Effect of targeting janus kinase 3 on the development of intestinal tumors in the Adenomatous Polyposis Colimin mouse model of familial adenomatous polyposis

Arzneimittel-Forschung/Drug Research

Volumn 57, Issue 6, 2007, Pages 320-329

  Uckun, Fatih M ^a,b   Erbeck, Douglas ^b   Qazi, Sanjive ^a,b   Venkatachalam, Taracad ^b   Tibbles, Heather E ^b   Vassilev, Alexei ^b  

^a Parker Hughes Cancer Center   (United States)

^b Paradigm Pharmaceuticals   (United States)

Author keywords

4 (4 Hydroxyphenyl) amino 6,7 dimethoxyquinazoline; Adenomatous polyposis coli; CAS 202475 60 3; Chemopreventive agents; Familial adenomatous polyposis; JANEX 1, effects on intestinal tumors, mouse; Janus kinase 3 inhibitors; WHI P131

Indexed keywords

2,5 DIOXOPYRROLIDINYL 3 [[5 HYDROXY 3 (4 METHOXYPHENYL) 4 OXO 3H CHROMEN 7 YL]OXOSULFONYL]BENZOATE; 4 (4 HYDROXYANILINO) 6,7 DIMETHOXYQUINAZOLINE; BETA CATENIN; CURCUMIN; DDE 24; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; UNCLASSIFIED DRUG;

ADENOMATOUS POLYP; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CARCINOGENESIS; COLON POLYPOSIS; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG MECHANISM; DRUG TARGETING; DRUG TISSUE LEVEL; FEEDING; INTESTINE TUMOR; MOUSE; NONHUMAN; OUTCOME ASSESSMENT; SURVIVAL RATE;

EID: 34447300198     PISSN: 00044172     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0031-1296626     Document Type: Article

References (81)

