A candidate targeting molecule of insulin-like growth factor-I receptor for gastrointestinal cancers

World Journal of Gastroenterology

Volumn 16, Issue 46, 2010, Pages 5779-5789

  Adachi, Yasushi ^a,b   Yamamoto, Hiroyuki ^a   Ohashi, Hirokazu ^a   Endo, Takao ^b   Carbone, David P ^c   Imai, Kohzoh ^a   Shinomura, Yasuhisa ^a  

^a SAPPORO MEDICAL UNIVERSITY   (Japan)

^b Sapporo Shirakabadai Hospital   (Japan)

^c VANDERBILT INGRAM CANCER CENTER   (United States)

Author keywords

Dominant negative; Gastrointestinal cancer; Insulin like growth factor I receptor; Monoclonal antibody; Tyrosine kinase inhibitor

Indexed keywords

A 928605; AMG 479; ANTINEOPLASTIC AGENT; AVE 1642; BIIB 022; BMS 536924; BMS 554417; BMS 754807; BVP 51004; CISPLATIN; CP 751 871; CYCLOLIGNAN; DALOTUZUMAB; EPIDERMAL GROWTH FACTOR RECEPTOR 2; FIGITUMUMAB; FLUOROURACIL; IGF BINDING PROTEIN 3; IMCA 12; INSM 18; INSULIN RECEPTOR; KM 1468; KM 3002; KM 3168; NVPADW 742; NVPAEW 541; NVPTAE 226; OSI 906; POLYPHENOL; R 1507; ROBATUMUMAB; SOMATOMEDIN C RECEPTOR; UNCLASSIFIED DRUG; UNINDEXED DRUG; XL 228;

ADRENAL CORTEX CARCINOMA; ADVANCED CANCER; ADVANCED SOLID TUMOR; ATYPICAL CHRONIC MYELOID LEUKEMIA; BLADDER CANCER; BRAIN CANCER; BREAST CANCER; CLINICAL TRIAL; COLON CANCER; COLORECTAL CANCER; DIGESTIVE SYSTEM CANCER; DRUG MECHANISM; ESOPHAGUS CANCER; HEAD AND NECK CANCER; HUMAN; IN VITRO STUDY; IN VIVO STUDY; KIDNEY CANCER; LEUKEMIA; LIVER CANCER; LIVER CELL CARCINOMA; LUNG CANCER; LUNG CARCINOGENESIS; LYMPHOMA; MYELODYSPLASTIC SYNDROME; MYELOMA; NEUROENDOCRINE DISEASE; NONHUMAN; OVARY CANCER; PANCREAS CANCER; PANCREAS ISLET CELL CARCINOMA; PROSTATE CANCER; PROTEIN FUNCTION; PROTEIN STRUCTURE; REVIEW; SARCOMA; SIGNAL TRANSDUCTION; SOLID TUMOR; THYMUS CANCER;

EID: 78650625659     PISSN: 10079327     EISSN: None     Source Type: Journal    
DOI: 10.3748/wjg.v16.i46.5779     Document Type: Review

References (100)

1. Baserga R. Oncogenes and the strategy of growth factors. Cell 1994; 79: 927-930
2. Ranson M, Hammond LA, Ferry D, Kris M, Tullo A, Murray PI, Miller V, Averbuch S, Ochs J, Morris C, Feyereislova A, Swaisland H, Rowinsky EK. ZD1839, a selective oral epidermal growth factor receptor-tyrosine kinase inhibitor, is well tolerated and active in patients with solid, malignant tumors: results of a phase I trial. J Clin Oncol 2002; 20: 2240-2250
3. Demetri GD, von Mehren M, Blanke CD, Van den Abbeele AD, Eisenberg B, Roberts PJ, Heinrich MC, Tuveson DA, Singer S, Janicek M, Fletcher JA, Silverman SG, Silberman SL, Capdeville R, Kiese B, Peng B, Dimitrijevic S, Druker BJ, Corless C, Fletcher CD, Joensuu H. Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. N Engl J Med 2002; 347: 472-480
4. Yau T, Chan P, Ng KK, Chok SH, Cheung TT, Fan ST, Poon RT. Phase 2 open-label study of single-agent sorafenib in treating advanced hepatocellular carcinoma in a hepatitis B-endemic Asian population: presence of lung metastasis predicts poor response. Cancer 2009; 115: 428-436
5. Norden-Zfoni A, Desai J, Manola J, Beaudry P, Force J, Maki R, Folkman J, Bello C, Baum C, DePrimo SE, Shalinsky DR, Demetri GD, Heymach JV. Blood-based biomarkers of SU11248 activity and clinical outcome in patients with metastatic imatinib-resistant gastrointestinal stromal tumor. Clin Cancer Res 2007; 13: 2643-2650
