SKLB1002, a novel potent inhibitor of VEGF receptor 2 signaling, inhibits angiogenesis and tumor growth in vivo

Clinical Cancer Research

Volumn 17, Issue 13, 2011, Pages 4439-4450

  Zhang, Shuang ^a   Cao, Zhixing ^a   Tian, Hongwei ^a   Shen, Guobo ^a   Ma, Yongping ^a   Xie, Huanzhang ^a   Liu, Yalin ^a   Zhao, Chengjian ^a   Deng, Senyi ^a   Yang, Yang ^a   Zheng, Renlin ^a   Li, Weiwei ^a   Zhang, Na ^a   Liu, Shengyong ^a   Wang, Wei ^a   Dai, Lixia ^a   Shi, Shuai ^a   Cheng, Lin ^a   Pan, Youli ^a   Feng, Shan ^a   Zhao, Xia ^b   Deng, Hongxin ^a   Yang, Shengyong ^a   Wei, Yuquan ^a   more..

^a SICHUAN UNIVERSITY   (China)

^b SICHUAN UNIVERSITY   (China)

Author keywords

[No Author keywords available]

Indexed keywords

ANGIOGENESIS INHIBITOR; FOCAL ADHESION KINASE; MITOGEN ACTIVATED PROTEIN KINASE; SKLB 1002; SUNITINIB; UNCLASSIFIED DRUG; VANDETANIB; VASCULOTROPIN INHIBITOR; VASCULOTROPIN RECEPTOR 2;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIANGIOGENIC ACTIVITY; ARTICLE; CANCER INHIBITION; CELL INVASION; CELL MIGRATION; CELL PROLIFERATION; CONTROLLED STUDY; CYTOTOXICITY; DRUG ACTIVITY; DRUG INHIBITION; ENZYME PHOSPHORYLATION; FEMALE; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MOUSE; NONHUMAN; PRIORITY JOURNAL; SIGNAL TRANSDUCTION; TUMOR XENOGRAFT; UMBILICAL VEIN ENDOTHELIAL CELL; ZEBRA FISH;

ANGIOGENESIS INHIBITORS; ANIMALS; APOPTOSIS; CELL LINE; CELL LINE, TUMOR; CELL MOVEMENT; CELL PROLIFERATION; ENDOTHELIAL CELLS; FEMALE; HEP G2 CELLS; HUMANS; MELANOMA, EXPERIMENTAL; MICE; MICE, NUDE; NEOPLASM INVASIVENESS; NEOPLASMS; NEOVASCULARIZATION, PATHOLOGIC; NEOVASCULARIZATION, PHYSIOLOGIC; SIGNAL TRANSDUCTION; TUMOR BURDEN; VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR-2; XENOGRAFT MODEL ANTITUMOR ASSAYS; ZEBRAFISH;

EID: 79960334843     PISSN: 10780432     EISSN: 15573265     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-10-3109     Document Type: Article

References (50)

