Translating an antagonist of chemokine receptor CXCR4: From bench to bedside

Clinical Cancer Research

Volumn 14, Issue 24, 2008, Pages 7975-7980

  Wong, Donald ^a   Korz, Walter ^a  

^a Chemokine Therapeutics Corporation   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

8 [(4 AMINOBUTYL)(2 BENZIMIDAZOLYLMETHYL)AMINO] 1,2,3,4 TETRAHYDROQUINOLINE; ANTINEOPLASTIC AGENT; CHEMOKINE RECEPTOR CXCR4; CHEMOKINE RECEPTOR CXCR4 ANTAGONIST; CHEMOKINE RECEPTOR CXCR4 ANTIBODY; CTCE 9908; CYTARABINE; DOCETAXEL; ETOPOSIDE; FC 131; GEMCITABINE; MITOXANTRONE; MONOCLONAL ANTIBODY DC101; MSX 122; N [1,4,8,11 TETRAAZACYCLOTETRADECANYL 1,4 PHENYLENEBIS(METHYLENE)] 2 (AMINOMETHYL)PYRIDINE; NEUTRALIZING ANTIBODY; PACLITAXEL; PLERIXAFOR; RCP 168; RECEPTOR ANTIBODY; SMALL INTERFERING RNA; STROMAL CELL DERIVED FACTOR 1; T 140; T 22; TN 14003; UNCLASSIFIED DRUG; VASCULOTROPIN ANTIBODY; VASCULOTROPIN RECEPTOR 2 ANTIBODY; CXCL12 PROTEIN, HUMAN; CXCR4 PROTEIN, HUMAN;

ANTIANGIOGENIC ACTIVITY; ANTIANGIOGENIC THERAPY; BONE METASTASIS; BREAST CANCER; CANCER INHIBITION; CELL MIGRATION; CELL PROLIFERATION; CELL SURVIVAL; CHEMOEMBOLIZATION; CLINICAL TRIAL; DRUG POTENTIATION; GENETIC TRANSCRIPTION; GLIOBLASTOMA; HUMAN; LIVER CELL CARCINOMA; LUNG ADENOCARCINOMA; LUNG METASTASIS; METASTASIS; METASTASIS INHIBITION; NEOPLASM; NONHUMAN; OVARY CANCER; PERITONEUM METASTASIS; PHLEBITIS; PRIORITY JOURNAL; PROSTATE CANCER; PROTEIN EXPRESSION; PROTEIN FUNCTION; RECEPTOR DOWN REGULATION; REVIEW; SIGNAL TRANSDUCTION; TUMOR ESCAPE; TUMOR VASCULARIZATION; DRUG ANTAGONISM; PHYSIOLOGY;

CHEMOKINE CXCL12; HUMANS; RECEPTORS, CXCR4; SIGNAL TRANSDUCTION;

EID: 58149332686     PISSN: 10780432     EISSN: None     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-07-4846     Document Type: Review

References (67)

