164
Views
1
CrossRef citations to date
0
Altmetric
Reviews

Targeting the EGF receptor ectodomain in the context of cancer

, &
Pages 1347-1361 | Published online: 22 Sep 2009

Bibliography

  • Downward J, Yarden Y, Mayes E, Close similarity of epidermal growth factor receptor and v-erb-B oncogene protein sequences. Nature 1984;307:521-7
  • Frykberg L, Palmieri S, Beug H, Transforming capacities of avian erythroblastosis virus mutants deleted in the erbA or erbB oncogenes. Cell 1983;32:227-38
  • Masui H, Kawamoto T, Sato JD, Growth inhibition of human tumor cells in athymic mice by anti-epidermal growth factor receptor monoclonal antibodies. Cancer Res 1984;44:1002-7
  • Gill GN, Bertics PJ, Santon JB. Epidermal growth factor and its receptor. Mol Cell Endocrinol 1987;51:169-86
  • Thompson DM, Gill GN. The EGF receptor: structure, regulation and potential role in malignancy. Cancer Surv 1985;4:767-88
  • Ciardiello F, Caputo R, Troiani T, Antisense oligonucleotides targeting the epidermal growth factor receptor inhibit proliferation, induce apoptosis, and cooperate with cytotoxic drugs in human cancer cell lines. Int J Cancer 2001;93:172-8
  • Jannot CB, Beerli RR, Mason S, Intracellular expression of a single-chain antibody directed to the EGFR leads to growth inhibition of tumor cells. Oncogene 1996;13:275-82
  • Yamazaki H, Kijima H, Ohnishi Y, Inhibition of tumor growth by ribozyme-mediated suppression of aberrant epidermal growth factor receptor gene expression. J Natl Cancer Inst 1998;90:581-7
  • Cohen S. Origins of growth factors: NGF and EGF. J Biol Chem 2008;283:33793-7
  • Ogiso H, Ishitani R, Nureki O, Crystal structure of the complex of human epidermal growth factor and receptor extracellular domains. Cell 2002;110:775-87
  • Harris RC, Chung E, Coffey RJ. EGF receptor ligands. Exp Cell Res 2003;284:2-13
  • Burgess AW, Cho H-S, Eigenbrot C, An open-and-shut case? Recent insights into the activation of EGF/ErbB receptors. Mol Cell 2003;12:541-52
  • Cho HS, Mason K, Ramyar KX, Structure of the extracellular region of HER2 alone and in complex with the Herceptin Fab. Nature 2003;421:756-60
  • Zhang X, Gureasko J, Shen K, An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell 2006;125:1137-49
  • Yarden Y, Sliwkowski MX. Untangling the ErbB signalling network. Nat Rev Mol Cell Biol 2001;2:127-37
  • Sclabas GM, Fujioka S, Schmidt C, Restoring apoptosis in pancreatic cancer cells by targeting the nuclear factor-κB signaling pathway with the anti-epidermal growth factor antibody IMC-C225. J Gastrointest Surg 2003;7:37-43
  • Singh S, Shi Q, Bailey ST, Nuclear factor-κB activation: a molecular therapeutic target for estrogen receptor-negative and epidermal growth factor receptor family receptor-positive human breast cancer. Mol Cancer Ther 2007;6:1973-82
  • Lo HW, Hung MC. Nuclear EGFR signalling network in cancers: linking EGFR pathway to cell cycle progression, nitric oxide pathway and patient survival. Br J Cancer 2006;94:184-8
  • Haj FG, Markova B, Klaman LD, Regulation of receptor tyrosine kinase signaling by protein tyrosine phosphatase-1B. J Biol Chem 2003;278:739-44
  • Keilhack H, Tenev T, Nyakatura E, Phosphotyrosine 1173 mediates binding of the protein-tyrosine phosphatase SHP-1 to the epidermal growth factor receptor and attenuation of receptor signaling. J Biol Chem 1998;273:24839-46
  • Kario E, Marmor MD, Adamsky K, Suppressors of cytokine signaling 4 and 5 regulate epidermal growth factor receptor signaling. J Biol Chem 2005;280:7038-48
  • Nicholson SE, Metcalf D, Sprigg NS, Suppressor of cytokine signaling (SOCS)-5 is a potential negative regulator of epidermal growth factor signaling. Proc Natl Acad Sci USA 2005;102:2328-33
  • Gavin AC, Nebreda AR. A MAP kinase docking site is required for phosphorylation and activation of p90rsk/MAPKAP kinase-1. Curr Biol 1999;9:281-4
  • Murphy LO, Smith S, Chen R-H, Molecular interpretation of ERK signal duration by immediate early gene products. Nat Cell Biol 2002;4:556-64
