A novel, potent, and selective insulin-like growth factor-I receptor kinase inhibitor blocks insulin-like growth factor-I receptor signaling in vitro and inhibits insulin-like growth factor-I receptor-dependent tumor growth in vivo

Molecular Cancer Therapeutics

Volumn 6, Issue 8, 2007, Pages 2158-2167

  Ji, Qun Sheng ^a,b   Mulvihill, Mark J ^a   Rosenfeld Franklin, Maryland ^a   Cooke, Andrew ^a   Feng, Lixin ^a   Mak, Gilda ^a   O'Connor, Matthew ^a   Yao, Yan ^a   Pirritt, Caroline ^a   Buck, Elizabeth ^a   Eyzaguirre, Alexandra ^a   Arnold, Lee D ^a   Gibson, Neil W ^a   Pachter, Jonathan A ^a  

^a OSI PHARMACEUTICALS INC   (United States)

^b Department of Cancer Biology ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [3 (4 METHYLPIPERAZIN 1 YL)CYCLOBUTYL] 1 (2 PHENYLQUINOLIN 7 YL)IMIDAZO[1,5 A]PYRAZIN 8 YLAMINE; MITOGEN ACTIVATED PROTEIN KINASE; PHOSPHOTRANSFERASE INHIBITOR; SOMATOMEDIN RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; AUTOCRINE EFFECT; AUTOPHOSPHORYLATION; CANCER CELL CULTURE; COLORECTAL CANCER; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG HALF LIFE; ENZYME ACTIVITY; FEMALE; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; IN VIVO STUDY; MOUSE; NONHUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION;

ANIMALS; ANTINEOPLASTIC AGENTS; AUTOCRINE COMMUNICATION; BLOOD GLUCOSE; CELL LINE, TUMOR; CELL PROLIFERATION; COLORECTAL NEOPLASMS; ENZYME ACTIVATION; FEMALE; HUMANS; IMIDAZOLES; INSULIN-LIKE GROWTH FACTOR II; MICE; MICE, NUDE; PHOSPHORYLATION; PROTEIN KINASE INHIBITORS; PYRAZINES; RECEPTOR, IGF TYPE 1; SIGNAL TRANSDUCTION; TUMOR STEM CELL ASSAY; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 34548058890     PISSN: 15357163     EISSN: None     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-07-0070     Document Type: Article

References (49)

