Molecular biology of epidermal growth factor receptor inhibition for cancer therapy

Expert Opinion on Biological Therapy

Volumn 6, Issue 6, 2006, Pages 605-617

  Oliveira, Sabrina ^a   Van Bergen En Henegouwen, Paul M P ^b   Storm, Gert ^a   Schiffelers, Raymond M ^a  

^a UTRECHT UNIVERSITY   (Netherlands)

^b UTRECHT UNIVERSITY   (Netherlands)

Author keywords

Cancer therapy; Combined strategies; EGFR inhibition; Targeting strategies

Indexed keywords

AMPHIREGULIN; BETACELLULIN; CETUXIMAB; CL 1033; CP 358 774; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR 2; EPIDERMAL GROWTH FACTOR RECEPTOR 3; EPIDERMAL GROWTH FACTOR RECEPTOR 4; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; EPIREGULIN; ERLOTINIB; GEFITINIB; HEPARIN BINDING EPIDERMAL GROWTH FACTOR; LAPATINIB; MATUZUMAB; MESSENGER RNA; MONOCLONAL ANTIBODY; PAN ERBB FAMILY TKI; PANITUMUMAB; PROTEIN TYROSINE KINASE; TRANSFORMING GROWTH FACTOR ALPHA; VASCULOTROPIN INHIBITOR;

ANGIOGENESIS; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; CANCER; CANCER INHIBITION; CANCER THERAPY; CELL ADHESION; CELL CYCLE ARREST; CELL FUNCTION; CELL INVASION; CELL MIGRATION; CELL PROLIFERATION; DRUG ACTIVITY; DRUG PROTEIN BINDING; DRUG TARGETING; FOOD AND DRUG ADMINISTRATION; GENE SILENCING; HUMAN; INTRACELLULAR MEMBRANE; LIGAND BINDING; METASTASIS; MOLECULAR BIOLOGY; PROTEIN EXPRESSION; PROTEIN INDUCTION; REVIEW; SIGNAL TRANSDUCTION;

ANIMALS; CELL PROLIFERATION; COMBINED MODALITY THERAPY; HUMANS; MODELS, BIOLOGICAL; NEOPLASM METASTASIS; NEOPLASMS; PROTEIN STRUCTURE, TERTIARY; RECEPTOR, EPIDERMAL GROWTH FACTOR; RNA, MESSENGER; SIGNAL TRANSDUCTION;

EID: 33744788613     PISSN: 14712598     EISSN: None     Source Type: Journal    
DOI: 10.1517/14712598.6.6.605     Document Type: Review

References (80)

