Targeting HER receptors in cancer

Current Pharmaceutical Design

Volumn 19, Issue 5, 2013, Pages 808-817

  Ocaña, Alberto ^b,c   Pandiella, Atanasio ^a  

^a CSIC   (Spain)

^b HOSPITAL GENERAL UNIVERSITARIO DE ALBACETE   (Spain)

^c UNIVERSITY OF TORONTO   (Canada)

Author keywords

EGF ligands; HER receptors; Kinase inhibitors; Targeted therapies

Indexed keywords

AFATINIB; CETUXIMAB; DACOMITINIB; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; LAPATINIB; NERATINIB; PANITUMUMAB; PERTUZUMAB; PHOSPHATIDYLINOSITOL 3 KINASE; PROTEIN KINASE C; PROTEIN TYROSINE KINASE INHIBITOR; SHORT HAIRPIN RNA; TRASTUZUMAB;

APOPTOSIS; BREAST CANCER; CELL PROLIFERATION; COLORECTAL CANCER; DIMERIZATION; ENZYME ACTIVITY; GENE MUTATION; GENE OVEREXPRESSION; HEAD AND NECK CANCER; HUMAN; LIGAND BINDING; LUNG CANCER; NONHUMAN; PANCREAS CANCER; PATHOPHYSIOLOGY; PRIORITY JOURNAL; PROGRESSION FREE SURVIVAL; PROTEIN CONFORMATION; PROTEIN FAMILY; PROTEIN PHOSPHORYLATION; PROTEIN TARGETING; REVIEW; SIGNAL TRANSDUCTION; STOMACH CANCER;

EID: 84876705235     PISSN: 13816128     EISSN: 18734286     Source Type: Journal    
DOI: 10.2174/138161213804547303     Document Type: Review

References (103)