6. Pegram MD, Lipton A, Hayes DF, Weber BL, Baselga JM, Tripathy D, Baly D, Baughman SA, Twaddell T, Glaspy JA, Slamon DJ. Phase II study of receptor-enhanced chemosensitivity using recombinant humanized anti-p185HER2/neu monoclonal antibody plus cisplatin in patients with HER2/ neu-overexpressing metastatic breast cancer refractory to chemotherapy treatment. J Clin Oncol 1998; 16: 2659-2671
7. Lenz HJ, Van Cutsem E, Khambata-Ford S, Mayer RJ, Gold P, Stella P, Mirtsching B, Cohn AL, Pippas AW, Azarnia N, Tsuchihashi Z, Mauro DJ, Rowinsky EK. Multicenter phase II and translational study of cetuximab in metastatic colorectal carcinoma refractory to irinotecan, oxaliplatin, and fluoropyrimidines. J Clin Oncol 2006; 24: 4914-4921
8. Hurwitz HI, Fehrenbacher L, Hainsworth JD, Heim W, Berlin J, Holmgren E, Hambleton J, Novotny WF, Kabbinavar F. Bevacizumab in combination with fluorouracil and leucovorin: an active regimen for first-line metastatic colorectal cancer. J Clin Oncol 2005; 23: 3502-3508
9. Miller BS, Yee D. Type I insulin-like growth factor receptor as a therapeutic target in cancer. Cancer Res 2005; 65: 10123-10127
10. Ullrich A, Gray A, Tam AW, Yang-Feng T, Tsubokawa M, Collins C, Henzel W, Le Bon T, Kathuria S, Chen E. Insulinlike growth factor I receptor primary structure: comparison with insulin receptor suggests structural determinants that define functional specificity. EMBO J 1986; 5: 2503-2512
11. Baserga R. The insulin-like growth factor I receptor: a key to tumor growth? Cancer Res 1995; 55: 249-252
12. Yu H, Rohan T. Role of the insulin-like growth factor family in cancer development and progression. J Natl Cancer Inst 2000; 92: 1472-1489
13. Rodon J, DeSantos V, Ferry RJ Jr, Kurzrock R. Early drug development of inhibitors of the insulin-like growth factor-I receptor pathway: lessons from the first clinical trials. Mol Cancer Ther 2008; 7: 2575-2588
14. Ma J, Pollak MN, Giovannucci E, Chan JM, Tao Y, Hennekens CH, Stampfer MJ. Prospective study of colorectal cancer risk in men and plasma levels of insulin-like growth factor (IGF)-I and IGF-binding protein-3. J Natl Cancer Inst 1999; 91: 620-625
15. Harper J, Burns JL, Foulstone EJ, Pignatelli M, Zaina S, Hassan AB. Soluble IGF2 receptor rescues Apc(Min/+) intestinal adenoma progression induced by Igf2 loss of imprinting. Cancer Res 2006; 66: 1940-1948
16. Miyamoto S, Nakamura M, Yano K, Ishii G, Hasebe T, Endoh Y, Sangai T, Maeda H, Shi-Chuang Z, Chiba T, Ochiai A. Matrix metalloproteinase-7 triggers the matricrine action of insulin-like growth factor-II via proteinase activity on insulin-like growth factor binding protein 2 in the extracellular matrix. Cancer Sci 2007; 98: 685-691
17. Foulstone E, Prince S, Zaccheo O, Burns JL, Harper J, Jacobs C, Church D, Hassan AB. Insulin-like growth factor ligands, receptors, and binding proteins in cancer. J Pathol 2005; 205: 145-153
18. Sell C, Rubini M, Rubin R, Liu JP, Efstratiadis A, Baserga R. Simian virus 40 large tumor antigen is unable to transform mouse embryonic fibroblasts lacking type 1 insulin-like growth factor receptor. Proc Natl Acad Sci USA 1993; 90: 11217-11221
19. Chan JM, Stampfer MJ, Giovannucci E, Gann PH, Ma J, Wilkinson P, Hennekens CH, Pollak M. Plasma insulin-like growth factor-I and prostate cancer risk: a prospective study. Science 1998; 279: 563-566
20. Hankinson SE, Willett WC, Colditz GA, Hunter DJ, Michaud DS, Deroo B, Rosner B, Speizer FE, Pollak M. Circulating concentrations of insulin-like growth factor-I and risk of breast cancer. Lancet 1998; 351: 1393-1396