1. MENDELSOHN J, BASELGA J: Status of epidermal growth factor receptor antagonists in the biology and treatment of cancer. J. Clin. Oncol. (2003) 21:2787-2799. A thorough review on EGFR mAbs and TKIs.
2. WELLS A: EGF receptor. Int. J. Biochem. Cell. Biol. (1999) 31:637-643.
3. YARDEN Y: The EGFR family and its ligands in human cancer: signalling mechanisms and therapeutic opportunities. Eur. J. Cancer (2001) 37:S3-S8.
4. FERGUSON KM: Active and inactive conformations of the epidermal growth factor receptor. Biochem. Soc. Trans. (2004) 32:742-745. A novel model for EGFR conformation and activation.
5. NAIR P: Epidermal growth factor receptor family and its role in cancer progression. Curr. Sci. (2005) 88:890-898.
6. SIGISMUND S, WOELK T, PURI C et al.: Clathrin-independent endocytosis of ubiquitinated cargos. Proc. Natl. Acad. Sci. USA (2005) 102:2760-2765. Describes concentration dependency for the EGFR endocytosis pathway.
7. DIKIC I: Mechanisms controlling EGF receptor endocytosis and degradation. Biochem. Soc. Trans. (2003) 31:1178-1181.
8. MENDELSOHN J: Targeting the epidermal growth factor receptor for cancer therapy. J. Clin. Oncol. (2002) 20:1S-13S.
9. BASELGA J: Why the epidermal growth factor receptor? The rationale for cancer therapy. Oncologist (2002) 7:2-8.
10. SATO JD, KAWAMOTO T, LE AD, MENDELSOHN J, POLIKOFF J, SATO GH: Biological effects in vitro of monoclonal antibodies to human epidermal growth factor receptors. Mol. Biol. Med. (1983) 1:511-529. One of the first studies with mAbs.
11. KAWAMOTO T, SATO J D, LE A, POLIKOFF J, SATO GH, MENDELSOHN J: 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) 80:1337-1341. One of the first studies with mAbs.
12. GILL GN, KAWAMOTO T, COCHET C et al.: Monoclonal anti-epidermal growth factor receptor antibodies which are inhibitors of epidermal growth factor binding and antagonists of epidermal growth factor-stimulated tyrosine protein kinase activity. J. Biol. Chem. (1984) 259:7755-7760. One of the first studies with mAbs.
13. HUANG SM, HARARI PM: Epidermal growth factor receptor inhibition in cancer therapy: biology, rationale and preliminary clinical results. Invest. New Drugs (1999) 17:259-269.
14. EL-RAYES BF, LORUSSO PM: Targeting the epidermal growth factor receptor. Br. J. Cancer (2004) 91:418-424.
15. LI S, SCHMITZ KR, JEFFREY PD, WILTZIUS JJ, KUSSIE P, FERGUSON KM: Structural basis for inhibition of the epidermal growth factor receptor by cetuximab. Cancer Cell (2005) 7:301-311.
16. CLYNES RA, TOWERS TL, PRESTA LG, RAVETCH JV: Inhibitory Fc receptors modulate in vivo cytoxicity against tumor targets. Nat. Med. (2000) 6:443-446.
17. SPEAKE G, HOLLOWAY B, COSTELLO G: Recent developments related to the EGFR as a target for cancer chemotherapy. Curr. Opin. Pharmacol. (2005) 5:343-349.
18. FRIEZE DA, MCCUNE JS: Current status of cetuximab for the treatment of patients with solid tumors. Ann. Pharmacother. (2006) 40:241-250.
19. HARARI PM: Epidermal growth factor receptor inhibition strategies in oncology. Endocr. Relat. Cancer (2004) 11:689-708.
20. ROWINSKY EK: The ErbB family: targets for therapeutic development against cancer and therapeutic strategies using monoclonal antibodies and tyrosine kinase inhibitors. Annu. Rev. Med. (2004) 55:433-457.
21. AZEMAR M, SCHMIDT M, ARLT F et al.: 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) 86:269-275.
22. HERBST R: Review of epidermal growth factor receptor biology. Int. J. Radiat. Oncol. Biol. Phys. (2004) 59:S21-S26.
23. GIACCONE G, HERBST RS, MANEGOLD C et al.: Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a Phase III trial-INTACT 1. J. Clin. Oncol. (2004) 22:777-784.
24. HERBST RS, GIACCONE G, SCHILLER JH et al.: Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a Phase III trial-INTACT 2. J. Clin. Oncol. (2004) 22:785-794.
25. COMIS RL: The current situation: erlotinib (Tarceva) and gefitinib (Iressa) in non-small cell lung cancer. Oncologist (2005) 10:467-470.