1. Hynes NE, Lane HA. ERBB receptors and cancer: the complexity of targeted inhibitors. Nat Rev Cancer 2005; 5: 341-54.
2. Slamon DJ, Godolphin W, Jones LA, et al. Studies of the HER-2/neu proto-oncogene in human breast and ovarian cancer. Science 1989; 244: 707-12.
3. Bang YJ, Van Cutsem E, Feyereislova A, et al. Trastuzumab in combination with chemotherapy versus chemotherapy alone for treatment of HER2-positive advanced gastric or gastro-oesophageal junction cancer (ToGA): a phase 3, open-label, randomised controlled trial. Lancet 2010; 376: 687-97.
4. Tanner M, Hollmen M, Junttila TT, et al. Amplification of HER-2 in gastric carcinoma: association with Topoisomerase IIalpha gene amplification, intestinal type, poor prognosis and sensitivity to trastuzumab. Ann Oncol 2005; 16: 273-8.
5. Olayioye MA, Neve RM, Lane HA, Hynes NE. The ErbB signaling network: receptor heterodimerization in development and cancer. Embo J 2000; 19: 3159-67.
6. Cohen S. Isolation of a mouse submaxillary gland protein accelerating incisor eruption and eyelid opening in the new-born animal. J Biol Chem 1962; 237: 1555-62.
7. Montero JC, Rodriguez-Barrueco R, Ocana A, et al. Neuregulins and cancer. Clin Cancer Res 2008; 14: 3237-41.
8. Massagué J, Pandiella A. Membrane-anchored growth factors. Annu. Rev. Biochem. 1993; 62: 515-41.
9. Bao J, Wolpowitz D, Role LW, Talmage DA. Back signaling by the Nrg-1 intracellular domain. J Cell Biol 2003; 161: 1133-41.
10. Wong ST, Winchell LF, McCune BK, et al. The TGF-alpha precursor expressed on the cell surface binds to the EGF receptor on adjacent cells, leading to signal transduction. Cell 1989; 56: 495-506.
11. Pandiella A, Massague J. Cleavage of the membrane precursor for transforming growth factor alpha is a regulated process. Proc Natl Acad Sci USA 1991; 88: 1726-30.
12. Montero JC, Yuste L, Diaz-Rodriguez E, et al. Differential shedding of transmembrane neuregulin isoforms by the tumor necrosis factor-alpha-converting enzyme. Mol Cell Neurosci 2000; 16: 631-48.
13. Black RA, Rauch CT, Kozlosky CJ, et al. A metalloproteinase disintegrin that releases tumour-necrosis factor-alpha from cells. Nature 1997; 385: 729-33.
14. Blobel CP. ADAMs: key components in EGFR signalling and development. Nat Rev Mol Cell Biol 2005; 6: 32-43.
15. Luo X, Prior M, He W, et al. Cleavage of neuregulin-1 by BACE1 or ADAM10 protein produces differential effects on myelination. J Biol Chem 2011; 286: 23967-74.
16. Juanes PP, Ferreira L, Montero JC, et al. N-terminal cleavage of proTGFalpha occurs at the cell surface by a TACE-independent activity. Biochem J 2005; 389: 161-72.
17. Diaz-Rodriguez E, Montero JC, Esparis-Ogando A, et al. Extracellular signal-regulated kinase phosphorylates tumor necrosis factor alpha-converting enzyme at threonine 735: a potential role in regulated shedding. Mol Biol Cell 2002; 13: 2031-44.
18. Carraway KL, 3rd, Sliwkowski MX, Akita R, et al. The erbB3 gene product is a receptor for heregulin. J Biol Chem 1994; 269: 14303-6.
19. Sliwkowski MX, Schaefer G, Akita RW, et al. Coexpression of erbB2 and erbB3 proteins reconstitutes a high affinity receptor for heregulin. J Biol Chem 1994; 269: 14661-5.
20. Jones RB, Gordus A, Krall JA, MacBeath G. A quantitative protein interaction network for the ErbB receptors using protein microarrays. Nature 2006; 439: 168-74.
21. Burgess AW, Cho HS, Eigenbrot C, et al. An open-and-shut case? Recent insights into the activation of EGF/ErbB receptors. Mol Cell 2003; 12: 541-52.
22. Zhang X, Gureasko J, Shen K, et al. An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell 2006; 125: 1137-49.
23. Endres NF, Engel K, Das R, et al. Regulation of the catalytic activity of the EGF receptor. Curr Opin Struct Biol 2011; 21: 777-84.
24. Slamon DJ, Clark GM, Wong SG, et al. Human breast cancer: correlation of relapse and survival with amplification of the HER-2/neu oncogene. Science 1987; 235: 177-82.
25. Paez JG, Janne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004; 304: 1497-500.
26. Lynch TJ, Bell DW, Sordella R, et al. 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.
27. Yang CH, Yu CJ, Shih JY, et al. Specific EGFR mutations predict treatment outcome of stage IIIB/IV patients with chemotherapynaive non-small-cell lung cancer receiving first-line gefitinib monotherapy. J Clin Oncol 2008; 26: 2745-53.