1. LeRoith D, Roberts CT, Jr. The insulin-like growth factor system and cancer. Cancer Lett 2003;195:127-37.
2. Ullrich A, Schlessiger J. Signal transduction by receptors tyrosine kinase activity. Cell 1990;61:203-12.
3. Baserga R, Peruzzi F, Reiss K. The IGF-1 receptor in cancer biology. Int J Cancer 2003;107:873-7.
4. Pollak MN, Schernhammer ES, Hankinson SE. Insulin-like growth factors and neoplasia. Nat Rev Cancer 2004;4:505-18.
5. Wang Y, Sun Y. Insulin-like growth factor receptor-1 as an anti-cancer target: blocking transformation and inducing apoptosis. Curr Cancer Drug Targets 2002;2:191-207.
6. Zhang H, Yee D. The therapeutic potential of agents targeting the type I insulin-like growth factor receptor. Expert Opin Investig Drugs 2004;13:1569-77.
7. Resnicoff M, Coppola D, Sell C, Rubin R, Ferrone S, Baserga R. Growth inhibition of human melanoma cells in nude mice byantisense strategies to type 1 insulin-like growth factor receptor. Cancer Res 1994;54:4848-50.
8. Chernicky CL, Yi L, Tan H, Gan SU, Ilan J. Treatment of human breast cancer cells with antisense RNA to the type I insulin-like growth factor receptor inhibits cell growth, suppresses tumourigenesis, alters the metastatic potential and prolongs survival in vivo. Cancer Gene Ther 2000;7:384-95.
9. Maloney EK, McLaughlin JL, Dagdigian NE, et al. An anti-insulin-like growth factor I receptor antibody that is a potent inhibitor of cancer cell proliferation. Cancer Res 2003;63:5073-83.
10. Wang Y, Hailey J, Williams D, et al. Inhibition of insulin-like growth factor-I receptor (IGF-1R) signaling and tumor cell growth by a fully human neutralizing anti-IGF-1R antibody. Mol Cancer Ther 2005;4:1214-21.
11. Cohen BD, Baker DA, Soderstrom C, et al. Combination therapy enhances the inhibition of tumor growth with the fully human anti-type 1 insulin-like factor receptor monoclonal antibody CP-751,871. Clin Cancer Res 2005;11:2063-73.
12. Goetsch L, Gonzalez A, Leger O, et al. 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;113:316-28.
13. Prager D, Li HL, Asa S, Melmed S. Dominant negative inhibition of tumourigenesis in vivo by human insulin-like growth factor I receptor mutant. Proc Natl Acad Sci U S A 1994;91:2181-5.
14. Kalebic T, Blakesley V, Slade C, Plasschaert S, Leroith D, Helman LJ. Expression of a kinase-deficient IGF-I-R suppresses tumorigenicity of rhabdomyosarcoma cells constitutively expressing a wild type IGF-I-R. Int J Cancer 1998;76:223-7.
15. Scotlandi K, Avnet S, Benini S, et al. Expression of an IGF-I receptor dominant negative mutant induces apoptosis, inhibits tumourigenesis and enhances chemosensitivity in Ewing's sarcoma cells. Int J Cancer 2002;101:11-6.
16. Garcia-Echeverria C, Pearson MA, Marti A, et al. In vivo antitumor activity of NVP-AEW541 - a novel, potent, and selective inhibitor of the IGF-1R kinase. Cancer Cell 2004;5:231-9.
17. Haluska P, Carboni JM, Loegering DA, et al. In vitro and in vivo antitumor effects of the dual insulin-like growth factor-I/insulin receptor inhibitor, BMS-554417. Cancer Res 2006;66:362-71.
18. Garcia-Echeverria C. Medicinal chemistry approaches to target the kinase activity of IGF-1R. IDrugs 2006;9:415-9.
19. Larsson O, Girnita A, Girnita L. Role of insulin-like growth factor I receptor signalling in cancer. Br J Cancer 2005;92:2097-101.
20. El-Badry OM, Helman LJ, Chatten J, et al. Insulin-like growth factor II-mediated proliferation of human neuroblastoma. J Clin Invest 1991;87:648-57.
21. Quinn KA, Treston AM, Unsworth EJ, et al. Insulin-like growth factor expression in human cancer cell lines. J Biol Chem 1996;271:11477-83.
22. Vella V, Pandini G, Sciacca L, et al. A novel autocrine loop involving IGF-II and the insulin receptor isoform-A stimulates growth of thyroid cancer. J Clin Endocrinol Metab 2002;87:245-54.
23. Qing RQ, Schmitt S, Ruelicke T, Stallmach T, Schoenle EJ. Autocrine regulation of growth by insulin-l ike growth factor (IGF)-II mediated by type I IGF-receptor in Wilms tumor cells. Pediatr Res 1996;39:160-5.
24. Ma J, Pollak MN, Giovannucci E, et al. Prospective studyof 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;91:620-5.
25. Chan JM, Stampfer MJ, Giovannucci E, et al. Plasma insulin-like growth factor-I and prostate cancer risk: a prospective study. Science 1998;279:563-6.