26. CAPUZZO F, FINOCCHIARO G, METRO G et al.: Clinical experience with gefitinib: an update. Crit. Rev. Oncol. Hematol. (2006) 58:31-45.
27. CIARDIELLO F, CAPUTO R, TROIANI T et al.: 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) 93:172-178.
28. YAMAZAKI H, KIJIMA H, OHNISHI Y et al.: Inhibition of tumor growth by ribozyme-mediated suppression of aberrant epidermal growth factor receptor gene expression. J. Natl. Cancer Inst. (1998) 90:581-587.
29. NAGY P, ARNDT-JOVIN DJ, JOVIN TM: Small interfering RNAs suppress the expression of endogenous and GFP-fused epidermal growth factor receptor (ErbB1) and induce apoptosis in ErbB1-overexpressing cells. Exp. Cell. Res. (2003) 285:39-49. The first reported study using siRNA to silence EGFR expression.
30. BEALE G, HOLLINS AJ, BENBOUBETRA M et al.: Gene silencing nucleic acids designed by scanning arrays: anti-EGFR activity of siRNA, ribozyme and DNA enzymes targeting a single hybridization-accessible region using the same delivery system. J. Drug Target. (2003) 11:449-456.
31. KLEIN DE, NAPPI VM, REEVES GT, SHVARTSMAN SY, LEMMON MA: Argos inhibits epidermal growth factor receptor signalling by ligand sequestration. Nature (2004) 430:1040-1044.
32. ZHU JX, GOLDONI S, BIX G et al.: Decorin evokes protracted internalization and degradation of the epidermal growth factor receptor via caveolar endocytosis. J. Biol. Chem. (2005) 280:32468-32479.
33. TESSEMA M, LEHMANN U, KREIPE H: Cell cycle and no end. Virchows Arch. (2004) 444:313-323.
34. MENDELSOHN J: Anti-EGF receptor monoclonal antibodies: biological studies and potential clinical applications. Trans. Am. Clin. Climatol. Assoc. (1988) 100:31-38.
35. WU X, FAN Z, MASUI H, ROSEN N, MENDELSOHN J: 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) 95:1897-1905.
36. WU X, RUBIN M, FAN Z et al.: Involvement of p27KIP1 in G1 arrest mediated by an anti-epidermal growth factor receptor monoclonal antibody. Oncogene (1996) 12:1397-1403.
37. PENG D, FAN Z, LU Y, DEBLASIO T, SCHER H, MENDELSOHN J: Anti-epidermal growth factor receptor monoclonal antibody 225 up-regulates p27KIP1 and induces G1 arrest in prostatic cancer cell line DU145. Cancer Res. (1996) 56:3666-3669.
38. GOLDSTEIN NI, PREWETT M, ZUKLYS K, ROCKWELL P, MENDELSOHN J: Biological efficacy of a chimeric antibody to the epidermal growth factor receptor in a human tumor xenograft model. Clin. Cancer Res. (1995) 1:1311-1318.
39. MOYER JD, BARBACCI EG, IWATA KK et al.: Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. (1997) 57:4838-4848.
40. HUETHER A, HÖPFNER M, SUTTER AP, SCHUPPAN D, SCHERÜBL H: Erlotinib induces cell cycle arrest and apoptosis in hepatocellular cancer cells and enhances chemosensitivity towards cytostatics. J. Hepatol. (2005) 43:661-669.
41. BUSSE D, DOUGHTY RS, RAMSEY TT et al.: Reversible G(1) arrest induced by inhibition of the epidermal growth factor receptor tyrosine kinase requires up-regulation of p27(KIP1) independent of MAPK activity. J. Biol. Chem. (2000) 275:6987-6995.
42. HARA F, AOE M, DOIHARA H et al.: Antitumor effect of gefitinib ('Iressa') on esophageal squamous cell carcinoma cell lines in vitro and in vivo. Cancer Lett. (2005) 226:37-47.
43. SHINTANI S, LI C, MIHARA M et al.: Gefitinib ('Iressa', ZD1839), an epidermal growth factor receptor tyrosine kinase inhibitor, up-regulates p27KIP1 and induces G1 arrest in oral squamous cell carcinoma cell lines. Oral Oncol. (2004) 40:43-51.
44. CHANG GC, HSU SL, TSAI JR et al.: Molecular mechanisms of ZD1839-induced G1-cell cycle arrest and apoptosis in human lung adenocarcinoma A549 cells. Biochem. Pharmacol. (2004) 68:1453-1464.
45. CAMPIGLIO M, LOCATELLI A, OLGIATI C et al.: Inhibition of proliferation and induction of apoptosis in breast cancer cells by the epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor ZD1839 ('Iressa') is independent of EGFR expression level. J. Cell. Physiol. (2004) 198:259-268.