28. Zhu CQ, da Cunha Santos G, Ding K, et al. Role of KRAS and EGFR as biomarkers of response to erlotinib in National Cancer Institute of Canada Clinical Trials Group Study BR.21. J Clin Oncol 2008; 26: 4268-75.
29. Arribas J, Baselga J, Pedersen K, Parra-Palau JL. p95HER2 and breast cancer. Cancer Res 2011; 71: 1515-9.
30. Ocana A, Amir E, Seruga B, Martin M, Pandiella A. The evolving landscape of protein kinases in breast cancer: Clinical implications. Cancer Treat Rev 2012 Jun 13. [Epub ahead of print]
31. Gan HK, Kaye AH, Luwor RB. The EGFRvIII variant in glioblastoma multiforme. J Clin Neurosci 2009; 16: 748-54.
32. Ullrich A, Schlessinger J. Signal transduction by receptors with tyrosine kinase activity. Cell 1990; 61: 203-12.
33. Sanchez-Martin M, Pandiella A. Differential action of small molecule HER kinase inhibitors on receptor heterodimerization: Therapeutic implications. Int J Cancer 2012; 131: 244-52.
34. Sun T, Aceto N, Meerbrey KL, et al. Activation of multiple protooncogenic tyrosine kinases in breast cancer via loss of the PTPN12 phosphatase. Cell 2011; 144: 703-18.
35. Yarden Y, Sliwkowski MX. Untangling the ErbB signalling network. Nat Rev Mol Cell Biol 2001; 2: 127-37.
36. Ullrich A, Schlessinger J. Signal transduction by receptors with tyrosine kinase activity. Cell 1990; 61: 203-12.
37. Weiner LM. Building better magic bullets--improving unconjugated monoclonal antibody therapy for cancer. Nat Rev Cancer 2007; 7: 701-6.
38. Hudziak RM, Lewis GD, Winget M, et al. p185HER2 monoclonal antibody has antiproliferative effects in vitro and sensitizes human breast tumor cells to tumor necrosis factor. Mol Cell Biol 1989; 9: 1165-72.
39. Sliwkowski MX, Lofgren JA, Lewis GD, et al. Nonclinical studies addressing the mechanism of action of trastuzumab (Herceptin). Semin Oncol 1999; 26: 60-70.
40. Kumar R, Shepard HM, Mendelsohn J. Regulation of phosphorylation of the c-erbB-2/HER2 gene product by a monoclonal antibody and serum growth factor(s) in human mammary carcinoma cells. Mol. Cell. Biol. 1991; 11: 979-86.
41. Clynes RA, Towers TL, Presta LG, Ravetch JV. Inhibitory Fc receptors modulate in vivo cytoxicity against tumor targets. Nat Med 2000; 6: 443-6.
42. Baselga J, Cortes J, Kim SB, et al. Pertuzumab plus Trastuzumab plus Docetaxel for Metastatic Breast Cancer. N Engl J Med 2012; 366: 109-19.
43. Cho HS, Mason K, Ramyar KX, et al. Structure of the extracellular region of HER2 alone and in complex with the Herceptin Fab. Nature 2003; 421: 756-60.
44. Agus DB, Akita RW, Fox WD, et al. Targeting ligand-activated ErbB2 signaling inhibits breast and prostate tumor growth. Cancer Cell 2002; 2: 127-37.
45. Yuste L, Montero JC, Esparis-Ogando A, Pandiella A. Activation of ErbB2 by overexpression or by transmembrane neuregulin results in differential signaling and sensitivity to herceptin. Cancer Res 2005; 65: 6801-10.
46. Baselga, J Swain SM. Novel anticancer targets: revisiting ERBB2 and discovering ERBB3. Nat Rev Cancer. 2009; 9: 463-75.
47. Agus DB, Akita RW, Fox WD, et al. Targeting ligand-activated ErbB2 signaling inhibits breast and prostate tumor growth. Cancer Cell 2002; 2: 127-37.
48. Sliwkowski MX, Schaefer G, Akita RW, et al. Coexpression of erbB2 and erbB3 proteins reconstitutes a high affinity receptor for heregulin. J Biol Chem 1994; 269: 14661-5.
49. 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: 1523-30.
50. Izumi Y, Xu L, di Tomaso E, et al. Tumour biology: herceptin acts as an anti-angiogenic cocktail. Nature 2002; 416: 279-80.
51. Pietras RJ, Pegram MD, Finn RS, et al. Remission of human breast cancer xenografts on therapy with humanized monoclonal antibody to HER-2 receptor and DNA-reactive drugs. Oncogene 1998; 17: 2235-49.
52. Pietras RJ, Poen JC, Gallardo D, et al. Monoclonal antibody to HER-2/neureceptor modulates repair of radiation-induced DNA damage and enhances radiosensitivity of human breast cancer cells overexpressing this oncogene. Cancer Res 1999; 59: 1347-55.
53. Seoane S, Montero JC, Ocana A, Pandiella A. Effect of multikinase inhibitors on caspase-independent cell death and DNA damage in HER2-overexpressing breast cancer cells. J Natl Cancer Inst 2010; 102: 1432-46.
