Advances in targeting Src in the treatment of breast cancer and other solid malignancies

Clinical Cancer Research

Volumn 16, Issue 14, 2010, Pages 3526-3532

  Mayer, Erica L ^a   Krop, Ian E ^a  

^a DANA FARBER CANCER INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; AZM 475271; BEVACIZUMAB; BISPHOSPHONIC ACID DERIVATIVE; BOSUTINIB; CAPECITABINE; CARBOPLATIN; CETUXIMAB; DASATINIB; DOCETAXEL; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; ESTROGEN RECEPTOR; EXEMESTANE; FLUOROURACIL; FOLINIC ACID; GEFITINIB; GEMCITABINE; LETROZOLE; N (5 CHLORO 1,3 BENZODIOXOL 4 YL) 7 [2 (4 METHYL 1 PIPERAZINYL)ETHOXY] 5 (TETRAHYDRO 2H PYRAN 4 YLOXY) 4 QUINAZOLINAMINE; OXALIPLATIN; PACLITAXEL; PROTEIN TYROSINE KINASE; PROTEIN TYROSINE KINASE INHIBITOR; TRASTUZUMAB; UNCLASSIFIED DRUG; VASCULOTROPIN; XL 999;

ACUTE LYMPHOBLASTIC LEUKEMIA; ANGIOGENESIS; ANOREXIA; ANTINEOPLASTIC ACTIVITY; BONE METASTASIS; BREAST CANCER; BREAST CELL; CANCER CELL; CANCER INHIBITION; CELL ADHESION; CELL FUNCTION; CELL GROWTH; CELL INVASION; CELL MIGRATION; CELL SURVIVAL; CHEMOTHERAPY INDUCED EMESIS; CHRONIC MYELOID LEUKEMIA; CLINICAL TRIAL; COLON CANCER; DIARRHEA; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG DOSE ESCALATION; DRUG DOSE REDUCTION; DRUG POTENTIATION; DRUG TOLERABILITY; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME REGULATION; FATIGUE; GASTROINTESTINAL TOXICITY; HUMAN; LUNG NON SMALL CELL CANCER; LUNG SMALL CELL CANCER; LUNG SQUAMOUS CELL CARCINOMA; MELANOMA; METASTASIS; MONOTHERAPY; NAUSEA; OVARY CANCER; PANCREAS CANCER; PHILADELPHIA CHROMOSOME POSITIVE CELL; PLEURA EFFUSION; PRIORITY JOURNAL; PROGRESSION FREE SURVIVAL; PROSTATE CANCER; PROTEIN PHOSPHORYLATION; PROTEIN PROTEIN INTERACTION; REVIEW; SIGNAL TRANSDUCTION; SOLID TUMOR; TREATMENT RESPONSE;

ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; BREAST NEOPLASMS; FEMALE; HUMANS; MALE; NEOVASCULARIZATION, PATHOLOGIC; PROSTATIC NEOPLASMS; PROTEIN KINASE INHIBITORS; SRC-FAMILY KINASES;

EID: 77954690732     PISSN: 10780432     EISSN: 15573265     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-09-1834     Document Type: Review

References (70)