21. Cui H, Cruz-Correa M, Giardiello FM, Hutcheon DF, Kafonek DR, Brandenburg S, Wu Y, He X, Powe NR, Feinberg AP. Loss of IGF2 imprinting: a potential marker of colorectal cancer risk. Science 2003; 299: 1753-1755
22. Liu JP, Baker J, Perkins AS, Robertson EJ, Efstratiadis A. Mice carrying null mutations of the genes encoding insulinlike growth factor I (Igf-1) and type 1 IGF receptor (Igf1r). Cell 1993; 75: 59-72
23. Thompson MA, Cox AJ, Whitehead RH, Jonas HA. Autocrine regulation of human tumor cell proliferation by insulin-like growth factor II: an in-vitro model. Endocrinology 1990; 126: 3033-3042
24. Chen SC, Chou CK, Wong FH, Chang CM, Hu CP. Overexpression of epidermal growth factor and insulin-like growth factor-I receptors and autocrine stimulation in human esophageal carcinoma cells. Cancer Res 1991; 51: 1898-1903
25. Lahm H, Suardet L, Laurent PL, Fischer JR, Ceyhan A, Givel JC, Odartchenko N. Growth regulation and co-stimulation of human colorectal cancer cell lines by insulin-like growth factor I, II and transforming growth factor alpha. Br J Cancer 1992; 65: 341-346
26. Remacle-Bonnet M, Garrouste F, el Atiq F, Roccabianca M, Marvaldi J, Pommier G. des-(1-3)-IGF-I, an insulin-like growth factor analog used to mimic a potential IGF-II autocrine loop, promotes the differentiation of human coloncarcinoma cells. Int J Cancer 1992; 52: 910-917
27. Bergmann U, Funatomi H, Yokoyama M, Beger HG, Korc M. Insulin-like growth factor I overexpression in human pancreatic cancer: evidence for autocrine and paracrine roles. Cancer Res 1995; 55: 2007-2011
28. Ajisaka H, Fushida S, Yonemura Y, Miwa K. Expression of insulin-like growth factor-2, c-MET, matrix metalloproteinase-7 and MUC-1 in primary lesions and lymph node metastatic lesions of gastric cancer. Hepatogastroenterology 2001; 48: 1788-1792
29. Pavelić K, Kolak T, Kapitanović S, Radosević S, Spaventi S, Kruslin B, Pavelić J. Gastric cancer: the role of insulin-like growth factor 2 (IGF 2) and its receptors (IGF 1R and M6-P/ IGF 2R). J Pathol 2003; 201: 430-438
30. Simmons JG, Pucilowska JB, Lund PK. Autocrine and paracrine actions of intestinal fibroblast-derived insulin-like growth factors. Am J Physiol 1999; 276: G817-G827
31. Mori M, Inoue H, Shiraishi T, Mimori K, Shibuta K, Nakashima H, Mafune K, Tanaka Y, Ueo H, Barnard GF, Sugimachi K, Akiyoshi T. Relaxation of insulin-like growth factor 2 gene imprinting in esophageal cancer. Int J Cancer 1996; 68: 441-446
32. Freier S, Weiss O, Eran M, Flyvbjerg A, Dahan R, Nephesh I, Safra T, Shiloni E, Raz I. Expression of the insulin-like growth factors and their receptors in adenocarcinoma of the colon. Gut 1999; 44: 704-708
33. Imsumran A, Adachi Y, Yamamoto H, Li R, Wang Y, Min Y, Piao W, Nosho K, Arimura Y, Shinomura Y, Hosokawa M, Lee CT, Carbone DP, Imai K. Insulin-like growth factor-I receptor as a marker for prognosis and a therapeutic target in human esophageal squamous cell carcinoma. Carcinogenesis 2007; 28: 947-956
34. Levitt RJ, Pollak M. Insulin-like growth factor-I antagonizes the antiproliferative effects of cyclooxygenase-2 inhibitors on BxPC-3 pancreatic cancer cells. Cancer Res 2002; 62: 7372-7376