1. IUIS/WHO Subcommittee on Chemokine Nomenclature. Chemokine/chemokine receptor nomenclature. Cytokine 2003;21:48-9.
2. Yu L, Cecil J, Peng SB, et al. Identification and expression of novel isoforms of human stromal cell-derived factor1. Gene 2006;374:174-9.
3. Shirozu M, NakanoT, Inazawa J, et al. Structure and chromosomal localization of the human stromal cell-derived factor 1 (SDF1) gene. Genomics 1995;28: 495-500.
4. Nagasawa T, Hirota S,Tachibana K, et al. Defects of B-cell lymphopoiesis and bone-marrow myelopoiesis in mice lacking the CXC chemokine PBSF/SDF-1. Nature1996;382:635 -8.
5. Zou YR, Kottmann AH, Kuroda M,Taniuchi I, Littman DR. Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development. Nature 1998;393:595-9.
6. Tachibana K, Hirota S, Iizasa H, et al. The chemokine receptor CXCR4 is essential for vascularization of the gastrointestinal tract. Nature1998;393:591 -4.
7. Diaz GA, Gulino AV. WHIM syndrome: a defect in CXCR4 signaling. Curr Allergy Asthma Rep 2005;5: 350-5.
8. Percherancier Y, Berchiche YA, Slight I, et al. Biolumi-nescence resonance energy transfer reveals ligand-induced conformational changes in CXCR4homo- and heterodimers. J Biol Chem 2005;280:9895-903.
9. Vila-CoroAJ, Rodríguez-Frade JM, MartínDe Ana A, Moreno-OrtízMC,Martínez-AC, Mellado M. The chemokine SDF-1 αtriggers CXCR4 receptor dimerization and activates the JAK/STAT pathway. FASEB J 1999; 13:1699 -710.
10. Holland JD, Kochetkova M, Akekawatchai C, Dottore M, Lopez A, McColl SR. Differential functional activation of chemokine receptor CXCR4 is mediated by G proteins in breast cancer cells. Cancer Res 2006;66:4117 -24.
11. Ganju RK, Brubaker SA, Meyer J, et al. The α-chemokine, stromal cell-derived factor-1 α, binds to the transmembrane G-protein-coupled CXCR-4 receptor and activates multiple signal transduction pathways. J Biol Chem 1998;273:23169 -75.
12. Zhao M, Discipio RG,WimmerAG, Schraufstatter IU. Regulation of CXCR4-mediated nuclear translocation of extracellular signal-related kinases 1 and 2. Mol Pharmacol 2006;69:66 -75.
13. Busillo JM, Benovic JL. Regulation of CXCR4 signaling. Biochim Biophys Acta 2007;1768:952-63.
14. Chinni SR, Sivalogan S, Dong Z, et al. CXCL12/ CXCR4 signaling activates Akt-1 and MMP-9 expression in prostate cancer cells: the role of bone microen-vironment-associated CXCL12. Prostate 2006;66: 32 -48.
15. Barbieri F, Bajetto A, Porcile C, et al. CXC receptor and chemokine expression in human meningioma: SDF1/CXCR4 signaling activates ERK1/2 and stimulates meningioma cell proliferation. Ann N Y Acad Sci 2006;1090:332-43.
16. Barbero S, Bonavia R, Bajetto A, et al. Stromal cell-derived factor 1 α stimulates human glioblastoma cell growth through the activation of both extracellular signal-regulated kinases 1/2 and Akt. Cancer Res 2003;63:1969 -74.
17. Moriguchi M, Hissong BD, Gadina M, et al. CXCL12 signaling is independent of Jak2 and Jak3. J Biol Chem 2005;280:17408-14.
18. Cheng ZJ,Zhao J,Sun Y, et al. β-Arrestin differentially regulates the chemokine receptor CXCR4-mediated signaling and receptor internalization, and this implicates multiple interaction sites between β-arrestin and CXCR4. J Biol Chem 2000;275: 2479 -85.
19. Richardson RM,Tokunaga K, Marjoram R, SataT, Snyderman R. Interleukin-8-mediated heterologous receptor internalization provides resistance to HIV-1 infectivity. Role of signal strength and receptor desensitization. J Biol Chem 2003;278:15867 -73.
20. SloaneAJ, RasoV, Dimitrov DS, etal. Marked structural and functional heterogeneity in CXCR4: separation of HIV-1 and SDF-1 α responses. Immunol Cell Biol 2005;83:129-43.
21. Airoldi I, Raffaghello L, Piovan E, et al. CXCL12 does not attract CXCR4+ human metastatic neuroblastoma cells: clinical implications. Clin Cancer Res 2006;12: 77 -82.
22. Balkwill F. Cancer and the chemokine network. Nat Rev Cancer 2004;4:540-50.
23. Salvucci O, Bouchard A, Baccarelli A, et al. The role of CXCR4 receptor expression in breast cancer: a large tissue microarray study. Breast Cancer Res Treat 2006;97:275 -83.
24. Scotton CJ,WilsonJL,Milliken D,StampG,Balkwill FR. Epithelial cancer cell migration: a role for chemokine receptors? Cancer Res 2001;61:4961 -5.