  • Perry JE, Grossmann ME, Tindall DJ. Epidermal growth factor induces cyclin D1 in a human prostate cancer cell line. Prostate 1998;35:117-24
  • Liang J, Zubovitz J, Petrocelli T, PKB/Akt phosphorylates p27, impairs nuclear import of p27 and opposes p27-mediated G1 arrest. Nat Med 2002;8:1153-60
  • Shin I, Yakes FM, Rojo F, PKB/Akt mediates cell-cycle progression by phosphorylation of p27Kip1 at threonine 157 and modulation of its cellular localization. Nat Med 2002;8:1145-52
  • Viglietto G, Motti ML, Bruni P, Cytoplasmic relocalization and inhibition of the cyclin-dependent kinase inhibitor p27Kip1 by PKB/Akt-mediated phosphorylation in breast cancer. Nat Med 2002;8:1136-44
  • Cantley LC. The phosphoinositide 3-kinase pathway. Science 2002;296:1655-7
  • Cardone MH, Roy N, Stennicke HR, Regulation of cell death protease caspase-9 by phosphorylation. Science 1998;282:1318-21
  • Franke TF, Hornik CP, Segev L, PI3K/Akt and apoptosis: size matters. Oncogene 2003;22:8983-98
  • Grandis JR, Drenning SD, Zeng Q, Constitutive activation of Stat3 signaling abrogates apoptosis in squamous cell carcinogenesis in vivo. Proc Natl Acad Sci USA 2000;97:4227-32
  • Azuma M, Tamatani T, Fukui K, Identification of EGF as an angiogenic factor present in conditioned medium from human salivary gland adenocarcinoma cell clones with varying degrees of metastatic potential. Cancer Lett 1994;84:189-98
  • Goldman CK, Kim J, Wong WL, Epidermal growth factor stimulates vascular endothelial growth factor production by human malignant glioma cells: a model of glioblastoma multiforme pathophysiology. Mol Biol Cell 1993;4:121-33
  • Schreiber AB, Winkler ME, Derynck R. Transforming growth factor-alpha: a more potent angiogenic mediator than epidermal growth factor. Science 1986;232:1250-3
  • Wang T, Niu G, Kortylewski M, Regulation of the innate and adaptive immune responses by Stat-3 signaling in tumor cells. Nat Med 2004;10:48-54
  • O-charoenrat P, Rhys-Evans P, Court WJ, Differential modulation of proliferation, matrix metalloproteinase expression and invasion of human head and neck squamous carcinoma cells by c-erbB ligands. Clin Exp Metastasis 1999;17:631-9
  • Rogers SJ, Harrington KJ, Rhys-Evans P, Biological significance of c-erbB family oncogenes in head and neck cancer. Cancer Metastasis Rev 2005;24:47-69
  • Zandi R, Larsen AB, Andersen P, Mechanisms for oncogenic activation of the epidermal growth factor receptor. Cell Signal 2007;19:2013-23
  • Croce CM. Oncogenes and cancer. N Engl J Med 2008;358:502-11
  • Ford AC, Grandis JR. Targeting epidermal growth factor receptor in head and neck cancer. Head Neck 2003;25:67-73
  • Franklin WA, Veve R, Hirsch FR, Epidermal growth factor receptor family in lung cancer and premalignancy. Semin Oncol 2002;29:3-14
  • Janmaat ML, Giaccone G. The epidermal growth factor receptor pathway and its inhibition as anticancer therapy. Drugs Today (Barc) 2003;39(Suppl C):61-80
  • Kim H, Muller WJ. The role of the epidermal growth factor receptor family in mammary tumorigenesis and metastasis. Exp Cell Res 1999;253:78-87
  • Maihle NJ, Baron AT, Barrette BA, EGF/ErbB receptor family in ovarian cancer. Cancer Treat Res 2002;107:247-58
  • Moch H, Sauter G, Buchholz N, Epidermal growth factor receptor expression is associated with rapid tumor cell proliferation in renal cell carcinoma. Hum Pathol 1997;28:1255-9
  • Nicholson RI, Gee JM, Harper ME. EGFR and cancer prognosis. Eur J Cancer 2001;37(Suppl 4):S9-15
  • Salomon DS, Brandt R, Ciardiello F, Epidermal growth factor-related peptides and their receptors in human malignancies. Crit Rev Oncol Hematol 1995;19:183-232
  • Uberall I, Kolar Z, Trojanec R, The status and role of ErbB receptors in human cancer. Exp Mol Pathol 2008;84:79-89
  • Witton CJ, Reeves JR, Going JJ, Expression of the HER1-4 family of receptor tyrosine kinases in breast cancer. J Pathol 2003;200:290-7
  • Xiong HQ, Abbruzzese JL. Epidermal growth factor receptor-targeted therapy for pancreatic cancer. Semin Oncol 2002;29:31-7