35. Nosho K, Yamamoto H, Taniguchi H, Adachi Y, Yoshida Y, Arimura Y, Endo T, Hinoda Y, Imai K. Interplay of insulinlike growth factor-II, insulin-like growth factor-I, insulin-like growth factor-I receptor, COX-2, and matrix metalloproteinase- 7, play key roles in the early stage of colorectal carcinogenesis. Clin Cancer Res 2004; 10: 7950-7957
36. Nosho K, Yamamoto H, Adachi Y, Endo T, Hinoda Y, Imai K. Gene expression profiling of colorectal adenomas and early invasive carcinomas by cDNA array analysis. Br J Cancer 2005; 92: 1193-1200
37. Nakamura M, Miyamoto S, Maeda H, Ishii G, Hasebe T, Chiba T, Asaka M, Ochiai A. Matrix metalloproteinase-7 degrades all insulin-like growth factor binding proteins and facilitates insulin-like growth factor bioavailability. Biochem Biophys Res Commun 2005; 333: 1011-1016
38. Adachi Y, Li R, Yamamoto H, Min Y, Piao W, Wang Y, Imsumran A, Li H, Arimura Y, Lee CT, Imai K, Carbone DP, Shinomura Y. Insulin-like growth factor-I receptor blockade reduces the invasiveness of gastrointestinal cancers via blocking production of matrilysin. Carcinogenesis 2009; 30: 1305-1313
39. De Meyts P, Whittaker J. Structural biology of insulin and IGF1 receptors: implications for drug design. Nat Rev Drug Discov 2002; 1: 769-783
40. Pandini G, Frasca F, Mineo R, Sciacca L, Vigneri R, Belfiore A. Insulin/insulin-like growth factor I hybrid receptors have different biological characteristics depending on the insulin receptor isoform involved. J Biol Chem 2002; 277: 39684-39695
41. Giovannucci E, Michaud D. The role of obesity and related metabolic disturbances in cancers of the colon, prostate, and pancreas. Gastroenterology 2007; 132: 2208-2225
42. Gunter MJ, Hoover DR, Yu H, Wassertheil-Smoller S, Rohan TE, Manson JE, Li J, Ho GY, Xue X, Anderson GL, Kaplan RC, Harris TG, Howard BV, Wylie-Rosett J, Burk RD, Strickler HD. Insulin, insulin-like growth factor-I, and risk of breast cancer in postmenopausal women. J Natl Cancer Inst 2009; 101: 48-60
43. Law JH, Habibi G, Hu K, Masoudi H, Wang MY, Stratford AL, Park E, Gee JM, Finlay P, Jones HE, Nicholson RI, Carboni J, Gottardis M, Pollak M, Dunn SE. Phosphorylated insulin-like growth factor-i/insulin receptor is present in all breast cancer subtypes and is related to poor survival. Cancer Res 2008; 68: 10238-10246
44. Schoen RE, Weissfeld JL, Kuller LH, Thaete FL, Evans RW, Hayes RB, Rosen CJ. Insulin-like growth factor-I and insulin are associated with the presence and advancement of adenomatous polyps. Gastroenterology 2005; 129: 464-475
45. Frasca F, Pandini G, Scalia P, Sciacca L, Mineo R, Costantino A, Goldfine ID, Belfiore A, Vigneri R. Insulin receptor isoform A, a newly recognized, high-affinity insulin-like growth factor II receptor in fetal and cancer cells. Mol Cell Biol 1999; 19: 3278-3288
46. Adachi Y, Lee CT, Coffee K, Yamagata N, Ohm JE, Park KH, Dikov MM, Nadaf SR, Arteaga CL, Carbone DP. Effects of genetic blockade of the insulin-like growth factor receptor in human colon cancer cell lines. Gastroenterology 2002; 123: 1191-1204
47. Min Y, Adachi Y, Yamamoto H, Ito H, Itoh F, Lee CT, Nadaf S, Carbone DP, Imai K. Genetic blockade of the insulin-like growth factor-I receptor: a promising strategy for human pancreatic cancer. Cancer Res 2003; 63: 6432-6441
48. Min Y, Adachi Y, Yamamoto H, Imsumran A, Arimura Y, Endo T, Hinoda Y, Lee CT, Nadaf S, Carbone DP, Imai K. Insulin- like growth factor I receptor blockade enhances chemotherapy and radiation responses and inhibits tumour growth in human gastric cancer xenografts. Gut 2005; 54: 591-600