25. SunYX,WangJ, Shelburne CE, et al. Expression of CXCR4 and CXCL12 (SDF-1) in human prostate cancers (PCa) in vivo. J Cell Biochem 2003;89:462-73.
26. Schimanski CC, Bahre R, Gockel I, et al. Dissemination of hepatocellular carcinoma is mediated via chemokine receptor CXCR4. Br J Cancer 2006;95: 210-7.
27. Pistoia V, Corcione A, Dallegri F, Ottonello L. Lym-phoproliferative disorders and chemokines. Curr Drug Targets 2006;7:81 -90.
28. Schioppa T, Uranchimeg B, Saccani A, et al. Regulation of the chemokine receptor CXCR4 by hypoxia. J Exp Med 2003;198:1391 -402.
29. Zagzag D, Lukyanov Y, Lan L, et al. Hypoxia-induc-ible factor 1 and VEGF up-regulate CXCR4 in glioblastoma: implications for angiogenesis and glioma cell invasion. Lab Invest 2006;86:1221 -32.
30. Kulbe H, Hagemann T, Szlosarek PW, Balkwill FR, Wilson JL. The inflammatory cytokine tumor necrosis factor-α regulates chemokine receptor expression on ovarian cancer cells. Cancer Res 2005; 65:10355 -62.
31. Müller A, Homey B, Soto H, et al. Involvement of chemokine receptors in breast cancer metastasis. Nature 2001;410:50-6.
32. Kim SY, Lee CH, Midura BV, et al. Inhibition of the CXCR4/CXCL12 chemokine pathway reduces the development of murine pulmonary metastases. Clin Exp Metastasis 2008;25:201 -11.
33. Wong D, Korz W, Merzouk A, Salari H. Apeptide antagonist of chemokine receptor CXCR4 reducestumor metastasis in a murine orthotopic model of human prostate cancer [abstract 2162]. AACR Annual Meeting 2006 Proceedings, vol. 47; April 2006.
34. Huang EH, Singh B, Cristofanilli M, et al. ACXCR4 antagonist CTCE-9908 inhibits primary tumor growth and metastasis of breast cancer. J Surg Res. In press 2008. doi:10.1016/j.jss.2008.06.044.
35. Leung E, Maksumova L, ZhaoY, Garcia L, Salari H, Abramovich C. Characterization of the anti-metastatic activity of a SDF-1 peptide analog in different tumor models [abstract 667]. AACR Annual Meeting 2007 Proceedings, vol. 48; April 2007.
36. Wong D, Korz W, Salari H. Anticancer effect of a combination of CXCR4 antagonist CTCE-9908 and Docetaxel in a murine model of human prostate cancer [abstract C20]. AACR/NCI/EORTC Molecular Targets and Cancer Therapeutics 2007 conference; October 2007.
37. Kok TW, Yang ZF, Poon RTP. Blockade of chemokine receptor CXCR4 for the treatment of hepatocellular carcinoma metastasis [abstract B223]. AACR/NCI/EORTC Molecular Targets and Cancer Therapeutics 2007 conference; October 2007.
38. Hassan S, Buchanan M, Salvucci O, Muller WJ, Basik M. Targeting CXCR4 inhibits primary tumor growth and distant metastasis in a transgenic breast cancer mouse model [abstract 1188]. AACR Annual Meeting 2008 Proceedings. Vol. 49; April 2008.
39. KajiyamaH,ShibataK,TerauchiM,InoK,NawaA, Kikkawa F. Involvement of SDF-1 α/CXCR4 axis in the enhanced peritoneal metastasis of epithelial ovarian carcinoma. IntJ Cancer 2008;122:91 -9.
40. Smith MC, Luker KE, GarbowJR, et al. CXCR4 regulates growth of both primary and metastatic breast cancer. Cancer Res 2004;64:8604-12.
41. Murakami T, Maki W, Cardones AR, et al. Expression of CXC chemokine receptor-4 enhances the pulmonary metastatic potential of murine B16 melanoma cells. Cancer Res 2002;62:7328-34.
42. Yoon Y, Liang Z, Zhang X, et al. CXC chemokine receptor-4 antagonist blocks both growth of primary tumor and metastasis of head and neck cancer in xenograft mouse models. Cancer Res 2007;67: 7518-24.
43. Sun YX, Schneider A, Jung Y. et al. Skeletal localization and neutralization of the SDF-1(CXCL12)/CXCR4 axis blocks prostate cancer metastasis and growth in osseous sites in vivo. J Bone Miner Res 2005;20: 318-29.
44. Huang YC, Hsiao YC, Chen YJ,Wei YY, Lai TH,Tang CH. Stromal cell-derived factor-1 enhances motility and integrin up-regulation through CXCR4, ERK and NF-κB-dependent pathway in human lung cancer cells. Biochem Pharmacol 2007;74:1702-12.
45. Zeng Z, Samudio IJ, Munsell M, et al. Inhibition of CXCR4 with the novel RCP168 peptide overcomes stroma-mediated chemoresistance in chronic and acute leukemias. Mol CancerTher 2006;5:3113 -21.
46. Burger M, Hartmann T, Krome M, et al. Small peptide inhibitors of the CXCR4 chemokine receptor (CD184) antagonize the activation, migration, and antiapoptotic responses of CXCL12 in chronic lymphocytic leukemia B cells. Blood 2005;106: 1824-30.