  • Peschard P, Park M. Escape from Cbl-mediated downregulation: a recurrent theme for oncogenic deregulation of receptor tyrosine kinases. Cancer Cell 2003;3:519-23
  • Waterman H, Katz M, Rubin C, A mutant EGF-receptor defective in ubiquitylation and endocytosis unveils a role for Grb2 in negative signaling. EMBO J 2002;21:303-13
  • Thien CB, Langdon WY. EGF receptor binding and transformation by v-cbl is ablated by the introduction of a loss-of-function mutation from the Caenorhabditis elegans sli-1 gene. Oncogene 1997;14:2239-49
  • Worthylake R, Opresko LK, Wiley HS. ErbB-2 amplification inhibits down-regulation and induces constitutive activation of both ErbB-2 and epidermal growth factor receptors. J Biol Chem 1999;274:8865-74
  • Lenferink AE, Pinkas-Kramarski R, van de Poll ML, Differential endocytic routing of homo- and hetero-dimeric ErbB tyrosine kinases confers signaling superiority to receptor heterodimers. EMBO J 1998;17:3385-97
  • Daub H, Wallasch C, Lankenau A, Signal characteristics of G protein-transactivated EGF receptor. EMBO J 1997;16:7032-44
  • Gschwind A, Prenzel N, Ullrich A. Lysophosphatidic acid-induced squamous cell carcinoma cell proliferation and motility involves epidermal growth factor receptor signal transactivation. Cancer Res 2002;62:6329-36
  • Hart S, Fischer OM, Prenzel N, GPCR-induced migration of breast carcinoma cells depends on both EGFR signal transactivation and EGFR-independent pathways. Biol Chem 2005;386:845-55
  • Lui VWY, Thomas SM, Zhang Q, Mitogenic effects of gastrin-releasing peptide in head and neck squamous cancer cells are mediated by activation of the epidermal growth factor receptor. Oncogene 2003;22:6183-93
  • Thomas SM, Grandis JR, Wentzel AL, Gastrin-releasing peptide receptor mediates activation of the epidermal growth factor receptor in lung cancer cells. Neoplasia 2005;7:426-31
  • Gan HK, Kaye AH, Luwor RB. The EGFRvIII variant in glioblastoma multiforme. J Clin Neurosci 2009;16:748-54
  • Kuan CT, Wikstrand CJ, Bigner DD. EGF mutant receptor vIII as a molecular target in cancer therapy. Endocr Relat Cancer 2001;8:83-96
  • Lammering G, Hewit TH, Valerie K, EGFRvIII-mediated radioresistance through a strong cytoprotective response. Oncogene 2003;22:5545-53
  • Lynch TJ, Bell DW, Sordella R, Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 2004;350:2129-39
  • Paez JG, Janne PA, Lee JC, EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004;304:1497-500
  • Pao W, Miller V, Zakowski M, EGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci USA 2004;101:13306-11
  • Bose R, Zhang X. The ErbB kinase domain: structural perspectives into kinase activation and inhibition. Exp Cell Res 2008;315:649-58
  • Sato JD, Kawamoto T, Le AD, Biological effects in vitro of monoclonal antibodies to human epidermal growth factor receptors. Mol Biol Med 1983;1:511-29
  • Gill GN, Kawamoto T, Cochet C, Monoclonal anti-epidermal growth factor receptor antibodies which are inhibitors of epidermal growth factor binding and antagonists of epidermal growth factor binding and antagonists of epidermal growth factor-stimulated tyrosine protein kinase activity. J Biol Chem 1984;259:7755-60
  • Kawamoto T, Sato JD, Le A, Growth stimulation of A431 cells by epidermal growth factor: identification of high-affinity receptors for epidermal growth factor by an anti-receptor monoclonal antibody. Proc Natl Acad Sci USA 1983;80:1337-41
  • Haigler H, Ash JF, Singer SJ, Visualization by fluorescence of the binding and internalization of epidermal growth factor in human carcinoma cells A-431. Proc Natl Acad Sci USA 1978;75:3317-21
  • Aerts HJWL, Dubois L, Hackeng TM, Development and evaluation of a cetuximab-based imaging probe to target EGFR and EGFRvIII. Radiother Oncol 2007;83:326-32
  • Kang X, Patel D, Shi J, Anti-EGFR monoclonal antibody Cetuximab binds the EGFR variant III receptor and internalizes phosphorylated receptor on the cell surface. Eur J Cancer 2002;38(Suppl 7):S149
  • Li S, Schmitz KR, Jeffrey PD, Structural basis for inhibition of the epidermal growth factor receptor by cetuximab. Cancer Cell 2005;7:301-11