49. Lee CT, Park KH, Adachi Y, Seol JY, Yoo CG, Kim YW, Han SK, Shim YS, Coffee K, Dikov MM, Carbone DP. Recombinant adenoviruses expressing dominant negative insulinlike growth factor-I receptor demonstrate antitumor effects on lung cancer. Cancer Gene Ther 2003; 10: 57-63
50. Surmacz E. Growth factor receptors as therapeutic targets: strategies to inhibit the insulin-like growth factor I receptor. Oncogene 2003; 22: 6589-6597
51. Szereday Z, Schally AV, Varga JL, Kanashiro CA, Hebert F, Armatis P, Groot K, Szepeshazi K, Halmos G, Busto R. Antagonists of growth hormone-releasing hormone inhibit the proliferation of experimental non-small cell lung carcinoma. Cancer Res 2003; 63: 7913-7919
52. Gill DS, Damle NK. Biopharmaceutical drug discovery using novel protein scaffolds. Curr Opin Biotechnol 2006; 17: 653-658
53. Long L, Rubin R, Baserga R, Brodt P. Loss of the metastatic phenotype in murine carcinoma cells expressing an antisense RNA to the insulin-like growth factor receptor. Cancer Res 1995; 55: 1006-1009
54. Bohula EA, Salisbury AJ, Sohail M, Playford MP, Riedemann J, Southern EM, Macaulay VM. The efficacy of small interfering RNAs targeted to the type 1 insulin-like growth factor receptor (IGF1R) is influenced by secondary structure in the IGF1R transcript. J Biol Chem 2003; 278: 15991-15997
55. Lee CT, Wu S, Gabrilovich D, Chen H, Nadaf-Rahrov S, Ciernik IF, Carbone DP. Antitumor effects of an adenovirus expressing antisense insulin-like growth factor I receptor on human lung cancer cell lines. Cancer Res 1996; 56: 3038-3041
56. Furukawa J, Wraight CJ, Freier SM, Peralta E, Atley LM, Monia BP, Gleave ME, Cox ME. Antisense oligonucleotide targeting of insulin-like growth factor-1 receptor (IGF-1R) in prostate cancer. Prostate 2010; 70: 206-218
57. Lee YJ, Imsumran A, Park MY, Kwon SY, Yoon HI, Lee JH, Yoo CG, Kim YW, Han SK, Shim YS, Piao W, Yamamoto H, Adachi Y, Carbone DP, Lee CT. Adenovirus expressing shRNA to IGF-1R enhances the chemosensitivity of lung cancer cell lines by blocking IGF-1 pathway. Lung Cancer 2007; 55: 279-286
58. Wang Y, Adachi Y, Imsumran A, Yamamoto H, Piao W, Li H, Ii M, Arimura Y, Park MY, Kim D, Lee CT, Carbone DP, Imai K, Shinomura Y. Targeting for insulin-like growth factor-I receptor with short hairpin RNA for human digestive/gastrointestinal cancers. J Gastroenterol 2010; 45: 159-170
59. Kull FC Jr, Jacobs S, Su YF, Svoboda ME, Van Wyk JJ, Cuatrecasas P. Monoclonal antibodies to receptors for insulin and somatomedin-C. J Biol Chem 1983; 258: 6561-6566
60. Arteaga CL, Kitten LJ, Coronado EB, Jacobs S, Kull FC Jr, Allred DC, Osborne CK. Blockade of the type I somatomedin receptor inhibits growth of human breast cancer cells in athymic mice. J Clin Invest 1989; 84: 1418-1423
61. Cohen BD, Baker DA, Soderstrom C, Tkalcevic G, Rossi AM, Miller PE, Tengowski MW, Wang F, Gualberto A, Beebe JS, Moyer JD. Combination therapy enhances the inhibition of tumor growth with the fully human anti-type 1 insulin-like growth factor receptor monoclonal antibody CP-751,871. Clin Cancer Res 2005; 11: 2063-2073
62. Wang Y, Hailey J, Williams D, Wang Y, Lipari P, Malkowski M, Wang X, Xie L, Li G, Saha D, Ling WL, Cannon-Carlson S, Greenberg R, Ramos RA, Shields R, Presta L, Brams P, Bishop WR, Pachter JA. Inhibition of insulin-like growth factor-I receptor (IGF-IR) signaling and tumor cell growth by a fully human neutralizing anti-IGF-IR antibody. Mol Cancer Ther 2005; 4: 1214-1221