54. Li L, Wang H, Yang ES, et al. Erlotinib attenuates homologous recombinational repair of chromosomal breaks in human breast cancer cells. Cancer Res 2008; 68: 9141-6.
55. Meyer D, Birchmeier C. Multiple essential functions of neuregulin in development. Nature 1995; 378: 386-90.
56. Meyer D, Yamaai T, Garratt A, et al. Isoform-specific expression and function of neuregulin. Development 1997; 124: 3575-86.
57. Ocana A, Rodriguez CA, Cruz JJ. Integrating trastuzumab in the treatment of breast cancer. Current status and future trends. Clin Transl Oncol 2005; 7: 99-100.
58. Piccart-Gebhart MJ, Procter M, Leyland-Jones B, et al. Trastuzumab after adjuvant chemotherapy in HER2-positive breast cancer. N Engl J Med 2005; 353: 1659-72.
59. Slamon D, Eiermann W, Robert N, et al. Adjuvant trastuzumab in HER2-positive breast cancer. N Engl J Med 2011; 365: 1273-83.
60. Amado RG, Wolf M, Peeters M, et al. Wild-type KRAS is required for panitumumab efficacy in patients with metastatic colorectal cancer. J Clin Oncol 2008; 26: 1626-34.
61. Jonker DJ, O'Callaghan CJ, Karapetis CS, et al. Cetuximab for the treatment of colorectal cancer. N Engl J Med 2007; 357: 2040-8.
62. Maughan TS, Adams RA, Smith CG, et al. Addition of cetuximab to oxaliplatin-based first-line combination chemotherapy for treatment of advanced colorectal cancer: results of the randomised phase 3 MRC COIN trial. Lancet 2011; 377: 2103-14.
63. Van Cutsem E, Kohne CH, Lang I, et al. Cetuximab plus irinotecan, fluorouracil, and leucovorin as first-line treatment for metastatic colorectal cancer: updated analysis of overall survival according to tumor KRAS and BRAF mutation status. J Clin Oncol 2011; 29: 2011-9.
64. Vermorken JB, Mesia R, Rivera F, et al. Platinum-based chemotherapy plus cetuximab in head and neck cancer. N Engl J Med 2008; 359: 1116-27.
65. Valero V, Forbes J, Pegram MD, et al. Multicenter phase III randomized trial comparing docetaxel and trastuzumab with docetaxel, carboplatin, and trastuzumab as first-line chemotherapy for patients with HER2-gene-amplified metastatic breast cancer (BCIRG 007 study): two highly active therapeutic regimens. J Clin Oncol 2011; 29: 149-56.
66. Robert N, Leyland-Jones B, Asmar L, et al. Randomized phase III study of trastuzumab, paclitaxel, and carboplatin compared with trastuzumab and paclitaxel in women with HER-2-overexpressing metastatic breast cancer. J Clin Oncol 2006; 24: 2786-92.
67. Zhang J, Yang PL, Gray NS. Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer 2009; 9: 28-39.
68. Geyer CE, Forster J, Lindquist D, et al. Lapatinib plus capecitabine for HER2-positive advanced breast cancer. N Engl J Med 2006; 355: 2733-43.
69. Johnston S, Pippen J, Jr., Pivot X, et al. Lapatinib combined with letrozole versus letrozole and placebo as first-line therapy for postmenopausal hormone receptor-positive metastatic breast cancer. J Clin Oncol 2009; 27: 5538-46.
70. Moore MJ, Goldstein D, Hamm J, et al. Erlotinib plus gemcitabine compared with gemcitabine alone in patients with advanced pancreatic cancer: a phase III trial of the National Cancer Institute of Canada Clinical Trials Group. J Clin Oncol 2007; 25: 1960-6.
71. Tsao MS, Sakurada A, Cutz JC, et al. Erlotinib in lung cancer-molecular and clinical predictors of outcome. N Engl J Med 2005; 353: 133-44.
72. Cappuzzo F, Ciuleanu T, Stelmakh L, et al. Erlotinib as maintenance treatment in advanced non-small-cell lung cancer: a multicentre, randomised, placebo-controlled phase 3 study. Lancet Oncol 2010; 11: 521-9.
73. Maemondo M, Inoue A, Kobayashi K, et al. Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR. N Engl J Med 2010; 362: 2380-8.
74. Mitsudomi T, Morita S, Yatabe Y, et al. Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial. Lancet Oncol 11: 121-8.
75. Ocana A, Amir E. Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: Current status and future directions. Cancer Treat Rev 2009; 35: 685-91.
76. Sharma SV, Bell DW, Settleman J, Haber DA. Epidermal growth factor receptor mutations in lung cancer. Nat Rev Cancer 2007; 7: 169-81.
77. Miller VA, Hirsh V, Cadranel J, et al. Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial. Lancet Oncol 2012, 13: 528-38.