46. SGAMBATO A, CAMERINI A, FARAGLIA B et al.: Targeted inhibition of the epidermal growth factor receptor-tyrosine kinase by ZD1839 ('Iressa') induces cell-cycle arrest and inhibits proliferation in prostate cancer cells. J. Cell. Physiol. (2004) 201:97-105.
47. HE Y, ZENG Q, DRENNING SD et al.: Inhibition of human squamous cell carcinoma growth in vivo by epidermal growth factor receptor antisense RNA transcribed from the U6 promoter. J. Natl. Cancer Inst. (1998) 90:1080-1087.
48. HAZAN RB, NORTON L: The epidermal growth factor receptor modulates the interaction of E-cadherin with the actin cytoskeleton. J. Biol. Chem. (1998) 273:9078-9084.
49. LICHTNER RB, KAUFMANN AM, KITTMANN A et al.: Ligand mediated activation of ectopic EGF receptor promotes matrix protein adhesion and lung colonization of rat mammary adenocarcinoma cells. Oncogene (1995) 10:1823-1832.
50. ADELSMAN MA, MCCARTHY JB, SHIMIZU Y: Stimulation of beta1-integrin function by epidermal growth factor and heregulin-beta has distinct requirements for ErbB2 but a similar dependence on phosphoinositide 3-OH kinase. Mol. Biol. Cell (1999) 10:2861-2878.
51. O-CHAROENRAT P, RHYS-EVANS P, COURT WJ, BOX GM, ECCLES SA: 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) 17:631-639.
52. O-CHAROENRAT P, MODJTAHEDI H, RHYS-EVANS P, COURT WJ, BOX GM, ECCLES SA: Epidermal growth factor-like ligands differentially up-regulate matrix metalloproteinase 9 in head and neck squamous carcinoma cells. Cancer Res. (2000) 60:1121-1128.
53. O-CHAROENRAT P, RHYS-EVANS P, MODJTAHEDI H, COURT W, BOX G, ECCLES S: Overexpression of epidermal growth factot receptor in human head and neck squamous carcinoma cell lines correlates with matrix metalloproteinase-9 expression and in vitro invasion. Int. J. Cancer (2000) 86:307-317.
54. DAMSTRUP L, VOLDBORG BR, SPANG-THOMSEN M, BRUNNER N, POULSEN HS: In vitro invasion of small-cell lung cancer cell lines correlates with expression of epidermal growth factor receptor. Br. J. Cancer (1998) 78:631-640.
55. HUANG SM, LIJ, HARARI PM: Molecular inhibition of angiogenesis and metastatic potential in human squamous cell carcinomas after epidermal growth factor receptor blockade. Mol. Cancer Ther. (2002) 1:507-514.
56. SHINTANI S, LI C, MIHARA M, NAKASHIRO KI, HAMAKAWA H: Gefitinib ('Iressa'), an epidermal growth factor receptor tyrosine kinase inhibitor, mediates the inhibition of lymph node metastasis in oral cancer cells. Cancer Lett. (2003) 201:149-155.
57. LIU Z, KLOMINEK J: Inhibition of proliferation, migration, and matrix metalloprotease production in malignant mesothelioma cells by tyrosine kinase inhibitors. Neoplasia (2004) 6:705-712.
58. ALPER Ö, DE SANTIS ML, STROMBERG K, HACKER NF, CHO-CHUNG YS, SALOMON DS: Anti-sense suppression of epidermal growth factor receptor expression alters cellular proliferation, cell-adhesion and tumorigenicity in ovarian cancer cells. Int. J. Cancer (2000) 88:566-574.
59. ALPER Ö, BERGMANN-LEITNER ES, BENNETT TA, HACKER NF, STROMBERG K, STETLER-STEVENSON WG: Epidermal growth factor receptor signaling and the invasive phenotype of ovarian carcinoma cells. J. Natl. Cancer Inst. (2001) 93:1375-1384.
60. GOLDMAN CK, KIM J, WONG WL, KING V, BROCK T, GILLESPIE GY: Epidermal growth factor stimulates vascular endothelial growth factor production by human malignant glioma cells: a model of glioblastoma multiforme pathophysiology. Mol. Biol. Cell (1993) 4:121-133.
61. PETIT AM, RAK J, HUNG MC et al.: 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 of solid tumors. Am. J. Pathol. (1997) 151:1523-1530.
62. PERROTTE P, MATSUMOTO T, INOUE K et al.: Anti-epidermal growth factor receptor antibody C225 inhibits angiogenesis in human transitional cell carcinoma growing orthotopically in nude mice. Clin. Cancer Res. (1999) 5:257-265.
63. CIARDIELLO F, CAPUTO R, BIANCO R et al.: Inhibition of growth factor production and angiogenesis in human cancer cells by ZD1839 (Iressa), a selective epidermal growth factor receptor tyrosine kinase inhibitor. Clin. Cancer Res. (2001) 7:1459-1465.