1. Hisamuddin IM, Yang VW. Genetics of colorectal cancer. MedGenMed. 2004 Sep 13;6(3):13.
2. Peek RM, Jr. Prevention of colorectal cancer through the use of COX-2 selective inhibitors. Cancer Chemother Pharmacol. 2004 Sep 7.
3. Plasilova M, Russell AM, Wanner A, Wolf A, Dobbie Z, Muller HJ, et al. Exclusion of an extracolonic disease modifier locus on chromosome 1p33-36 in a large Swiss familial adenomatous polyposis kindred. Eur J Hum Genet. 2004 Jun;12(5):365-71.
4. Lynch HT, Tinley ST, Shaw TG, Lynch JF, Howe JR, Attard TM. Challenging colonic polyposis pedigrees: differential diagnosis, surveillance, and management concerns. Cancer Genet Cytogenet. 2004 Feb 15;148(2):104-17.
5. Church J, Kiringoda R, LaGuardia L. Inherited colorectal cancer registries in the United States. Dis Colon Rectum. 2004 Jun;47(5):674-8.
6. Boman BM, Walters R, Fields JZ, Kovatich AJ, Zhang T, Isenberg GA, et al. Colonic Crypt Changes during Adenoma Development in Familial Adenomatous Polyposis: Immunohistochemical Evidence for Expansion of the Crypt Base Cell Population. Am J Pathol. 2004 Dec;165(5):1489-98.
7. Bisgaard ML, Ripa R, Knudsen AL, Bulow S. Familial adenomatous polyposis patients without an identified APC germline mutation have a severe phenotype. Gut. 2004 Mar;53(2):266-70.
8. Friedrich A, Kullmann F. [Familial adenomatous polyposis syndrome (FAP): pathogenesis and molecular mechanisms]. Med Klin (Munich). 2003 Dec 15;98(12):776-82.
9. du Sart D. APC gene and familial adenomatous polyposis. J Gastroenterol Hepatol. 2004 Jun;19(5):598.
10. Ahnen D. The Molecular Basis of Colorectal Cancer Risk. In: Grunberg S, editor. 2005 Gastrointestinal Cancers Symposium: Multidisciplinary Approaches to Gastrointestinal Malignancies and Premalignancies; 2005; Hollywood, Florida: American Society of Clinical Oncology; 2005. p. 66-7.
11. Hulit J, Wang C, Li Z, Albanese C, Rao M, Di Vizio D, et al. Cyclin D1 genetic heterozygosity regulates colonic epithelial cell differentiation and tumor number in ApcMin mice. Mol Cell Biol. 2004 Oct;24(17):7598-611.
12. Choi J, Park SY, Costantini F, Jho EH, Joo CK. APC is downregulated by the ubiquitin-proteasome pathway in a process facilitated by Axin. J Biol Chem. 2004 Oct 7.
13. Boland CR. The Use of Microsatellite Instability in Making Treatment Decisions for Colorectal Cancer. In: Grunberg S, editor. 2005 Gastrointestinal Cancers Symposium: Multidisciplinary Approaches to Gastrointestinal Malignancies and Premalignancies; 2005: Hollywood, FL; 2005. p. 76.
14. Su LK, Kinzler KW, Vogelstein B, Preisinger AC, Moser AR, Luongo C, et al. Multiple intestinal neoplasia caused by a mutation in the murine homolog of the APC gene. Science. 1992 Jun 1;256(5057):668-70.
15. Moser AR, Pitot HC, Dove WF. A dominant mutation that predisposes to multiple intestinal neoplasia in the mouse. Science. 1990 Feb 19;247(4940):322-4.
16. Wilks AF, Harpur AG, Kurban RR, Ralph SJ, Zurcher G, Ziemiecki A. Two novel protein-tyrosine kinases, each with a second phosphotransferase-related catalytic domain, define a new class of protein kinase. Mol Cell Biol. 1991;11(4):2057-65.
17. Harpur AG, Andreas AC, Ziemiecki A, Aston RR, Wilks AF. JAK2, a third member of the JAK family of protein tyrosine kinases. Oncogene. 1992;7(7):1347-53.
18. Takahashi T, Shirasawa T. Molecular cloning of rat JAK3, a novel member of the JAK family of protein tyrosine kinases. FEBS Lett. 1994;342(2):124-8.
19. Krolewski JJ, Lee R, Eddy R, Shows TB, Dalla-Favera R. Identification and chromosomal mapping of new human tyrosine kinase genes. Oncogene. 1990;5(3):277-82.
20. Yamaoka K, Saharinen P, Pesu M, Holt VE, 3rd, Silvennoinen O, O'Shea JJ. The Janus kinases (Jaks). Genome Biol. 2004;5(12):253.
21. Velazquez L, Fellous M, Stark GR, Pellegrini S. A protin tyrosine kinase in the interferon alpha/beta signaling pathway. Cell 1992;70(2):313-22.