  • Fan Z, Masui H, Altas I, Blockade of epidermal growth factor receptor function by bivalent and monovalent fragments of 225 anti-epidermal growth factor receptor monoclonal antibodies. Cancer Res 1993;53:4322-8
  • Fan Z, Lu Y, Wu X, Antibody-induced epidermal growth factor receptor dimerization mediates inhibition of autocrine proliferation of A431 squamous carcinoma cells. J Biol Chem 1994;269:27595-602
  • Jaramillo ML, Leon Z, Grothe S, Effect of the anti-receptor ligand-blocking 225 monoclonal antibody on EGF receptor endocytosis and sorting. Exp Cell Res 2006;312:2778-90
  • Goldstein NI, Prewett M, Zuklys K, Biological efficacy of a chimeric antibody to the epidermal growth factor receptor in a human tumor xenograft model. Clin Cancer Res 1995;1:1311-8
  • Eller JL, Longo SL, Hicklin DJ, Activity of anti-epidermal growth factor receptor monoclonal antibody C225 against glioblastoma multiforme. Neurosurgery 2002;51:1005-13; discussion 13-14
  • Huang SM, Bock JM, Harari PM. Epidermal growth factor receptor blockade with C225 modulates proliferation, apoptosis, and radiosensitivity in squamous cell carcinomas of the head and neck. Cancer Res 1999;59:1935-40
  • Jung YD, Mansfield PF, Akagi M, Effects of combination anti-vascular endothelial growth factor receptor and anti-epidermal growth factor receptor therapies on the growth of gastric cancer in a nude mouse model. Eur J Cancer 2002;38:1133-40
  • Nahta R, Hortobagyi GN, Esteva FJ. Growth factor receptors in breast cancer: potential for therapeutic intervention. Oncologist 2003;8:5-17
  • Overholser JP, Prewett MC, Hooper AT, Epidermal growth factor receptor blockade by antibody IMC-C225 inhibits growth of a human pancreatic carcinoma xenograft in nude mice. Cancer 2000;89:74-82
  • Prewett M, Rockwell P, Rockwell RF, The biologic effects of C225, a chimeric monoclonal antibody to the EGFR, on human prostate carcinoma. J Immunother Emphasis Tumor Immunol 1996;19:419-27
  • Prewett M, Rothman M, Waksal H, Mouse-human chimeric anti-epidermal growth factor receptor antibody C225 inhibits the growth of human renal cell carcinoma xenografts in nude mice. Clin Cancer Res 1998;4:2957-66
  • Prewett MC, Hooper AT, Bassi R, Enhanced antitumor activity of anti-epidermal growth factor receptor monoclonal antibody IMC-C225 in combination with irinotecan (CPT-11) against human colorectal tumor xenografts. Clin Cancer Res 2002;8:994-1003
  • Hynes NE, Lane HA. ERBB receptors and cancer: the complexity of targeted inhibitors. Nat Rev Cancer 2005;5:341-54
  • Petit AM, Rak J, Hung MC, Neutralizing antibodies against epidermal growth factor and ErbB-2/neu receptor tyrosine kinases down-regulate vascular endothelial growth factor production by tumor cells in vitro and in vivo: angiogenic implications for signal transduction therapy. Am J Pathol 1997;151:1523-30
  • Peng D, Fan Z, Lu Y, Anti-epidermal growth factor receptor monoclonal antibody 225 up-regulates p27KIP1 and induces G1 arrest in prostatic cancer cell line DU145. Cancer Res 1996;56:3666-9
  • Tortora G, Caputo R, Pomatico G, Cooperative inhibitory effect of novel mixed backbone oligonucleotide targeting protein kinase A in combination with docetaxel and anti-epidermal growth factor-receptor antibody on human breast cancer cell growth. Clin Cancer Res 1999;5:875-81
  • Perrotte P, Matsumoto T, Inoue K, Anti-epidermal growth factor receptor antibody C225 inhibits angiogenesis in human transitional cell carcinoma growing orthotopically in nude mice. Clin Cancer Res 1999;5:257-65
  • Kurai J, Chikumi H, Hashimoto K, Antibody-dependent cellular cytotoxicity mediated by cetuximab against lung cancer cell lines. Clin Cancer Res 2007;13:1552-61
  • Kimura H, Sakai K, Arao T, Antibody-dependent cellular cytotoxicity of cetuximab against tumor cells with wild-type or mutant epidermal growth factor receptor. Cancer Sci 2007;98:1275-80
  • Clynes RA, Towers TL, Presta LG, Inhibitory Fc receptors modulate in vivo cytoxicity against tumor targets. Nat Med 2000;6:443-6
