Br J Cancer,2011,105(12):1850-1855.
[33] Holt DP,Ravert HT,Dannals RF,et al.Synthesis of [11C]gefitinib for imaging epidermal growth factor receptor tyrosine kinase with positron emission tomography[J/OL].J label compd Radiopharm,2006,49(10):883-888[2014-11-8].http://onlinelibrary.wi-ley.com/doi/10.1002/jlcr.1104/abstract.
[34] Zhang MR,Kumata K,Hatori A,et al.[11C]Gefitinib ([11C]Iressa):radiosynthesis,in vitro uptake,and in vivo imaging of intact murine fibrosarcoma[J].Mol Imaging Biology,2010,12(2):181-191.
[35] Murali D,Flores Lg.Evaluation of[F-18] iressa as a PET imaging agent for tumor overexpressing epidermal growth factor (EGFR) re-ceptors[J/OL].J Label Compd Radiopharm,2005,48(S1):S1-S341[2014-11-09].http://onlinelibrary.wiley.com/doi/10.1002/jlcr.v48:1%2B/issuetoc.
[36] Seimbille Y,Phelps ME,Czernin J,et al.Fluorine-18 labeling of 6,7-disubstituted anilinoquinazoline derivatives for positron emission tomography (PET) imaging of tyrosine kinase receptors:synthe-sis of 18F-Iressa and related molecular probes[J/OL].J Label Compd Radiopharm,2005,48(11):829-843[2014-11-01].http://onlinelibrary.wiley.com/doi/10.1002/jlcr.998/abstract.
[37] Su H,Seimbille Y,Ferl GZ,et al.Evaluation of [18F]gefitinib as a molecular imaging probe for the assessment of the epidermal growth factor receptor status in malignant tumors[J].Eur J Nucl Med Mol Imaging,2008,35(6):1089-1099.
[38] Bonasera TA,Ortu G,Rozen Y,et al.Potential 18F-labeled biomark-ers for epidermal growth factor receptor tyrosine kinase[J].Nucl Med Biol,2001,28(4):359-374.
[39] Ortu G,Ben-David I,Rozen Y,et al.Labeled EGFr-TK irreversible inhibitor(ML03):in vitro and in vivo properties,potential as PET biomarker for cancer and feasibility as anticancer drug[J].Int J Cancer,2002,101(4):360-370.
[40] Tsou HR,Mamuya N,Johnson BD,et al.6-Substituted-4-(3-bro-mophenylamino) quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epider-mal growth factor receptor(HER-2) tyrosine kinases with enhanced antitumor activity[J].J Med Chem,2001,44(17):2719-2734.
[41] Mishani E,Abourbeh G,Rozen Y,et al.Novel carbon-11 labeled 4-dimethylamino-but-2-enoic acid[4-(phenylamino)-quinazoline-6-yl]-amides:potential PET bioprobes for molecular imaging of EGFR-positive tumors[J].Nucl Med Biol,2004,31(4):469-476.
[42] Dissoki S,Laky D,Mishani E,et al.Fluorine-18 labeling of ML04-presently the most promising irreversible inhibitor candidate for vi-sulization of E GFR in cancer[J/OL].J Label Compd Radiopharm,2006,49(6):533-543[2014-11-9].http://onlinelibrary.wiley.com/doi/10.1002/jlcr.1071/abstract.
[43] Abourbeh G,Dissoki S,Jacobson O,et al.Evaluation of radiola-beled ML04,a putative irreversible inhibitor of epidermal growth factor receptor,as a bioprobe for PET imaging of EGFR-overex-pressing tumors[J].Nucl Med Biol,2007,34(1):55-70.
[44] Shaul M,Abourbeh G,Jacobson O,et al.Novel iodine-124 labeled EGFR inhibitors as potential PET agents for molecular imaging in cancer[J].Bioorg Med Chem,2004,12(13):3421-3429.
[45] Solca F,Dahl G,Zoephel A,et al.Target binding properties and cellular activity of afatinib (BIBW 2992),an irreversible ErbB family blocker[J].J Pharmacol Exp Ther,2012,343(2):342-350.
[46] Slobbe P,Windhorst AM.Development of [18F]afatinib as a new TKI-PET tracer for EGFR positive tumors[J].Nucl Med Biol,2014,41(9):749-757.
[47] Fernandes C,Oliveira C,Gano L,et al.Radioiodination of new EGFR inhibitors as potential SPECT agents for molecular imaging of breast cancer[J].Bioorg Med Chem,2007,15(12):3974-3980.
[48] Neto C,Fernandes C,Oliveira MC,et al.Radiohalogenated 4-anili-noquinazoline-based EGFR-TK inhibitors as potential cancer imag-ing agents[J].Nucl Med Biol,2012,39(2):247-260.
[49] Bourkoula A,Paravatou-Petsotas M,Papadopoulos A,et al.Synthe-sis and characterization of Rhenium and technetium-99m tricar-bonyl complexes bearing the 4-[3-bromophenyl] quinazoline moi-ety as a biomarker for EGFR-TK imaging[J].Eur J Med Chem,2009,44(10):4021-4027.
[50] Hirata M,Kanai Y,Naka S,et al.Evaluation fo radioiodinated quinazoline derivative as a new ligand for EGF receptor tyrosine ki-nase activity using SPECT[J].Ann Nucl Med,2011,25(2):117-124.
[51] Hirata M,Kanai Y,Naka S,et al.Synthesis and evaluation of ra-dioiodinated phenoxyquinazoline and benzylaminoquinazoline derivatives as new EGF receptor tyrosine kinase imaging ligands fortumor diagnosis using SPECT[J].Ann Nucl Med,2012,26(5):381-389.
[52] Hirata M,Kanai Y,Naka S,et al.A useful EGFR-TK ligand for tu-mor diagnosis with SPECT:development of radioiodinated 6-(3-morpholinopropoxy)-7-ethoxy-4-(3’-iodophenoxy) quinazoline[J].Ann Nucl Med,2013,27(5):431-443.
[53] Cai W,Niu G,Chen X.Multimodality imaging of the HER-kinase axis in cancer[J].Eur J Nucl Med Mol Imaging,2008,35(1):186-208.

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备注/Memo

备注/Memo:
收稿日期:2014-11-10。
通讯作者:唐明灯,Email:tmd0603@126.com
更新日期/Last Update: 1900-01-01