1. Folkman J. Angiogenesis in cancer, vascular, rheumatoid and other disease. Nat Med 1995;1:27-31.
2. Carmeliet P, Jain RK. Angiogenesis in cancer and other diseases. Nature 2000;407:249-57.
3. Dvorak HF. Angiogenesis: update 2005. J Thromb Haemost 2005;3: 1835-42.
4. Ivy SP, Wick JY, Kaufman BM. An overview of small-molecule inhibitors of VEGFR signaling. Nat Rev Clin Oncol 2009;6:569-79.
5. Bergers G, Benjamin LE. Tumorigenesis and the angiogenic switch. Nat Rev Cancer 2003;3:401-10. (Pubitemid 37328844)
6. Folkman J. Role of angiogenesis in tumor growth and metastasis. Semin Oncol 2002;29:15-8.
7. Carmeliet P. VEGF as a key mediator of angiogenesis in cancer. Oncology 2005;69:4-10. (Pubitemid 41680947)
8. Ferrara N, Gerber HP, LeCouter J. The biology of VEGF and its receptors. Nat Med 2003;9:669-76. (Pubitemid 36749215)
9. Neufeldaname G, Cohena T, Gengrinovitcha S, Poltorak Z. Vascular endothelial growth factor (VEGF) and its receptors. FASEB J 1999;13:9-22. (Pubitemid 29038270)
10. Holmes K, Roberts OL, Thomas AM, Cross MJ. Vascular endothelial growth factor receptor-2:Structure, function, intracellular signalling and therapeutic inhibition. Cell Signal 2007;19:2003-12. (Pubitemid 47354167)
11. Olsson AK, Dimberg A, Kreuger J, Claesson-Welsh L. VEGF receptor signaling in control of vascular function. Nat Rev Mol Cell Biol 2006;7:359-71.
12. Meadows KN, Bryant P, Pumiglia K. Vascular endothelial growth factor induction of the angiogenic phenotype requires Ras activation. J Biol Chem 2001;276:49289-98.
13. Takahashi T, Ueno H, Shibuya M. VEGF activates protein kinase C-dependent, but Ras-independent Raf-MEK-MAP kinase pathway for DNA synthesis in primary endothelial cells. Oncogene 1999;18: 2221-30. (Pubitemid 29186923)
14. Ferrara N. Vascular endothelial growth factor as a target for anticancer therapy. Oncologist 2004;9:2-10. (Pubitemid 38747842)
15. Hanrahan EO, Heymach JV. Vascular endothelial growth factor receptor tyrosine kinase inhibitors vandetanib (ZD6474) and AZD2171 in lung cancer. Clin Cancer Res 2007;13:s4617-22.
16. Faivre S, Demetri G, Sargent W, Raymond E. Molecular basis for sunitinib efficacy and future clinical development. Nat Rev Drug Discov 2007;6:734-45. (Pubitemid 47338181)
17. Li WW, Chen JJ, Zheng RL, Zhang WQ, Cao ZX, Yang LL, et al. Taking quinazoline as a general support-nog to design potent and selective kinase inhibitors: application to FMS-like tyrosine kinase 3. Chem-MedChem 2010;5:513-16.
18. Jaffe EA, Nachman RL, Becker CG, Minick CR. Culture of human endothelial cells derived from umbilical veins. Identification by morphologic and immunologic criteria. J Clin Invest 1973;52: 2745-56.
19. Heo DS, Park JG, Hata K, Day R, Herberman RB, Whiteside TL. Evaluation of tetrazolium-based semiautomatic colorimetric assay for measurement of human antitumor cytotoxicity. Cancer Res 1990;50: 3681-90. (Pubitemid 20194116)
20. Timke C, Zieher H, Roth A, Hauser K, Lipson KE, Weber KJ, et al. Combination of vascular endothelial growth factor receptor/platelet-derived growth factor receptor inhibition markedly improves radiation tumor therapy. Clin Cancer Res 2008;14:2210-9. (Pubitemid 351551134)
21. Pang X, Yi Z, Zhang X, Sung B, Qu W, Lian X, et al. Acetyl-11-keto- β-boswellic acid inhibits prostate tumor growth by suppressing vascular endothelial growth factor receptor 2-mediated angiogenesis. Cancer Res 2009;69:5893-900.
22. Kimmel CB, Ballard WW, Kimmel SR, Ullmann B, Schilling TF. Stages of embryonic development of the zebrafish. Dev Dyn 1995;203:253-310.
23. Hans F, Dimitrov S. Histone H3 phosphorylation and cell division. Oncogene 2001;20:3021-27. (Pubitemid 32553556)
24. Blezinger P, Wang J, Gondo M, Quezada A, Mehrens D, French M, et al. Systemic inhibition of tumor growth and tumor metastases by intramuscular administration of the endostatin gene. Nat Biotechnol 1999;17:343-48. (Pubitemid 29166035)
25. Hoffmann J, Schirner M, Menrad A, Schneider MR. A highly sensitive model for quantification of in vivo tumor angiogenesis induced by alginate- encapsulated tumor cells. Cancer Res 1997;57:3847-51. (Pubitemid 27381234)
26. Luo J, Xia Q, Zhang R, Lv C, Zhang W, Wang Y, et al. Treatment of cancer with a novel dual-targeted conditionally replicative adenovirus armed with mda-7/IL-24 gene. Clin Cancer Res 2008;14:2450-7. (Pubitemid 351551080)
27. Wang H, Zhang J, Tian J, Qu B, Li T, Chen Y, et al. Using dual-tracer PET to predict the biologic behavior of human colorectal cancer. J Nucl Med 2009;50:1857-64.
28. Wang H, Liu B, Tian JH, Xu BX, Guan ZW, Qu BL, et al. Monitoring early responses to irradiation with dual-tracer micro-PET in dual-tumor bearing mice. World J Gastroenterol 2010;16:5416-23.