47. Yang L, Jackson E,Woerner BM, Perry A, Piwnica-Worms D, Rubin JB. Blocking CXCR4-mediated cyclic AMP suppression inhibits brain tumor growth in vivo. Cancer Res 2007;67:651 -8.
48. Yasumoto K, Koizumi K, Kawashima A, et al. Role of the CXCL12/CXCR4 axis in peritoneal carcinomatosis of gastric cancer. Cancer Res 2006;66:2181 -7.
49. Mirshahi F, Pourtau J, Li H, et al. SDF-1 activity on microvascular endothelial cells: consequences on angiogenesis in in vitro and in vivo models. Thromb Res 2000;99:587 -94.
50. GulengB,Tateishi K,OhtaM, et al. Blockade of the stromal cell-derived factor-1/CXCR4 axis attenuates in vivo tumor growth by inhibiting angiogenesis in a vascular endothelial growth factor-independent manner. Cancer Res 2005;65:5864-71.
51. Strieter RM, Belperio JA, Phillips RJ, Keane MP. CXC chemokines in angiogenesis of cancer. Semin Cancer Biol 2004;14:195 -200.
52. Petit I, Jin D, Rafii S. The SDF-1-CXCR4 signaling pathway: a molecular hub modulating neo-angiogen-esis. Trends Immunol 2007;28:299-307.
53. Naik RP, Jin D, Chuang E, et al. Circulating endothelial progenitor cells correlate to stage in patients with invasive breast cancer. Breast Cancer ResTreat 2008; 107:133-8.
54. Kaplan RN, Rutigliano D, Bomsztyk E, et al. Elevated levels of circulating bone marrow-derived hematopoietic progenitor cells in newly diagnosed breast cancer patients [abstract 4193]. AACR Annual Meeting 2008 Proceedings, vol. 49; April 2008.
55. Ho JW, Pang RW, Lau C, et al. Significanceofcir-culating endothelial progenitor cells in hepatocellular carcinoma. Hepatology 2006;44:836 -43.
56. Poon RT, Yang ZF, Li ML, Chu PW, Yu D, Fan ST. Blockade of therapy-induced acute recruitment of bone marrow-derived CXCR4+Flt-1 + hemangiocytes inhibits hypoxia-induced tumor angiogenesis in hepatocellular carcinoma [abstract 5323]. AACR Annual Meeting 2008 Proceedings, vol. 49; April 2008.
57. Aghi M, Cohen KS, Klein RJ, Scadden DT, Chiocca EA. Tumor stromal-derived factor-1 recruits vascular progenitors to mitotic neovasculature, where microenvironment influences their differentiated phenotypes. Cancer Res 2006;66:9054-64.
58. Shaked Y, Henke E, Roodhart JM, et al. Rapid chemotherapy-induced acute endothelial progenitor cell mobilization: implications for antiangiogenic drugs as chemosensitizing agents. Cancer Cell 2008;14: 263-73.
59. Batchelor TT, Sorensen AG, di Tomaso E, et al. AZD2171, a pan-VEGF receptor tyrosine kinase inhibitor, normalizes tumor vasculature and alleviates edema in glioblastoma patients. Cancer Cell 2007;11:83-95.
60. Kryczek I, Lange A, Mottram P, et al. CXCL12 and vascular endothelial growth factor synergistically induce neoangiogenesis in human ovarian cancers. Cancer Res 2005;65:465 -72.
61. Li YM, Pan Y, Wei Y, et al. Upregulation of CXCR4 is essential for HER2-mediated tumor metastasis. Cancer Cell 2004;6:459 -69.
62. Cabioglu N, Summy J, Miller C, et al. CXCL-12/stro-mal cell-derived factor-1 α transactivates HER2-neu in breast cancer cells by a novel pathway involving Src kinase activation. Cancer Res 2005;65:6493 -7.
63. Chinni SR,Yamamoto H, Dong Z, Sabbota A, Bonfil RD, Cher ML. CXCL12/CXCR4 transactivates HER2 in lipid rafts of prostate cancer cells and promotes growth of metastatic deposits in bone. Mol Cancer Res 2008;6:446-57.
64. A.W. Tolcher. AACR Annual Meeting 2008. Symposium: Translating the Molecular Biology of Metastasis to the Clinic, San Diego; April 15, 2008.
65. Hotte SJ, Hirte HW, Iacobucci A, et al. Final results of a PhaseI/II study of CTCE-9908, a novel anticancer agent that inhibits CXCR4, in patients with advanced solid cancers. [abstract 405] EORTC/NCI/AACR MolecularTargets and Cancer Therapeutics 2008 conference; October 2008. Eur J Cancer 2008;6:127.
66. Burger JA, Bürkle A. The CXCR4 chemokine receptor in acute and chronic leukaemia: a marrow homing receptor and potential therapeutic target. Br J Haematol 2007;137:288-96.
67. Zhang Y, Liang Z,Wu H, et al. MSX-122, an orally available small molecule targeting CXCR4, inhibitsprimary tumor growth in an orthotopic mouse model of lung cancer and improves the effect of paclitaxel [abstract 1190]. AACR Annual Meeting 2009 Proceedings.Vol. 49; April 2008.