63. Burtrum D, Zhu Z, Lu D, Anderson DM, Prewett M, Pereira DS, Bassi R, Abdullah R, Hooper AT, Koo H, Jimenez X, Johnson D, Apblett R, Kussie P, Bohlen P, Witte L, Hicklin DJ, Ludwig DL. A fully human monoclonal antibody to the insulin-like growth factor I receptor blocks ligand-dependent signaling and inhibits human tumor growth in vivo. Cancer Res 2003; 63: 8912-8921
64. Kurzrock R, Patnaik A, Aisner J, Warren T, Leong S, Benjamin R, Eckhardt SG, Eid JE, Greig G, Habben K, McCarthy CD, Gore L. A phase I study of weekly R1507, a human monoclonal antibody insulin-like growth factor-I receptor antagonist, in patients with advanced solid tumors. Clin Cancer Res 2010; 16: 2458-2465
65. Beltran PJ, Mitchell P, Chung YA, Cajulis E, Lu J, Belmontes B, Ho J, Tsai MM, Zhu M, Vonderfecht S, Baserga R, Kendall R, Radinsky R, Calzone FJ. AMG 479, a fully human anti-insulin- like growth factor receptor type I monoclonal antibody, inhibits the growth and survival of pancreatic carcinoma cells. Mol Cancer Ther 2009; Epub ahead of print
66. Goetsch L, Gonzalez A, Leger O, Beck A, Pauwels PJ, Haeuw JF, Corvaia N. A recombinant humanized anti-insulin-like growth factor receptor type I antibody (h7C10) enhances the antitumor activity of vinorelbine and anti-epidermal growth factor receptor therapy against human cancer xenografts. Int J Cancer 2005; 113: 316-328
67. Descamps G, Gomez-Bougie P, Venot C, Moreau P, Bataille R, Amiot M. A humanised anti-IGF-1R monoclonal antibody (AVE1642) enhances Bortezomib-induced apoptosis in myeloma cells lacking CD45. Br J Cancer 2009; 100: 366-369
68. Sachdev D, Yee D. Disrupting insulin-like growth factor signaling as a potential cancer therapy. Mol Cancer Ther 2007; 6: 1-12
69. Mitsiades CS, Mitsiades NS, McMullan CJ, Poulaki V, Shringarpure R, Akiyama M, Hideshima T, Chauhan D, Joseph M, Libermann TA, García-Echeverría C, Pearson MA, Hofmann F, Anderson KC, Kung AL. Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors. Cancer Cell 2004; 5: 221-230
70. García-Echeverría C, Pearson MA, Marti A, Meyer T, Mestan J, Zimmermann J, Gao J, Brueggen J, Capraro HG, Cozens R, Evans DB, Fabbro D, Furet P, Porta DG, Liebetanz J, Martiny-Baron G, Ruetz S, Hofmann F. In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell 2004; 5: 231-239
71. Liu TJ, LaFortune T, Honda T, Ohmori O, Hatakeyama S, Meyer T, Jackson D, de Groot J, Yung WK. Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation in vitro and in vivo. Mol Cancer Ther 2007; 6: 1357-1367
72. Wittman M, Carboni J, Attar R, Balasubramanian B, Balimane P, Brassil P, Beaulieu F, Chang C, Clarke W, Dell J, Eummer J, Frennesson D, Gottardis M, Greer A, Hansel S, Hurlburt W, Jacobson B, Krishnananthan S, Lee FY, Li A, Lin TA, Liu P, Ouellet C, Sang X, Saulnier MG, Stoffan K, Sun Y, Velaparthi U, Wong H, Yang Z, Zimmermann K, Zoeckler M, Vyas D. Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. J Med Chem 2005; 48: 5639-5643
73. Haluska P, Carboni JM, Loegering DA, Lee FY, Wittman M, Saulnier MG, Frennesson DB, Kalli KR, Conover CA, Attar RM, Kaufmann SH, Gottardis M, Erlichman C. In vitro and in vivo antitumor effects of the dual insulin-like growth factor-I/insulin receptor inhibitor, BMS-554417. Cancer Res 2006; 66: 362-371