64. RIEDEL F, GOTTE K, LI M, HORMANN K, GRANDIS JR: EGFR antisense treatment of human HNSCC cell lines down-regulates VEGF expression and endothelial cell migration. Int. J. Oncol. (2002) 21:11-16.
65. CASTILLO L, ETIENNE-GRIMALDI MC, FISCHEL JL, FORMENTO P, MAGNÉ N, MILANO G: Pharmacological background of EGFR targeting. Ann. Oncol. (2004) 15:1007-1012.
66. NIWA H, WENTZEL AL, LI M, GOODING WE, LUI VW, GRANDIS JR: Antitumor effects of epidermal growth factor receptor antisense oligonucleotides in combination with docetaxel in squamous cell carcinoma of the head and neck. Clin. Cancer Res. (2003) 9:5028-5035.
67. HUANG S, ARMSTRONG EA, BENAVENTE S, CHINNAIYAN P, HARARI PM: Dual-agent molecular targeting of the epidermal growth factor receptor (EGFR): combining anti-EGFR antibody with tyrosine kinase inhibitor. Cancer Res. (2004) 64:5355-5362. One of the reports presenting combined strategies.
68. FISCHEL JL, FORMENTO P, MILANO G: Epidermal growth factor receptor double targeting by a tyrosine kinase inhibitor (Iressa) and a monoclonal antibody (cetuximab). Impact on cell growth and molecular factors. Br. J. Cancer (2005) 92:1063-1068.
69. FORMENTO P, HANNOUN-LEVI J, GÉRARD F et al.: Gefitinib-trastuzumab combination on hormone-refractory prostate cancer xenograft. Eur. J. Cancer (2005) 41:1467-1473.
70. FRIESS T, SCHEUER W, HASMANN M: Combination treatment with erlotinib and pertuzumab against human tumor xenografts is superior to monotherapy. Clin. Cancer Res. (2005) 11:5300-5309.
71. JUNG YD, MANSFIELD PF, AKAGI M et al.: 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) 38:1133-1140. One of the reports presenting combined strategies.
72. CIARDIELLO F, BIANCO R, DAMIANO V et al.: Antiangiogenic and antitumor activity of anti-epidermal growth factor receptor C225 monoclonal antibody in combination with vascular endothelial growth factor antisense oligonucleotide in human GEO colon cancer cells. Clin. Cancer Res. (2000) 6:3739-3747. One of the reports presenting combined strategies.
73. SINI P, WYDER L, SCHNELL C et al.: The antitumor and antiangiogenic activity of vascular endothelial growth factor receptor inhibition is potentiated by erbb1 blockade. Clin. Cancer Res. (2005) 11:4521-4532.
74. RYAN AJ, WEDGE SR: ZD6474-a novel inhibitor of VEGFR and EGFR tyrosine kinase activity. Br. J. Cancer (2005) 92:S6-S13.
75. YOKOI K, THAKER PH, YAZICI S et al.: Dual inhibition of epidermal growth factor receptor and vascular endothelial growth factor receptor phosphorylation by AEE788 reduces growth and metastasis of human colon carcinoma in an orthotopic nude mouse model. Cancer Res. (2005) 65:3716-3725.
76. YAZICI S, KIM SJ, BUSBY JE et al.: Dual inhibition of the epidermal growth factor and vascular endothelial growth factor phosphorylation for antivascular therapy of human prostate cancer in the prostate of nude mice. Prostate (2005) 65:203-215.
77. YOUNES MN, YIGITBASI OG, PARK YW et al.: Antivascular therapy of human follicular thyroid cancer experimental bone metastasis by blockade of epidermal growth factor receptor and vascular growth factor receptor phosphorylation. Cancer Res. (2005) 65:4716-4727.
78. RABEN D, BIANCO C, DAMIANO V et al.: Antitumor activity of ZD6126, a novel vascular-targeting agent, is enhanced when combined with ZD1839, an epidermal growth factor receptor tyrosine kinase inhibitor, and potentiates the effects of radiation in a human non-small cell lung cancer xenograft model. Mol. Cancer Ther. (2004) 3:977-983. One of the reports presenting combined strategies.
79. SALCEDO R, MARTINS-GREEN M, GERTZ B, OPPENHEIM JJ, MURPHY WJ: Combined administration of antibodies to human interleukin 8 and epidermal growth factor receptor results in increased antimetastatic effects on human breast carcinoma xenografts. Clin. Cancer Res. (2002) 8:2655-2665.
80. LU D, ZHANG H, LUDWIG D et al.: 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) 279:2856-2865.