22. Muller M, Briscoe J, Laxton C, Guschin D, Ziemicki A, Silvennoinen O, et al. The protein tyrosine kinase JAK1 complements defects in intrferon-alpha/beta and-gamma signal transduction. Nature. 1993;366(6451):129-35.
23. Leonard WJ, O'Shea JJ. Jaks and Stats: Biological implications. Annu Rev Immunol. 1998;16(1):293-322.
24. Schindler CW. Series introduction. JAK-STAT signaling in human disease. J Clin Invest. 2002 May;109(9):1133-7.
25. Kisseleva T, Bhattacharya S, Braunstein J, Schindler CW. Signaling through the JAK/STAT pathway, recent advances and future challenges. Gene. 2002 Feb 20;285(1-2):1-24.
26. Miyazaki T, Taniguchi T. Coupling of the IL2 receptor complex with non-receptor protien tyrosine kinases. Cancer Surv. 1996;27:25-39.
27. Levy DE. The house that Jak/Stat built. Cytokine Growth Factor Rev. 1997;8:81-9s0.
28. Ihle JN, Kerr IR. Jaks and Stats in signaling by the cytokine receptor superfamily. Trends Genet. 1995;11:69-74.
29. Vassilev AO, Lorenz DR, Tibbles HE, Uckun FM. Role of the leukemia-associated transcription factor STAT3 in platelet physiology. Leuk Lymphoma. 2002 Jul;43(7):1461-7.
30. Darnell JEJ, Kerr IM, Stark GR. Jak-STAT pathways and transcriptional activation in response to IFNs and other extracellular signaling proteins. Science. 1994;264:1415-21.
31. Macchi P, Villa A, Giliani S, Sacco MG, Frattini A, Porta F, et al. Mutations of Jak-3 gene in patients with autosomal severe combined immune deficiency (SCID). Nature. 1995;377:65-8.
32. Russell SM, Tayebi N, Nakajima H, Riedy MC, Roberts JL, Aman MJ, et al. Mutation of Jak3 in a patient with SCID: essential role of Jak3 in lymphoid development. Science. 1995;270:797-800.
33. Buckley RH, Schiff RI, Schiff SE, Markert ML, Williams LW, Harville TO, et al. Human severe combined immunodeficiency: genetic phenotypic and functional diversity in one hundred eight infants. J Pediatr. 1997;130:378-87.
34. Cetkovic-Cvrlje M, Uckun FM. Targeting Janus kinase 3 in the treatment of leukemia and inflammatory diseases. Arch Immunol Ther Exp (Warsz). 2004 Mar-Apr;52(2):69-82.
35. Cetkovic-Cvrlje M, Roers BA, Schonhoff D, Waurzyniak B, Liu XP, Uckun FM. Treatment of post-bone marrow transplant acute graft-versus-host disease with a rationally designed JAK3 inhibitor. Leukemia and lymphoma. 2002;43:1447-553.
36. Cetkovic-Cvrlje M, Tibbles HE. Therapeutic potential of Janus kinase 3 (JAK3) inhibitors. Curr Pharm Des. 2004;10(15):1767-84.
37. Vassilev AO, Tibbles HE, DuMez D, Venkatachalam TK, Uckun FM. Targeting JAK3 and BTK tyrosine kinases with rationally-designed inhibitors. Curr Drug Targets. 2006 Mar;7(3):327-43.
38. Uckun FM, Mao C. Tyrosine kinases as new molecular targets in treatment of inflammatory disorders and leukemia. Curr Pharm Des. 2004;10(10):1083-91.
39. Krejsgaard T, Vetter-Kauczok CS, Woetmann A, Lovato P, Labuda T, Eriksen KW, et al. Jak3- and JNK-dependent vascular endothelial growth factor expression in cutaneous T-cell lymphoma. Leukemia. 2006 Aug 17.
40. Han Y, Amin HM, Frantz C, Franko B, Lee J, Lin Q, et al. Restoration of shp1 expression by 5-AZA-2′-deoxycytidine is associated with downregulation of JAK3/STAT3 signaling in ALK-positive anaplastic large cell lymphoma. Leukemia. 2006 Sep;20(9):1602-9.
41. Walters DK, Mercher T, Gu TL, O'Hare T, Tyner JW, Loriaux M, et al. Activating alleles of JAK3 in acute megakaryoblastic leukemia. Cancer Cell. 2006 Jul;10(1):65-75.
42. Choi YL, Kaneda R, Wada T, Fujiwara SI, Soda M, Watanabe H, et al. Identification of a constitutively active mutant of JAK3 by retroviral expression screening. Leuk Res. 2006 Jun 19.
43. Lin Q, Lai R, Chirieac LR, Li C, Thomazy VA, Grammatikakis I, et al. Constitutive activation of JAK3/STAT3 in colon carcinoma tumors and cell lines: inhibition of JAK3/STAT3 signaling induces apoptosis and cell cycle arrest of colon carcinoma cells. Am J Pathol. 2005 Oct;167(4):969-80.