1. Summy JM, Gallick GE. Src family kinases in tumor progression and metastasis. Cancer Metastasis Rev 2003;22:337-58.
2. Parsons SJ, Parsons JT. Src family kinases, key regulators of signal transduction. Oncogene 2004;23:7906-9.
3. Belsches-Jablonski AP, Biscardi JS, Peavy DR, et al. Src family kinases and HER2 interactions in human breast cancer cell growth and survival. Oncogene 2001;20:1465-75.
4. Lesslie DP, Summy JM, Parikh NU, et al. Vascular endothelial growth factor receptor-1 mediates migration of human colorectal carcinoma cells by activation of Src family kinases. Br J Cancer 2006;94:1710-7.
5. Thomas SM, Brugge JS. Cellular functions regulated by Src family kinases. Annu Rev Cell Dev Biol 1997;13:513-609.
6. Roche S, Fumagalli S, Courtneidge SA. Requirement for Src family protein tyrosine kinases in G2 for fibroblast cell division. Science 1995;269:1567-9.
7. Brown MT, Cooper JA. Regulation, substrates and functions of src. Biochim Biophys Acta 1996;1287:121-49.
8. Miyazaki T, Sanjay A, Neff L, et al. Src kinase activity is essential for osteoclast function. J Biol Chem 2004;279:17660-6. (Pubitemid 38560531)
9. Boyce BF, Yoneda T, Lowe C, et al. Requirement of pp60c-src expression for osteoclasts to form ruffled borders and resorb bone in mice. J Clin Invest 1992;90:1622-7.
10. Soriano P, Montgomery C, Geske R, Bradley A. Targeted disruption of the c-src proto-oncogene leads to osteopetrosis in mice. Cell 1991;64:693-702. (Pubitemid 121001157)
11. Irby RB, Yeatman TJ. Role of Src expression and activation in human cancer. Oncogene 2000;19:5636-42.
12. Tatarov O, Mitchell TJ, Seywright M, et al. SRC family kinase activity is up-regulated in hormone-refractory prostate cancer. Clin Cancer Res 2009;15:3540-9.
13. Verbeek BS, Vroom TM, Adriaansen-Slot SS, et al. c-Src protein expression is increased in human breast cancer. An immunohistochemical and biochemical analysis. J Pathol 1996;180:383-8.
14. Cartwright CA, Eckhart W, Simon S, Kaplan PL. Cell transformation by pp60c-src mutated in the carboxy-terminal regulatory domain. Cell 1987;49:83-91.
15. Avizienyte E, Frame MC. Src and FAK signalling controls adhesion fate and the epithelial-to-mesenchymal transition. Curr Opin Cell Biol 2005;17:542-7. (Pubitemid 41267169)
16. Myoui A, Nishimura R, Williams PJ, et al. C-SRC tyrosine kinase activity is associated with tumor colonization in bone and lung in an animal model of human breast cancer metastasis. Cancer Res 2003;63:5028-33. (Pubitemid 37022641)
17. Park SI, Zhang J, Phillips KA, et al. Targeting SRC family kinases inhibits growth and lymph node metastases of prostate cancer in an orthotopic nude mouse model. Cancer Res 2008;68:3323-33.
18. Lombardo LJ, Lee FY, Chen P, et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem 2004;47:6658-61.
19. Schittenhelm MM, Shiraga S, Schroeder A, et al. Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies. Cancer Res 2006;66:473-81.
20. Talpaz M, Shah NP, Kantarjian H, et al. Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N Engl J Med 2006;354:2531-41.
21. Bantscheff M, Eberhard D, Abraham Y, et al. Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors. Nat Biotechnol 2007;25:1035-44.
22. Nam S, Kim D, Cheng JQ, et al. Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. Cancer Res 2005;65:9185-9. (Pubitemid 41507982)
23. Finn RS, Dering J, Ginther C, et al. Dasatinib, an orally active small molecule inhibitor of both the src and abl kinases, selectively inhibits growth of basal-type/"triple-negative" breast cancer cell lines growing in vitro. Breast Cancer Res Treat 2007;105:319-26.
24. Jallal H, Valentino ML, Chen G, et al. A Src/Abl kinase inhibitor, SKI-606, blocks breast cancer invasion, growth, and metastasis in vitro and in vivo. Cancer Res 2007;67:1580-8. (Pubitemid 46383382)
25. Nautiyal J, Majumder P, Patel BB, et al. Src inhibitor dasatinib inhibits growth of breast cancer cells by modulating EGFR signaling. Cancer Lett 2009;283:143-51.
26. Song L, Morris M, Bagui T, et al. Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res 2006;66:5542-8. (Pubitemid 43927102)