  • Beano A, Signorino E, Evangelista A, Correlation between NK function and response to trastuzumab in metastatic breast cancer patients. J Transl Med 2008;6:25. Published online 16 May 2008, doi:10.1186/1479-5876-6-25
  • Musolino A, Naldi N, Bortesi B, Immunoglobulin G fragment C receptor polymorphisms and clinical efficacy of trastuzumab-based therapy in patients with HER-2/neu-positive metastatic breast cancer. J Clin Oncol 2008;26:1789-96
  • Cunningham D, Humblet Y, Siena S, Cetuximab monotherapy and cetuximab plus irinotecan in irinotecan-refractory metastatic colorectal cancer. N Engl J Med 2004;351:337-45
  • Lenz H-J, Van Cutsem E, Khambata-Ford S, Multicenter Phase II and translational study of cetuximab in metastatic colorectal carcinoma refractory to irinotecan, oxaliplatin, and fluoropyrimidines. J Clin Oncol 2006;24:4914-21
  • Saltz LB, Meropol NJ, Loehrer PJ Sr, Phase II trial of cetuximab in patients with refractory colorectal cancer that expresses the epidermal growth factor receptor. J Clin Oncol 2004;22:1201-8
  • Van Cutsem E, Nowacki M, Lang I, Randomized phase III study of irinotecan and 5-FU/FA with or without cetuximab in the first-line treatment of patients with metastatic colorectal cancer (mCRC): the CRYSTAL trial. J Clin Oncol 2007;25 :abstract 4000
  • Vermorken JB, Trigo J, Hitt R, Open-label, uncontrolled, multicenter Phase II study to evaluate the efficacy and toxicity of cetuximab as a single agent in patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck who failed to respond to platinum-based therapy. J Clin Oncol 2007;25:2171-7
  • Shin DM, Donato NJ, Perez-Soler R, Epidermal growth factor receptor-targeted therapy with C225 and cisplatin in patients with head and neck cancer. Clin Cancer Res 2001;7:1204-13
  • Peipp M, Dechant M, Valerius T. Effector mechanisms of therapeutic antibodies against ErbB receptors. Curr Opin Immunol 2008;20:436-43
  • Yang XD, Jia XC, Corvalan JR, Eradication of established tumors by a fully human monoclonal antibody to the epidermal growth factor receptor without concomitant chemotherapy. Cancer Res 1999;59:1236-43
  • Carteni G, Fiorentino R, Vecchione L, Panitumumab a novel drug in cancer treatment. Ann Oncol 2007;18(Suppl 6):vi16-21
  • Hecht JR, Patnaik A, Berlin J, Panitumumab monotherapy in patients with previously treated metastatic colorectal cancer. Cancer 2007;110:980-8
  • Mitchell EP, Hecht JR, Baranda J. Panitumumab activity in metastatic colorectal cancer (mCRC) patients (pts) with low or negative tumor epidermal growth factor receptor (EGFr) levels: an updated analysis. J Clin Oncol 2007;25:4082
  • Van Cutsem E, Peeters M, Siena S, Open-label Phase III trial of panitumumab plus best supportive care compared with best supportive care alone in patients with chemotherapy-refractory metastatic colorectal cancer. J Clin Oncol 2007;25:1658-64
  • Crombet Ramos T, Figueredo J, Catala M, Treatment of high-grade glioma patients with the humanized anti-epidermal growth factor receptor (EGFR) antibody h-R3: report from a Phase I/II trial. Cancer Biol Ther 2006;5:375-9
  • Rivera F, Vega-Villegas ME, Lopez-Brea MF, Current situation of panitumumab, matuzumab, nimotuzumab and zalutumumab. Acta Oncol 2008;47:9-19
  • Schmiedel J, Blaukat A, Li S, Matuzumab binding to EGFR prevents the conformational rearrangement required for dimerization. Cancer Cell 2008;13:365-73
  • Rodeck U, Herlyn M, Herlyn D, Tumor growth modulation by a monoclonal antibody to the epidermal growth factor receptor: immunologically mediated and effector cell-independent effects. Cancer Res 1987;47:3692-6
  • Seiden MV, Burris HA, Matulonis U, A phase II trial of EMD72000 (matuzumab), a humanized anti-EGFR monoclonal antibody, in patients with platinum-resistant ovarian and primary peritoneal malignancies. Gynecol Oncol 2007;104:727-31
  • Lammerts van Bueren JJ, Bleeker WK, Brannstrom A, The antibody zalutumumab inhibits epidermal growth factor receptor signaling by limiting intra- and intermolecular flexibility. Proc Natl Acad Sci USA 2008;105:6109-14