74. Carboni JM, Wittman M, Yang Z, Lee F, Greer A, Hurlburt W, Hillerman S, Cao C, Cantor GH, Dell-John J, Chen C, Discenza L, Menard K, Li A, Trainor G, Vyas D, Kramer R, Attar RM, Gottardis MM. BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR. Mol Cancer Ther 2009; 8: 3341-3349
75. Pitts TM, Tan AC, Kulikowski GN, Tentler JJ, Brown AM, Flanigan SA, Leong S, Coldren CD, Hirsch FR, Varella-Garcia M, Korch C, Eckhardt SG. Development of an integrated genomic classifier for a novel agent in colorectal cancer: approach to individualized therapy in early development. Clin Cancer Res 2010; 16: 3193-3204
76. Pappano WN, Jung PM, Meulbroek JA, Wang YC, Hubbard RD, Zhang Q, Grudzien MM, Soni NB, Johnson EF, Sheppard GS, Donawho C, Buchanan FG, Davidsen SK, Bell RL, Wang J. Reversal of oncogene transformation and suppression of tumor growth by the novel IGF1R kinase inhibitor A-928605. BMC Cancer 2009; 9: 314
77. Li M, He Z, Ermakova S, Zheng D, Tang F, Cho YY, Zhu F, Ma WY, Sham Y, Rogozin EA, Bode AM, Cao Y, Dong Z. Di- rect inhibition of insulin-like growth factor-I receptor kinase activity by (-)-epigallocatechin-3-gallate regulates cell transformation. Cancer Epidemiol Biomarkers Prev 2007; 16: 598-605
78. Vasilcanu D, Girnita A, Girnita L, Vasilcanu R, Axelson M, Larsson O. The cyclolignan PPP induces activation loop-specific inhibition of tyrosine phosphorylation of the insulin-like growth factor-1 receptor. Link to the phosphatidyl inositol-3 kinase/Akt apoptotic pathway. Oncogene 2004; 23: 7854-7862
79. D'Ambrosio C, Ferber A, Resnicoff M, Baserga R. A soluble insulin-like growth factor I receptor that induces apoptosis of tumor cells in vivo and inhibits tumorigenesis. Cancer Res 1996; 56: 4013-4020
80. Dunn SE, Ehrlich M, Sharp NJ, Reiss K, Solomon G, Hawkins R, Baserga R, Barrett JC. A dominant negative mutant of the insulin-like growth factor-I receptor inhibits the adhesion, invasion, and metastasis of breast cancer. Cancer Res 1998; 58: 3353-3361
81. Prager D, Li HL, Asa S, Melmed S. Dominant negative inhibition of tumorigenesis in vivo by human insulin-like growth factor I receptor mutant. Proc Natl Acad Sci USA 1994; 91: 2181-2185
82. Li S, Resnicoff M, Baserga R. Effect of mutations at serines 1280-1283 on the mitogenic and transforming activities of the insulin-like growth factor I receptor. J Biol Chem 1996; 271: 12254-12260
83. Goya M, Miyamoto S, Nagai K, Ohki Y, Nakamura K, Shitara K, Maeda H, Sangai T, Kodama K, Endoh Y, Ishii G, Hasebe T, Yonou H, Hatano T, Ogawa Y, Ochiai A. Growth inhibition of human prostate cancer cells in human adult bone implanted into nonobese diabetic/severe combined immunodeficient mice by a ligand-specific antibody to human insulin-like growth factors. Cancer Res 2004; 64: 6252-6258
84. Miyamoto S, Nakamura M, Shitara K, Nakamura K, Ohki Y, Ishii G, Goya M, Kodama K, Sangai T, Maeda H, Shi-Chuang Z, Chiba T, Ochiai A. Blockade of paracrine supply of insulin-like growth factors using neutralizing antibodies suppresses the liver metastasis of human colorectal cancers. Clin Cancer Res 2005; 11: 3494-3502
85. Matsunaka T, Miyamoto S, Shitara K, Ochiai A, Chiba T. Ligand-specific antibodies to insulin-like growth factors suppress intestinal polyp formation in Apc+/- mice. Mol Cancer Ther 2010; 9: 419-428
86. Alami N, Page V, Yu Q, Jerome L, Paterson J, Shiry L, Leyland-Jones B. Recombinant human insulin-like growth factor-binding protein 3 inhibits tumor growth and targets the Akt pathway in lung and colon cancer models. Growth Horm IGF Res 2008; 18: 487-496