26. Hankinson SE, Willett WC, Colditz GA, et al. Circulating concentrations of insulin-like growth factor-I and risk of breast cancer. Lancet 1998;351:1393-6.
27. Yu H, Spitz MR, Mistry J, Gu J, Hong WK, Wu X. Plasma levels of insulin-like growth factor-I and lung cancer risk: a case-control analysis. J Natl Cancer Inst 1999;91:151-6.
28. Zhao H, Grossman HB, Spitz MR, Lerner SP, Zhang K, Wu X. Plasma levels of insulin-like growth factor-1 and binding protein-3, and their association with bladder cancer risk. J Urol 2003;169:714-7.
29. Parker AS, Cheville JC, Janney CA, Cerhan JR. High expression levels of insulin-like growth factor-I receptor predict poor survival among women with clear-cell renal cell carcinomas. Hum Pathol 2002;33:801-5.
30. 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;62:200-7.
31. Zhang L, Zhou W, Velculescu VE, et al. Gene expression profiles in normal and cancer cells. Science 1997;276:1268-71.
32. Hassan AB, Macaulay VM. The insulin-like growth factor system as a therapeutic target in colorectal cancer. Ann Oncol 2002;13:349-56.
33. Chen CL, Ip SM, Cheng D, Wong LC, Ngan HY. Loss of imprinting of the IGF-II and H19 genes in epithelial ovarian cancer. Clin Cancer Res 2000;6:474-9.
34. Kalli KR, Falowo OI, Bale LK, Zschunke MA, Roche PC, Conover CA. Functional insulin receptors on human epithelial ovarian carcinoma cells: implications for IGF-II mitogenic signaling. Endocrinology 2002;143:3259-67.
35. Kondo M, Suzuki H, Ueda R, et al. Frequent loss of imprinting of the H19 gene is often associated with its overexpression in human lung cancers. Oncogene 1995;10:1193-8.
36. Wang Z, Ruan YB, Guan Y, Liu SH. Expression of IGF-II in early experimental hepatocellular carcinomas and its significance in early diagnosis. World J Gastroenterol 2003;9:267-70.
37. Cui H, Cruz-Correa M, Giardiello FM, et al. Loss of IGF2 imprinting: a potential marker of colorectal cancer risk. Science 2003;299:1753-5.
38. Arnold LD, Cesario C, Coate H, et al. 6,6-Bicyclic ring substituted heterobicyclic protein kinase inhibitors. PCT International Patent Application WO 2005/097800A1.
39. Garton AJ, Crew AP, Franklin M, et al. OSI-930: a novel selective inhibitor of kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res 2006;66:1015-24.
40. Ji QS, Winnier GE, Niswender KD et al. Essential role of the tyrosine kinase substrate phospholipase C-γ1 in mammalian growth and development. Proc Natl Acad Sci U S A 1997;94:2999-3003.
41. Haluzik M, Yakar S, Gavrilova O, Setser J, Boisclair Y, LeRoith D. Insulin resistance in the liver-specific IGF-1 gene-deleted mouse is abrogated by deletion of the acid-labile subunit of the IGF-binding protein-3 complex: relative roles of growth hormone and IGF-1 in insulin resistance. Diabetes 2003;52:2483-9.
42. Duronio V. Insulin receptor is phosphorylated in response to treatment of HepG2 cells with insulin-like growth factor I. Biochem J 1990;270:27-32.
43. Hurbin A, Dubrez L, Coll JL, Favrot MC. Inhibition of apoptosis by amphiregulin via an insulin-like growth factor-1 receptor-dependent pathwayin non-small cell lung cancer cell lines. J Biol Chem 2002;277:49127-33.
44. Kaufmann SH, Desnoyers S, Ottaviano Y, Davidson NE, Poirier GG. Specific proteolytic cleavage of poly(ADP-ribose) polymerase: an early marker of chemotherapy-induced apoptosis. Cancer Res 1993;53:3976-85.
45. Hailey J, Maxwell E, Koukouras K, Bishop WR, Pachter JA, Wang Y. Neutralizing anti-insulin-like growth factor receptor 1 antibodies inhibit receptor function and induce receptor degradation in tumor cells. Mol Cancer Ther 2002;1:1349-53.
46. Lu Y, Zi X, Pollak M. Molecular mechanisms underlying IGF-I-induced attenuation of the growth-inhibitory activity of trastuzumab (Herceptin) on SKBR3 breast cancer cells. Int J Cancer 2004;108:334-41.
47. Beech DJ, Perer E, Helms J, Gratzer A, Deng N. Insulin-like growth factor-I receptor activation blocks doxorubicin cytotoxicity in sarcoma cells. Oncol Rep 2003;10:181-4.
48. Peretz S, Jensen R, Baserga R, Glazer PM. ATM-dependent expression of the insulin-like growth factor-I receptor in a pathway regulating radiation response. Proc Natl Acad Sci U S A 2001;98:1676-81.
49. Ji QS, Mak G, O'Connor M, et al. A novel IGF-1R small molecule inhibitor potentiates erlotinib activity in NSCLC cell lines in vitro and in vivo [abstract]. Proc Supplement AACR 2006;97:74.