  • Lu D, Zhang H, Ludwig D, Simultaneous blockade of both the epidermal growth factor receptor and the insulin-like growth factor receptor signaling pathways in cancer cells with a fully human recombinant bispecific antibody. J Biol Chem 2004;279:2856-65
  • Kuenen B, Witteveen E, Ruijter R, A phase I study of IMC-11F8, a fully human anti-epidermal growth factor receptor (EGFR) IgG1 monoclonal antibody in patients with solid tumors. Interim results. J Clin Oncol 2006;24:abstract 3024
  • Li S, Kussie P, Ferguson KM. Structural basis for EGF receptor inhibition by the therapeutic antibody IMC-11F8. Structure 2008;16:216-27
  • Luwor RB, Johns TG, Murone C, Monoclonal antibody 806 inhibits the growth of tumor xenografts expressing either the de2-7 or amplified epidermal growth factor receptor (EGFR) but not wild-type EGFR. Cancer Res 2001;61:5355-61
  • Mishima K, Johns TG, Luwor RB, Growth suppression of intracranial xenografted glioblastomas overexpressing mutant epidermal growth factor receptors by systemic administration of monoclonal antibody (mAb) 806, a novel monoclonal antibody directed to the receptor. Cancer Res 2001;61:5349-54
  • Johns TG, Mellman I, Cartwright GA, The antitumor monoclonal antibody 806 recognizes a high-mannose form of the EGF receptor that reaches the cell surface when cells over-express the receptor. FASEB J 2005;19:780-2
  • Scott AM, Lee F-T, Tebbutt N, A phase I clinical trial with monoclonal antibody ch806 targeting transitional state and mutant epidermal growth factor receptors. Proc Natl Acad Sci USA 2007;104:4071-6
  • Beerli RR, Wels W, Hynes NE. Autocrine inhibition of the epidermal growth factor receptor by intracellular expression of a single-chain antibody. Biochem Biophys Res Commun 1994;204:666-72
  • Beerli RR, Wels W, Hynes NE. Inhibition of signaling from Type 1 receptor tyrosine kinases via intracellular expression of single-chain antibodies. Breast Cancer Res Treat 1996;38:11-7
  • Suzuki M, Takayanagi A, Shimizu N. Targeted gene delivery using humanized single-chain antibody with negatively charged oligopeptide tail. Cancer Sci 2004;95:424-9
  • Asano R, Sone Y, Ikoma K, Preferential heterodimerization of a bispecific diabody based on a humanized anti-EGFR antibody 528. Protein Eng Des Sel 2008;21:597-603
  • Bruell D, Bruns CJ, Yezhelyev M, Recombinant anti-EGFR immunotoxin 425(scFv)-ETA′ demonstrates anti-tumor activity against disseminated human pancreatic cancer in nude mice. Int J Mol Med 2005;15:305-13
  • Schmidt M, Vakalopoulou E, Schneider DW, Construction and functional characterization of scFv(14E1)-ETA – a novel, highly potent antibody-toxin specific for the EGF receptor. Br J Cancer 1997;75:1575-84
  • Zhao X, Dai W, Cao L, Selection and characterization of an internalizing epidermal-growth-factor-receptor antibody. Biotechnol Appl Biochem 2007;46:27-33
  • Kuan CT, Reist CJ, Foulon CF, 125I-labeled anti-epidermal growth factor receptor-vIII single-chain Fv exhibits specific and high-level targeting of glioma xenografts. Clin Cancer Res 1999;5:1539-49
  • Nakayashiki N, Yoshikawa K, Nakamura K, Production of a single-chain variable fragment antibody recognizing type III mutant epidermal growth factor receptor. Jpn J Cancer Res 2000;91:1035-43
  • Mamot C, Drummond DC, Greiser U, Epidermal growth factor receptor (EGFR)-targeted immunoliposomes mediate specific and efficient drug delivery to EGFR- and EGFRvIII-overexpressing tumor cells. Cancer Res 2003;63:3154-61
  • Wels W, Beerli R, Hellmann P, EGF receptor and p185erbB-2-specific single-chain antibody toxins differ in their cell-killing activity on tumor cells expressing both receptor proteins. Int J Cancer 1995;60:137-44
  • Azemar M, Schmidt M, Arlt F, Recombinant antibody toxins specific for ErbB2 and EGF receptor inhibit the in vitro growth of human head and neck cancer cells and cause rapid tumor regression in vivo. Int J Cancer 2000;86:269-75
  • Bremer E, Samplonius DF, van Genne L, Simultaneous inhibition of epidermal growth factor receptor (EGFR) signaling and enhanced activation of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) receptor-mediated apoptosis induction by an scFv:sTRAIL fusion protein with specif. J Biol Chem 2005;280:10025-33