27. Messersmith WA, Rajeshkumar NV, Tan AC, et al. Efficacy and pharmacodynamic effects of bosutinib (SKI-606), a Src/Abl inhibitor, in freshly generated human pancreas cancer xenografts. Mol Cancer Ther 2009;8:1484-93.
28. Golas JM, Lucas J, Etienne C, et al. SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res 2005;65:5358-64.
29. Weis S, Cui J, Barnes L, Cheresh D. Endothelial barrier disruption by VEGF-mediated Src activity potentiates tumor cell extravasation and metastasis. J Cell Biol 2004;167:223-9. (Pubitemid 39435066)
30. Migliaccio A, Di Domenico M, Castoria G, et al. Tyrosine kinase/p21ras/MAP-kinase pathway activation by estradiol-receptor complex in MCF-7 cells. EMBO J 1996;15:1292-300. (Pubitemid 26093465)
31. Varricchio L, Migliaccio A, Castoria G, et al. Inhibition of estradiol receptor/Src association and cell growth by an estradiol receptor alpha tyrosine-phosphorylated peptide. Mol Cancer Res 2007;5:1213-21. (Pubitemid 350137116)
32. Hiscox S, Morgan L, Green TP, et al. Elevated Src activity promotes cellular invasion and motility in tamoxifen resistant breast cancer cells. Breast Cancer Res Treat 2006;97:263-74. (Pubitemid 43945756)
33. Riggins RB, Thomas KS, Ta HQ, et al. Physical and functional interactions between Cas and c-Src induce tamoxifen resistance of breast cancer cells through pathways involving epidermal growth factor receptor and signal transducer and activator of transcription 5b. Cancer Res 2006;66:7007-15.
34. Unni E, Sun S, Nan B, et al. Changes in androgen receptor nongenotropic signaling correlate with transition of LNCaP cells to androgen independence. Cancer Res 2004;64:7156-68. (Pubitemid 39331031)
35. Mendiratta P, Mostaghel E, Guinney J, et al. Genomic strategy for targeting therapy in castration-resistant prostate cancer. J Clin Oncol 2009;27:2022-9.
36. Yang JC, Ok JH, Busby JE, et al. Aberrant activation of androgen receptor in a new neuropeptide-autocrine model of androgen-insensitive prostate cancer. Cancer Res 2009;69:151-60.
37. Hiscox S, Jordan NJ, Smith C, et al. Dual targeting of Src and ER prevents acquired antihormone resistance in breast cancer cells. Breast Cancer Res Treat 2009;115:57-67.
38. Chen Y, Guggisberg N, Jorda M, et al. Combined Src and aromatase inhibition impairs human breast cancer growth in vivo and bypass pathways are activated in AZD0530-resistant tumors. Clin Cancer Res 2009;15:3396-405.
39. Muthuswamy SK, Siegel PM, Dankort DL, et al. Mammary tumors expressing the neu proto-oncogene possess elevated c-Src tyrosine kinase activity. Mol Cell Biol 1994;14:735-43.
40. Marcotte R, Zhou L, Kim H, et al. c-Src associates with ErbB2 through an interaction between catalytic domains and confers enhanced transforming potential. Mol Cell Biol 2009;29:5858-71.
41. Tan M, Li P, Klos KS, et al. ErbB2 promotes Src synthesis and stability: novel mechanisms of Src activation that confer breast cancer metastasis. Cancer Res 2005;65:1858-67. (Pubitemid 40478614)
42. Zhuang G, Brantley-Sieders DM, Vaught D, et al. Elevation of receptor tyrosine kinase EphA2 mediates resistance to trastuzumab therapy. Cancer Res 2010;70:299-308.
43. Wang SE, Xiang B, Zent R, et al. Transforming growth factor beta induces clustering of HER2 and integrins by activating Src-focal adhesion kinase and receptor association to the cytoskeleton. Cancer Res 2009;69:475-82.
44. Seoane S, Montero JC, Pandiella A, Ocana A. Effect of dasatinib on the activity of trastuzumab in HER2-overexpressing breast cancer cells. J Clin Oncol 2009;27:1084.
45. Demetri GD, Lo Russo P, MacPherson IR, et al. Phase I dose-escalation and pharmacokinetic study of dasatinib in patients with advanced solid tumors. Clin Cancer Res 2009;15:6232-40.
46. Johnson FM, Agrawal S, Burris H, et al. Phase 1 pharmacokinetic and drug-interaction study of dasatinib in patients with advanced solid tumors. Cancer 2010;116:1582-91.
47. Messersmith WA, Krishnamurthi S, Hewes BA, et al. Bosutinib (SKI-606), a dual Src/Abl tyrosine kinase inhibitor: Preliminary results from a phase 1 study in patients with advanced malignant solid tumors. J Clin Oncol 2007;25:3552.
48. Luo F, Barrett Y, Ji P, et al. Dasatinib (BMS-354825) pharmacokinetics correlate with pSRC pharmacodynamics in phase I studies of patients with cancer (CA180002, CA180003). J Clin Oncol 2006;24:3046.