78. Giaccone G, Wang Y. Strategies for overcoming resistance to EGFR family tyrosine kinase inhibitors. Cancer Treat Rev 2011; 37: 456-64.
79. de Alava E, Ocana A, Abad M, et al. Neuregulin expression modulates clinical response to trastuzumab in patients with metastatic breast cancer. J Clin Oncol 2007; 25: 2656-63.
80. Kwak EL, Sordella R, Bell DW, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci USA 2005; 102: 7665-70.
81. Giaccone G, Wang Y. Strategies for overcoming resistance to EGFR family tyrosine kinase inhibitors. Cancer Treat Rev 37: 456-64.
82. Montagut C, Dalmases A, Bellosillo B, et al. Identification of a mutation in the extracellular domain of the Epidermal Growth Factor Receptor conferring cetuximab resistance in colorectal cancer. Nat Med 2012; 18: 221-3.
83. Bardelli A, Janne PA. The road to resistance: EGFR mutation and cetuximab. Nat Med 2012; 18: 199-200.
84. Holbro T, Beerli RR, Maurer F, et al. The ErbB2/ErbB3 heterodimer functions as an oncogenic unit: ErbB2 requires ErbB3 to drive breast tumor cell proliferation. Proc Natl Acad Sci USA 2003; 100: 8933-8.
85. Ritter CA, Perez-Torres M, Rinehart C, et al. Human breast cancer cells selected for resistance to trastuzumab in vivo overexpress epidermal growth factor receptor and ErbB ligands and remain dependent on the ErbB receptor network. Clin Cancer Res 2007; 13: 4909-19.
86. Engelman JA, Zejnullahu K, Mitsudomi T, et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 2007; 316: 1039-43.
87. Sergina NV, Rausch M, Wang D, et al. Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3. Nature 2007; 445: 437-41.
88. Zhou BB, Peyton M, He B, et al. Targeting ADAM-mediated ligand cleavage to inhibit HER3 and EGFR pathways in non-small cell lung cancer. Cancer Cell 2006; 10: 39-50.
89. Engelman JA. Targeting PI3K signalling in cancer: opportunities, challenges and limitations. Nat Rev Cancer 2009; 9: 550-62.
90. Harris TE, Lawrence JC, Jr. TOR signaling. Sci STKE 2003; 2003: re15.
91. Jacinto E, Hall MN. Tor signalling in bugs, brain and brawn. Nat Rev Mol Cell Biol 2003; 4: 117-26.
92. Fingar DC, Richardson CJ, Tee AR, et al. mTOR controls cell cycle progression through its cell growth effectors S6K1 and 4EBP1/ eukaryotic translation initiation factor 4E. Mol Cell Biol 2004; 24: 200-16.
93. Sun H, Lesche R, Li DM, et al. PTEN modulates cell cycle progression and cell survival by regulating phosphatidylinositol 3,4,5,-trisphosphate and Akt/protein kinase B signaling pathway. Proc Natl Acad Sci USA 1999; 96: 6199-204.
94. Nagata Y, Lan KH, Zhou X, et al. PTEN activation contributes to tumor inhibition by trastuzumab, and loss of PTEN predicts trastuzumab resistance in patients. Cancer Cell 2004; 6: 117-27.
95. Morrow PK, Wulf GM, Ensor J, et al. Phase I/II study of trastuzumab in combination with everolimus (RAD001) in patients with HER2-overexpressing metastatic breast cancer who progressed on trastuzumab-based therapy. J Clin Oncol 2011; 29: 3126-32.
96. De Roock W, Claes B, Bernasconi D, et al. Effects of KRAS, BRAF, NRAS, and PIK3CA mutations on the efficacy of cetuximab plus chemotherapy in chemotherapy-refractory metastatic colorectal cancer: a retrospective consortium analysis. Lancet Oncol 2010; 11: 753-62.
97. Courtney KD, Corcoran RB, Engelman JA. The PI3K pathway as drug target in human cancer. J Clin Oncol 2010; 28: 1075-83.
98. Vanhaesebroeck B, Guillermet-Guibert J, Graupera M, Bilanges B. The emerging mechanisms of isoform-specific PI3K signalling. Nat Rev Mol Cell Biol 2010; 11: 329-41.
99. Eichhorn PJ, Gili M, Scaltriti M, et al. Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVPBEZ235. Cancer Res 2008; 68: 9221-30.
100. Barbacid M. ras genes. Annu Rev Biochem 1987; 56: 779-827.
101. Faber AC, Li D, Song Y, et al. Differential induction of apoptosis in HER2 and EGFR addited cancers following PI3K inhibition. Proc Natl Acad Sci USA 2009; 106: 19503-8.
102. Pao W, Wang TY, Riely GJ, et al. KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib. PLoS Med 2005; 2: e17.
103. Eberhard DA, Johnson BE, Amler LC, et al. Mutations in the epidermal growth factor receptor and in KRAS are predictive and prognostic indicators in patients with non-small-cell lung cancer treated with chemotherapy alone and in combination with erlotinib. J Clin Oncol 2005; 23: 5900-9.