  • Dalken B, Giesubel U, Knauer SK, Targeted induction of apoptosis by chimeric granzyme B fusion proteins carrying antibody and growth factor domains for cell recognition. Cell Death Differ 2006;13:576-85
  • Pirker R, Pereira JR, Szczesna A, Cetuximab plus chemotherapy in patients with advanced non-small-cell lung cancer (FLEX): an open-label randomised phase III trial. Lancet 2009;373:1525-31
  • Jansman FGA, Postma MJ, Brouwers JRBJ. Cost considerations in the treatment of colorectal cancer. Pharmacoeconomics 2007;25:537-62
  • Bevacizumab and cetuximab for the treatment of metastatic colorectal cancer. NICE technology appraisal guidance 118, London, UK: National Institute for Health and Clinical Excellence, 2007. Available from: http://www.nice.org.uk/nicemedia/pdf/TA118Guidance.pdf [Last accessed 30 August 2009]
  • Cetuximab for the treatment of metastatic colorectal cancer followinf failure of oxaliplatin-containing chemotherapy 9terminated appraisal. NICE technology appraisal 150, London, UK: National Institute for Health and Clinical Excellence, 2008. Available from: http://www.nice.org.uk/nicemedia/pdf/TA150Advice.pdf [Last accessed 30 August 2009]
  • Spano JP, Milano G, Vignot S, Potential predictive markers of response to EGFR-targeted therapies in colorectal cancer. Crit Rev Oncol Hematol 2008;66:21-30
  • Chung KY, Shia J, Kemeny NE, Cetuximab shows activity in colorectal cancer patients with tumors that do not express the epidermal growth factor receptor by immunohistochemistry. J Clin Oncol 2005;23:1803-10
  • Normanno N, De Luca A, Bianco C, Epidermal growth factor receptor (EGFR) signaling in cancer. Gene 2006;366:2-16
  • Personeni N, Hendlisz A, Gallez J, Correlation between the response to cetuximab alone or in combination with irinotecan and the activated/phosphorylated epidermal growth factor receptor in metastatic colorectal cancer. Semin Oncol 2005;32:S59-62
  • Sergina NV, Rausch M, Wang D, Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3. Nature 2007;445:437-41
  • Weihua Z, Tsan R, Huang W-C, Survival of cancer cells is maintained by EGFR independent of its kinase activity. Cancer Cell 2008;13:385-93
  • Wu X, Fan Z, Masui H, Apoptosis induced by an anti-epidermal growth factor receptor monoclonal antibody in a human colorectal carcinoma cell line and its delay by insulin. J Clin Invest 1995;95:1897-905
  • Bianco R, Garofalo S, Rosa R, Inhibition of mTOR pathway by everolimus cooperates with EGFR inhibitors in human tumours sensitive and resistant to anti-EGFR drugs. Br J Cancer 2008;98:923-30
  • Kelly K, Huang C. Biological agents in non-small cell lung cancer: a review of recent advances and clinical results with a focus on epidermal growth factor receptor and vascular endothelial growth factor. J Thorac Oncol 2008;3:664-73
  • Dei Tos AP, Ellis I. Assessing epidermal growth factor receptor expression in tumours: what is the value of current test methods? Eur J Cancer 2005;41:1383-92
  • Penault-Llorca F, Cayre A, Arnould L, Is there an immunohistochemical technique definitively valid in epidermal growth factor receptor assessment? Oncol Rep 2006;16:1173-9
  • Van de Wiele C, Revets H, Mertens N. Radioimmunoimaging. Advances and prospects. Q J Nucl Med Mol Imaging 2004;48:317-25
  • Muyldermans S. Single domain camel antibodies: current status. J Biotechnol 2001;74:277-302
  • Yokota T, Milenic DE, Whitlow M, Rapid tumor penetration of a single-chain Fv and comparison with other immunoglobulin forms. Cancer Res 1992;52:3402-8
  • Mallender WD, Carrero J, Voss EW Jr. Comparative properties of the single chain antibody and Fv derivatives of mAb 4-4-20. Relationship between interdomain interactions and the high affinity for fluorescein ligand. J Biol Chem 1996;271:5338-46
  • Ward ES, Gussow D, Griffiths AD, Binding activities of a repertoire of single immunoglobulin variable domains secreted from Escherichia coli. Nature 1989;341:544-6