29. Liu J, Agarwal S. Mechanical signals activate vascular endothelial growth factor receptor-2 to upregulate endothelial cell proliferation during inflammation. J Immunol 2010;185:1215-21.
30. Takahashi T, Yamaguchi S, Chida K, Shibuya M. A single autophosphorylation site on KDR/Flk-1 is essential for VEGF-A-dependent activation of PLC-γ and DNA synthesis in vascular endothelial cells. EMBO J 2001;20:2768-78. (Pubitemid 32938560)
31. Eliceiri BP, Puente XS, Hood JD, Stupack DG, Schlaepfer DD, Huang XZ, et al. Src-mediated coupling of focal adhesion kinase to integrin alpha(v)beta5 in vascular endothelial growth factor signaling. J Cell Biol 2002;157:149-60.
32. Holmqvist K, Cross MJ, Rolny C, H€agerkvist R, Rahimi N, Matsumoto T, et al. The adaptor protein shb binds to tyrosine 1175 in vascular endothelial growth factor (VEGF) receptor-2 and regulates VEGF-dependent cellular migration. J Biol Chem 2004;279:22267-75. (Pubitemid 38679423)
33. Abedi H, Zachary I. Vascular endothelial growth factor stimulates tyrosine phosphorylation and recruitment to new focal adhesions of focal adhesion kinase and paxillin in endothelial cells. J Biol Chem 1997;272:15442-51. (Pubitemid 27255570)
34. Avraham HK, Lee TH, Koh Y, Kim TA, Jiang S, Sussman M, et al. Vascular endothelial growth factor regulates focal adhesion assembly in human brain microvascular endothelial cells through activation of the focal adhesion kinase and related adhesion focal tyrosine kinase. J Biol Chem 2003;278:36661-8. (Pubitemid 37139998)
35. Auerbach R, Lewis R, Shinners B, Kubai L, Akhtar N. Angiogenesis assays: a critical overview. Clin Chem 2003;49:32-40. (Pubitemid 36078551)
36. Zon LI, Peterson RT. In vivo drug discovery in the zebrafish. Nat Rev Drug Discov 2005;4:35-44.
37. Tran TC, Sneed B, Haider J, Blavo D, White A, Aiyejorun T, et al. Automated, quantitative screening assay for antiangiogenic compounds using transgenic zebrafish. Cancer Res 2007;67:11386-92. (Pubitemid 350248566)
38. Wu X, Zhong H, Song J, Damoiseaux R, Yang Z, Lin S. Mycophenolic acid is a potent inhibitor of angiogenesis. Arterioscler Thromb Vasc Biol 2006;26:2414-16. (Pubitemid 44465742)
39. Cross LM, Cook MA, Lin S, Chen JN, Rubinstein AL. Rapid analysis of angiogenesis drugs in a live fluorescent zebrafish assay. Arterioscler Thromb Vasc Biol 2003;23:911-12. (Pubitemid 36566186)
40. Habeck H, Odenthal J, Walderich B, Maischein H, Schulte-Merker S. T€ubingen 2000 Screen Consortium. Analysis of a zebrafish VEGF receptor mutant reveals specific disruption of angiogenesis. Curr Biol 2002;12:1405-12.
41. Nicoli S, Ribatti D, Cotelli F, Presta M. Mammalian tumor xenografts induce neovascularization in zebrafish embryos. Cancer Res 2007;67:2927-31. (Pubitemid 46724826)
42. Stoletov K, Montel V, Lester RD, Gonias SL, Klemke R. High-resolution imaging of the dynamic tumor cell-vascular interface in transparent zebrafish. Proc Natl Acad Sci U S A 2007;104:17406-11. (Pubitemid 350219851)
43. Fogh J, Fogh JM, Orfeo T. One hundred and twenty-seven cultured human tumor cell lines producing tumors in nude mice. J Natl Cancer Inst 1977;59:221-26. (Pubitemid 8144854)
44. Rubenstein JL, Kim J, Ozawa T, Zhang M, Westphal M, Deen DF,, et al. Anti-VEGF antibody treatment of glioblastoma prolongs survival but results in increased vascular cooption. Neoplasia 2000; 2:306-14.
45. Liu L, Cao Y, Chen C, Zhang X, McNabola A, Wilkie D, et al. Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5. Cancer Res 2006;66:11851-8. (Pubitemid 46094197)
46. Faivre S, Delbaldo C, Vera K, Robert C, Lozahic S, Lassau N, et al. Safety, pharmacokinetic, and antitumor activity of SU11248, a novel oral multitarget tyrosine kinase inhibitor, in patients with cancer. J Clin Oncol 2006;24:25-35. (Pubitemid 46630490)
47. Abou-Alfa GK, Schwartz L, Ricci S, Amadori D, Santoro A, Figer A, et al. Phase II study of sorafenib in patients with advanced hepatocellular carcinoma. J Clin Oncol 2006;24:4293-300. (Pubitemid 46630787)
48. Drevs J, Siegert P, Medinger M, Mross K, Strecker R, Zirrgiebel U, et al. Phase I clinical study of AZD2171, an oral vascular endothelial growth factor signaling inhibitor, in patients with advanced solid tumors. J Clin Oncol 2007;25:3045-54. (Pubitemid 47218051)
49. Eskens FA, Verweij J. The clinical toxicity profile of vascular endothelial growth factor (VEGF) and vascular endothelial growth factor receptor (VEGFR) targeting angiogenesis inhibitors; a review. Eur J Cancer 2006;42:3127-39. (Pubitemid 44869016)
50. Verheul HM, Pinedo HM. Possible molecular mechanisms involved in the toxicity of angiogenesis inhibition. Nat Rev Cancer 2007;7: 475-85. (Pubitemid 46809172)