44. Mori D, Nakafusa Y, Miyazaki K, Tokunaga O. Differential expression of Janus kinase 3 (JAK3), matrix metalloproteinase 13 (MMP13), heat shock protein 60 (HSP60), and mouse double minute 2 (MDM2) in human colorectal cancer progression using human cancer cDNA microarrays. Pathol Res Pract. 2005;201(12):777-89.
45. Chen WS, Kung HJ, Yang WK, Lin W. Comparative tyrosine-kinase profiles in colorectal cancers: enhanced arg expression in carcinoma as compared with adenoma and normal mucosa. Int J Cancer. 1999 Nov 26;83(5):579-84.
46. Goodman PA, Niehoff LB, Uckun FM. Role of tyrosine kinases in induction of the c-jun proto-oncogene in irradiated B-lineage lymphoid cells. J Biol Chem. 1998 Jul 10;273(28):17742-8.
47. Sudbeck EA, Liu XP, Narla RK, Mahajan S, Ghosh S, Mao C, et al. Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents. Clin Cancer Res. 1999 Jun;5(6):1569-82.
48. Witthuhn BA, Williams MD, Kerawalla H, Uckun FM. Differential substrate recognition capabilities of Janus family protein tyrosine kinases within the interleukin 2 receptor (IL2R) system: Jak3 as a potential molecular target for treatment of leukemias with a hyperactive Jak-Stat signaling machinery. Leuk Lymphoma. 1999 Jan;32(3-4):289-97.
49. Cetkovic-Cvrlje M, Roers BA, Waurzyniak B, Liu XP, Uckun FM. Targeting Janus Kinase 3 to attenuate the severity of acute graft-versus-host disease across the major histocompatibility barrier in mice. Blood. 2001;98:1607-13.
50. Cetkovic-Cvrlje M, Dragt AL, Vassilev A, Liu XP, Uckun FM. Targeting JAK3 with JANEX-1 for prevention of autoimmune type 1 diabtes in NOD mice. Clin Immunol. 2003;106:213-25.
51. Uckun FM, Roers BA, Waurzyniak B, Cetkovic-Cvrlje M. Janus kinase 3 inhibitor WHI-P131/JANEX-1 prevents graft-versus-host disease but spares the graft-versus-leukemia function of the bone marrow allografts in a murine bone marrow transplantation model. Blood. 2002;99:4192-99.
52. Bach JF, Chatenoud L. Tolerance to islet autoantigens in type 1 diabetes. Annu Rev Immunol 2001;19:131-61.
53. Martinez-Lostao L, Briones J, Forne I, Martinez-Gallo M, Ferrer B, Sierra J, et al. Role of the STAT1 pathway in apoptosis induced by fludarabine and JAK kinase inhibitors in B-cell chronic lymphocytic leukemia. Leuk Lymphoma. 2005 Mar;46(3):435-42.
54. Uckun FM, Ek O, Liu X-P, Chen C-L. In vivo toxicity and pharmacokinetic features of the Janus kinase 3 inhibitor WHI-P131 [4-(4′-hydroxyphenyl)- amino-6,7-dimethoxyquinazoline]. Clin Cancer Res. 1999;5:2954-62.
55. Malavija R, Chen CL, Liu XP, Uckun FM. In vivo pharmacokinetics and anti-anaphylactic activity of the novel mast cell inhibitor 4-(4′- hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P131). Am J Ther. 2001;8(1):35-9.
56. Uckun FM, Thoen J, Chen H, Sudbeck E, Mao C, Malaviya R, et al. CYP1A-mediated metabolism of the Janus kinase-3 inhibitor 4-(4′- hydroxyphenyl)-amino-6,7-dimethoxyquinazoline: structural basis for inactivation by regioselective O-demethylation. Drug Metab Dispos. 2002 Jan;30(1):74-85.
57. Chen CL, Malaviya R, Chen H, Liu XP, Uckun FM. Quantitative high-performance liquid chromatographic method for pharmacokinetic studies of the potent mast cell inhibitor 4-(4′-hydroxyphenyl)amino-6,7- dimethoxyquinazoline (WHI-P131). J Chromatogr B Biomed Sci Appl. 1999 Apr 30;727(1-2):205-12.
58. Uckun F, Vassilev A, Tibbles H. Chemoprevention of Colorectal Cancer by Targeting of Janus Kinase 3 (JAK3) in the APCMin Mouse Model of Familial Adenomatous Polyposis (FAP). Third Annual Conference on Frontiers in Cancer Prevention Research; 2004 October 16-20, 2004; Seattle, Washington; 2004.
59. Uckun F, Vassilev A, Tibbles H, Erbeck D, Liu X-P. Chemoprevention of Colorectal Cancer by Targeting of Janus Kinase 3 (JAK3) in the APCMin Mouse Model of Familial Adenomatous Polyposis (FAP). Gastrointestinal Cancers Symposium (ASCO); 2005 January 27-29, 2005; Hollywood, Florida; 2005.
60. Uckun FM, Vassilev AO. Anti-inflammatory and immunosuppresive activity profile of JANEX-1 in preclinical animal models of inflammation and transplantation. Submitted 2006.