  • Borrebaeck CA, Malmborg AC, Furebring C, Kinetic analysis of recombinant antibody-antigen interactions: relation between structural domains and antigen binding. Biotechnology (NY) 1992;10:697-8
  • Hamers-Casterman C, Atarhouch T, Muyldermans S, Naturally occurring antibodies devoid of light chains. Nature 1993;363:446-8
  • Padlan EA. Anatomy of the antibody molecule. Mol Immunol 1994;31:169-217
  • Arbabi Ghahroudi M, Desmyter A, Wyns L, Selection and identification of single domain antibody fragments from camel heavy-chain antibodies. FEBS Lett 1997;414:521-6
  • Davies J, Riechmann L. Single antibody domains as small recognition units: design and in vitro antigen selection of camelized, human VH domains with improved protein stability. Protein Eng 1996;9:531-7
  • Davies J, Riechmann L. ‘Camelising’ human antibody fragments: NMR studies on VH domains. FEBS Lett 1994;339:285-90
  • Cortez-Retamozo V, Lauwereys M, Hassanzadeh Gh G, Efficient tumor targeting by single-domain antibody fragments of camels. Int J Cancer 2002;98:456-62
  • Coppieters K, Dreier T, Silence K, Formatted anti-tumor necrosis factor alpha VHH proteins derived from camelids show superior potency and targeting to inflamed joints in a murine model of collagen-induced arthritis. Arthritis Rheum 2006;54:1856-66
  • Baral TN, Magez S, Stijlemans B, Experimental therapy of African trypanosomiasis with a nanobody-conjugated human trypanolytic factor. Nat Med 2006;12:580-4
  • Lafaye P, Achour I, England P, Single-domain antibodies recognize selectively small oligomeric forms of amyloid beta, prevent Abeta-induced neurotoxicity and inhibit fibril formation. Mol Immunol 2009;46:695-704
  • Roovers RC, Laeremans T, Huang L, Efficient inhibition of EGFR signaling and of tumour growth by antagonistic anti-EFGR Nanobodies. Cancer Immunol Immunother 2007;56:303-17
  • Tijink BM, Laeremans T, Budde M, Improved tumor targeting of anti-epidermal growth factor receptor Nanobodies through albumin binding: taking advantage of modular Nanobody technology. Mol Cancer Ther 2008;7:2288-97
  • Gainkam LOT, Huang L, Caveliers V, Comparison of the biodistribution and tumor targeting of two 99mTc-labeled anti-EGFR nanobodies in mice, using pinhole SPECT/micro-CT. J Nucl Med 2008;49:788-95
  • Huang L, Gainkam LOT, Caveliers V, SPECT imaging with 99mTc-labeled EGFR-specific nanobody for in vivo monitoring of EGFR expression. Mol Imaging Biol 2008;10:167-75
  • Friedman M, Nordberg E, Höidén-Guthenberg I, Phage display selection of Affibody molecules with specific binding to the extracellular domain of the epidermal growth factor receptor. Protein Eng Des Sel 2007;20:189-99
  • Tolmachev V, Orlova A, Nilsson FY, Affibody molecules: potential for in vivo imaging of molecular targets for cancer therapy. Expert Opin Biol Ther 2007;7:555-68
  • Steffen A-C, Orlova A, Wikman M, Affibody-mediated tumour targeting of HER-2 expressing xenografts in mice. Eur J Nucl Med Mol Imaging 2006;33:631-8
  • Orlova A, Tolmachev V, Pehrson R, Synthetic affibody molecules: a novel class of affinity ligands for molecular imaging of HER2-expressing malignant tumors. Cancer Res 2007;67:2178-86
  • Hoskin DW, Ramamoorthy A. Studies on anticancer activities of antimicrobial peptides. Biochim Biophys Acta 2008;1778:357-75
  • Webb SED, Roberts SK, Needham SR, Single-molecule imaging and fluorescence lifetime imaging microscopy show different structures for high- and low-affinity epidermal growth factor receptors in A431 cells. Biophys J 2008;94:803-19
  • Bruggemann M, Smith JA, Osborn MJ, Heavy-chain-only antibody expression and B-cell development in the mouse. Crit Rev Immunol 2006;26:377-90
  • Janssens R, Dekker S, Hendriks RW, Generation of heavy-chain-only antibodies in mice. Proc Natl Acad Sci USA 2006;103:15130-5
  • Vincke C, Loris R, Saerens D, General strategy to humanize a camelid single-domain antibody and identification of a universal humanized nanobody scaffold. J Biol Chem 2009;284:3273-84

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.