87. Russo VC, Gluckman PD, Feldman EL, Werther GA. The insulin-like growth factor system and its pleiotropic functions in brain. Endocr Rev 2005; 26: 916-943
88. Laustsen PG, Russell SJ, Cui L, Entingh-Pearsall A, Holzenberger M, Liao R, Kahn CR. Essential role of insulin and insulin-like growth factor 1 receptor signaling in cardiac development and function. Mol Cell Biol 2007; 27: 1649-1664
89. Sachdev D, Singh R, Fujita-Yamaguchi Y, Yee D. Downregulation of insulin receptor by antibodies against the type I insulin-like growth factor receptor: implications for antiinsulin- like growth factor therapy in breast cancer. Cancer Res 2006; 66: 2391-2402
90. Clemmons DR. Modifying IGF1 activity: an approach to treat endocrine disorders, atherosclerosis and cancer. Nat Rev Drug Discov 2007; 6: 821-833
91. Pan M, Santamaria M, Wollman DB. CNS response after erlotinib therapy in a patient with metastatic NSCLC with an EGFR mutation. Nat Clin Pract Oncol 2007; 4: 603-607
92. Kaaks R, Lukanova A. Energy balance and cancer: the role of insulin and insulin-like growth factor-I. Proc Nutr Soc 2001; 60: 91-106
93. de Bono JS, Attard G, Adjei A, Pollak MN, Fong PC, Haluska P, Roberts L, Melvin C, Repollet M, Chianese D, Connely M, Terstappen LW, Gualberto A. Potential applications for circulating tumor cells expressing the insulin-like growth factor-I receptor. Clin Cancer Res 2007; 13: 3611-3616
94. Tolcher AW, Sarantopoulos J, Patnaik A, Papadopoulos K, Lin CC, Rodon J, Murphy B, Roth B, McCaffery I, Gorski KS, Kaiser B, Zhu M, Deng H, Friberg G, Puzanov I. Phase I, pharmacokinetic, and pharmacodynamic study of AMG 479, a fully human monoclonal antibody to insulin-like growth factor receptor 1. J Clin Oncol 2009; 27: 5800-5807
95. Dunn SE, Hardman RA, Kari FW, Barrett JC. Insulin-like growth factor 1 (IGF-1) alters drug sensitivity of HBL100 human breast cancer cells by inhibition of apoptosis induced by diverse anticancer drugs. Cancer Res 1997; 57: 2687-2693
96. Trojanek J, Ho T, Del Valle L, Nowicki M, Wang JY, Lassak A, Peruzzi F, Khalili K, Skorski T, Reiss K. Role of the insulin- like growth factor I/insulin receptor substrate 1 axis in Rad51 trafficking and DNA repair by homologous recombination. Mol Cell Biol 2003; 23: 7510-7524
97. Lu Y, Zi X, Zhao Y, Mascarenhas D, Pollak M. Insulin-like growth factor-I receptor signaling and resistance to trastuzumab (Herceptin). J Natl Cancer Inst 2001; 93: 1852-1857
98. Nahta R, Yuan LX, Zhang B, Kobayashi R, Esteva FJ. Insulinlike growth factor-I receptor/human epidermal growth factor receptor 2 heterodimerization contributes to trastuzumab resistance of breast cancer cells. Cancer Res 2005; 65: 11118-11128
99. Chakravarti A, Loeffler JS, Dyson NJ. Insulin-like growth factor receptor I mediates resistance to anti-epidermal growth factor receptor therapy in primary human glioblastoma cells through continued activation of phosphoinositide 3-kinase signaling. Cancer Res 2002; 62: 200-207
100. Huang F, Greer A, Hurlburt W, Han X, Hafezi R, Wittenberg GM, Reeves K, Chen J, Robinson D, Li A, Lee FY, Gottardis MM, Clark E, Helman L, Attar RM, Dongre A, Carboni JM. The mechanisms of differential sensitivity to an insulin-like growth factor-1 receptor inhibitor (BMS-536924) and rationale for combining with EGFR/HER2 inhibitors. Cancer Res 2009; 69: 161-170