49. Campone M, Bondarenko I, Brincat S, et al. Preliminary results of a phase 2 study of bosutinib (SKI-606), a dual Src/Abl kinase inhibitor, in patients with advanced breast cancer. Breast Cancer Res Treat 2007;106:6062.
50. Finn R, Bengala C, Ibrahim N, et al. Phase II trial of dasatinib in triple-negative breast cancer: results of study CA180059. Cancer Res 2009;69:3118.
51. Mayer E, Baurain J, Sparano J, et al. Dasatinib in advanced HER2/neu amplified and ER/PR-positive breast cancer: Phase II study CA180088. J Clin Oncol 2009;27:1011.
52. Strauss L, Sy O, Fairchild J, et al. Biomarker analyses in phase 2 single-agent trials of dasatinib for breast cancer. Cancer Res 2009;69:2034.
53. Ischenko I, Camaj P, Seeliger H, et al. Inhibition of Src tyrosine kinase reverts chemoresistance toward 5-fluorouracil in human pancreatic carcinoma cells: an involvement of epidermal growth factor receptor signaling. Oncogene 2008;27:7212-22.
54. Cortes J, Specht J, Gradishar W, et al. Dasatinib plus capecitabine for advanced breast cancer: safety and efficacy data from phase 1 study CA180-004. Cancer Res 2009;69:3092.
55. Morris P, Abbruzzi A, Chang J, et al. A phase i study of dasatinib (D) in Combination with Weekly (w) Paclitaxel (P) for patients (pts) with metastatic breast carcinoma (MBC): activity despite prior taxane exposure. Cancer Res 2009;69:5070.
56. Yu EY, Wilding G, Posadas E, et al. Phase II study of dasatinib in patients with metastatic castration-resistant prostate cancer. Clin Cancer Res 2009;15:7421-8.
57. Araujo J, Armstrong A, Braud E, et al. Dasatinib and docetaxel combination treatment for patients with castration-resistant progressive prostate cancer: A phase I/II study (CA180086). J Clin Oncol 2009;27:5061.
58. Miller AA, Pang H, Hodgson L, et al. A phase II study of dasatinib in patients with chemosensitive relapsed small cell lung cancer (Cancer and Leukemia Group B 30602). J Thorac Oncol 2010;5:380-4.
59. Kluger H, Dudek A, McCann C, et al. A phase II trial of dasatinib in advanced melanoma. J Clin Oncol 2009;27:9010.
60. Haura EB, Tanvetyanon T, Chiappori A, et al. Phase I/II study of the Src inhibitor dasatinib in combination with erlotinib in advanced nonsmall-cell lung cancer. J Clin Oncol 2010;28:1387-94.
61. Lieu CH, Wolff RA, Eng C, et al. Phase IB study of the Src inhibitor dasatinib with FOLFOX and cetuximab in metastatic colorectal cancer. J Clin Oncol 2010;28:3536.
62. Mukhopadhyay D, Tsiokas L, Zhou XM, et al. Hypoxic induction of human vascular endothelial growth factor expression through c-Src activation. Nature 1995;375:577-81.
63. Ellis LM, Staley CA, Liu W, et al. Down-regulation of vascular endothelial growth factor in a human colon carcinoma cell line transfected with an antisense expression vector specific for c-src. J Biol Chem 1998;273:1052-7. (Pubitemid 28049203)
64. Eliceiri BP, Paul R, Schwartzberg PL, et al. Selective requirement for Src kinases during VEGF-induced angiogenesis and vascular permeability. Mol Cell 1999;4:915-24. (Pubitemid 30054898)
65. Doukas J, Mahesh S, Umeda N, et al. Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. J Cell Physiol 2008;216:29-37.
66. Denduluri N, Yang SX, Berman AW, et al. Circulating biomarkers of bevacizumab activity in patients with breast cancer. Cancer Biol Ther 2008;7:15-20.
67. Sos ML, Michel K, Zander T, et al. Predicting drug susceptibility of non-small cell lung cancers based on genetic lesions. J Clin Invest 2009;119:1727-40.
68. Bild AH, Yao G, Chang JT, et al. Oncogenic pathway signatures in human cancers as a guide to targeted therapies. Nature 2006;439:353-7.
69. Lara PN, Jr., Longmate J, Evans CP, et al. A phase II trial of the Src-kinase inhibitor AZD0530 in patients with advanced castration-resistant prostate cancer: a California Cancer Consortium study. Anticancer Drugs 2009;20:179-84.
70. Nallapareddy S, Arcaroli J, Touban B, et al. A phase II trial of saracatinib (AZD0530), an oral Src inhibitor, in previously treated metastatic pancreatic cancer [abstract]. Proceedings of ASCO Gastrointestinal Cancers Symposium 2010. Orlando (FL): January 23, 2010, p. Abstract nr 165.