61. Uckun FM, Ek O, Liu XP, Chen CL. In vivo toxicity and pharmacokinetic features of the janus kinase 3 inhibitor WHI-P131 [4-(4′hydroxyphenyl)- amino-6,7- dimethoxyquinazoline. Clin Cancer Res. 1999 Oct;5(10):2954-62.
62. Uckun FM, Roers BA, Waurzyniak B, Liu XP, Cetkovic-Cvrlje M. Janus kinase 3 inhibitor WHI-P131/JANEX-1 prevents graft-versus-host disease but spares the graft-versus-leukemia function of the bone marrow allografts in a murine bone marrow transplantation model. Blood. 2002 Jun 1;99(11):4192-9.
63. Uckun FM, Sudbeck EA, Mao C, Ghosh S, Liu XP, Vassilev AO, et al. Structure-based design of novel anticancer agents. Curr Cancer Drug Targets. 2001 May;1(1):59-71.
64. Uckun FM, Narla RK, Jun X, Zeren T, Venkatachalam T, Waddick KG, et al. Cytotoxic activity of epidermal growth factor-genistein against breast cancer cells. Clin Cancer Res. 1998 Apr;4(4):901-12.
65. Perkins S, Verschoyle RD, Hill K, Parveen I, Threadgill MD, Sharma RA, et al. Chemopreventive efficacy and pharmacokinetics of curcumin in the min/+ mouse, a model of familial adenomatous polyposis. Cancer Epidemiol Biomarkers Prev. 2002 Jun;11(6):535-40.
66. Paoni NF, Feldman MW, Gutierrez LS, Ploplis VA, Castellino FJ. Transcriptional profiling of the transition from normal intestinal epithelia to adenomas and carcinomas in the APCMin/+ mouse. Physiol Genomics. 2003 Nov 11;15(3):228-35.
67. Rodriquez-Bigas M, Lin E, Crane C. Adenocarcinoma of the Colon and Rectum. In: Kufe DW, Pollack RE, Weichselbaum RR, Bast RC, Gansler TS, Holland JF, et al., eds. Cancer Medicine 6. Hamilton, ON: BC Decker 2003:1635-65.
68. Janne PA, Mayer RJ. Chemoprevention of colorectal cancer. N Engl J Med. 2000 Jun 29;342(26):1960-8.
69. Rao CV, Cooma I, Rodriguez JG, Simi B, El-Bayoumy K, Reddy BS. Chemoprevention of familial adenomatous polyposis development in the APC(min) mouse model by 1,4-phenylene bis(methylene)selenocyanate. Carcinogenesis. 2000 Apr;21(4):617-21.
70. Corpet DE, Pierre F. Point: From animal models to prevention of colon cancer. Systematic review of chemoprevention in min mice and choice of the model system. Cancer Epidemiol Biomarkers Prev. 2003 May;12(5):391-400.
71. Mann JR, DuBois RN. Cyclooxygenase-2 and gastrointestinal cancer. Cancer J. 2004 May-Jun;10(3):145-52.
72. Jacoby RF, Seibert K, Cole CE, Kelloff G, Lubet RA. The cyclooxygenase-2 inhibitor celecoxib is a potent preventive and therapeutic agent in the min mouse model of adenomatous polyposis. Cancer Res. 2000 Sep 15;60(18):5040-4.
73. Chun KS, Kim SH, Song YS, Surh YJ. Celecoxib inhibits phorbol ester-induced expression of COX-2 and activation of AP-1 and p38 MAP kinase in mouse skin. Carcinogenesis. 2004 Jun;25(5):713-22.
74. Friedman B, Orlet HK, Still JM, Law E. Toxic epidermal necrolysis due to administration of celecoxib (Celebrex). South Med J. 2002 Oct;95(10):1213-4.
75. Davies NM, Jamali F. COX-2 selective inhibitors cardiac toxicity: getting to the heart of the matter. J Pharm Pharm Sci. 2004 Oct 29;7(3):332-6.
76. Schror K. [Cardiovascular risks of selective COX-2-inhibitors]. Dtsch Med Wochenschr. 2004 Dec 3;129(49):2653-6.
77. Waddell WR. The effect of sulindac on colon polyps: circumvention of a transformed phenotype - a hypothesis. J Surg Oncol. 1994 Jan;55(1):52-5.
78. DuBois RN. Nonsteroidal anti-inflammatory drug use and sporadic colorectal adenomas. Gastroenterology. 1995 Apr;108(4):1310-4.
79. Ishikawa H. Chemoprevention of carcinogenesis in familial tumors. Int J Clin Oncol. 2004 Sep;9(4):299-303.
80. Reuter BK, Zhang XJ, Miller MJ. Therapeutic utility of aspirin in the ApcMin/+ murine model of colon carcinogenesis. BMC Cancer. 2002 Aug 9;2(1):19.
81. Cetkovic-Cvrlje M, Roers BA, Schonhoff D, Waurzyniak B, Liu XP, Uckun FM. Treatment of post-bone marrow transplant acute graft-versus-host disease with a rationally designed JAK3 inhibitor. Leuk Lymphoma. 2002 Jul;43(7):1447-53.