The Jak2 inhibitor, G6, alleviates jak2-V617F-mediated myeloproliferative neoplasia by providing significant therapeutic efficacy to the bone marrow

Neoplasia

Volumn 13, Issue 11, 2011, Pages 1058-1068

  Kirabo, Annet ^a   Park, Sung O ^a   Majumder, Anurima ^a   Gali, Meghanath ^b   Reinhard, Mary K ^c   Wamsley, Heather L ^d   Zhao, Zhizhuang Joe ^e   Cogle, Christopher R ^a   Bisht, Kirpal S ^b   Keseru, György M ^f   Sayeski, Peter P ^a  

^a UNIVERSITY OF FLORIDA COLLEGE OF MEDICINE   (United States)

^b UNIVERSITY OF SOUTH FLORIDA   (United States)

^c UNIVERSITY OF FLORIDA   (United States)

^d University of Florida College of Veterinary Medicine   (United States)

^e UNIVERSITY OF OKLAHOMA COLLEGE OF MEDICINE   (United States)

^f BUDAPEST UNIVERSITY OF TECHNOLOGY AND ECONOMICS   (Hungary)

Author keywords

[No Author keywords available]

Indexed keywords

G6; INTERLEUKIN 6; JANUS KINASE 2; JANUS KINASE 2 INHIBITOR; STAT5 PROTEIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BONE MARROW; BONE MARROW CANCER; CELL HYPERPLASIA; CLONOGENIC ASSAY; CONTROLLED STUDY; DRUG EFFICACY; DRUG MECHANISM; ERYTHROCYTOSIS; EXTRAMEDULLARY HEMATOPOIESIS; HEMATOPOIETIC STEM CELL; LEUKOCYTOSIS; MALE; MEGAKARYOCYTIC HYPERPLASIA; MOUSE; MUTANT; MYELOPROLIFERATIVE NEOPLASIA; NONHUMAN; PRIORITY JOURNAL; PROTEIN BLOOD LEVEL; SPLENOMEGALY; THROMBOCYTOSIS;

EID: 81355133678     PISSN: 15228002     EISSN: 14765586     Source Type: Journal    
DOI: 10.1593/neo.111112     Document Type: Article

References (30)

1. Talarico L, Wolf BC, Kumar A, and Weintraub LR (1989). Reversal of bone marrow fibrosis and subsequent development of polycythemia in patients with myeloproliferative disorders. Am J Hematol 30, 248-253.
2. Campbell PJ and Green AR (2006). The myeloproliferative disorders. N Engl J Med 355, 2452-2466.
3. Marchioli R, Finazzi G, Landolfi R, Kutti J, Gisslinger H, Patrono C, Marilus R, Villegas A, Tognoni G, and Barbui T (2005). Vascular and neoplastic risk in a large cohort of patients with polycythemia vera. J Clin Oncol 23, 2224-2232.
4. Harrison CN, Campbell PJ, Buck G, Wheatley K, East CL, Bareford D, Wilkins BS, van der Walt JD, Reilly JT, Grigg AP, et al. (2005). Hydroxyurea compared with anagrelide in high-risk essential thrombocythemia. N Engl J Med 353, 33-45.
5. Cervantes F, Alvarez-Larran A, Arellano-Rodrigo E, Granell M, Domingo A, and Montserrat E (2006). Frequency and risk factors for thrombosis in idiopathic myelofibrosis: analysis in a series of 155 patients from a single institution. Leukemia 20, 55-60.
6. De Stefano V, Za T, Rossi E, Vannucchi AM, Ruggeri M, Elli E, Mico C, Tieghi A, Cacciola RR, Santoro C, et al. (2008). Recurrent thrombosis in patients with polycythemia vera and essential thrombocythemia: incidence, risk factors, and effect of treatments. Haematologica 93, 372-380.
7. Kiladjian JJ, Cervantes F, Leebeek FW, Marzac C, Cassinat B, Chevret S, Cazals-Hatem D, Plessier A, Garcia-Pagan JC, Darwish Murad S, et al. (2008). The impact of JAK2 and MPL mutations on diagnosis and prognosis of splanchnic vein thrombosis: a report on 241 cases. Blood 111, 4922-4929.
8. Wang JC, Chang TH, Goldberg A, Novetsky AD, Lichter S, and Lipton J (2006). Quantitative analysis of growth factor production in the mechanism of fibrosis in agnogenic myeloid metaplasia. Exp Hematol 34, 1617-1623.
9. Schmitt A, Jouault H, Guichard J, Wendling F, Drouin A, and Cramer EM (2000). Pathologic interaction between megakaryocytes and polymorphonuclear leukocytes in myelofibrosis. Blood 96, 1342-1347.
10. Xu M, Bruno E, Chao J, Huang S, Finazzi G, Fruchtman SM, Popat U, Prchal JT, Barosi G, and Hoffman R (2005). Constitutive mobilization of CD34+ cells into the peripheral blood in idiopathic myelofibrosis may be due to the action of a number of proteases. Blood 105, 4508-4515.
11. Panteli KE, Hatzimichael EC, Bouranta PK, Katsaraki A, Seferiadis K, Stebbing J, and Bourantas KL (2005). Serum interleukin (IL)-1, IL-2, sIL-2Ra, IL-6 and thrombopoietin levels in patients with chronic myeloproliferative diseases. Br J Haematol 130, 709-715.
12. Tefferi A (2000). Myelofibrosis with myeloid metaplasia. N Engl J Med 342, 1255-1265.
13. Mesa RA, Silverstein MN, Jacobsen SJ, Wollan PC, and Tefferi A (1999). Population-based incidence and survival figures in essential thrombocythemia and agnogenic myeloid metaplasia: an Olmsted County Study, 1976-1995. Am J Hematol 61, 10-15.
14. Santos FP and Verstovsek S (2011). JAK2 inhibitors: what's the true therapeutic potential? Blood Rev 25, 53-63.
15. Kiss R, Polgar T, Kirabo A, Sayyah J, Figueroa NC, List AF, Sokol L, Zuckerman KS, Gali M, Bisht KS, et al. (2009). Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening. Bioorg Med Chem Lett 19, 3598-3601.
16. Majumder A, Govindasamy L, Magis A, Kiss R, Polgar T, Baskin R, Allan RW, Agbandje-McKenna M, Reuther GW, Keseru GM, et al. (2010). Structurefunction correlation of G6, a novel small molecule inhibitor of Jak2: indispensability of the stilbenoid core. J Biol Chem 285, 31399-31407.
17. Kirabo A, Embury J, Kiss R, Polgar T, Gali M, Majumder A, Bisht KS, Cogle CR, Keseru GM, and Sayeski PP (2011). The stilbenoid tyrosine kinase inhibitor, G6, suppresses Jak2-V617F-mediated human pathological cell growth in vitro and in vivo. J Biol Chem 286, 4280-4291.
18. Xing S, Wanting TH, Zhao W, Ma J, Wang S, Xu X, Li Q, Fu X, Xu M, and Zhao ZJ (2008). Transgenic expression of JAK2V617F causes myeloproliferative disorders in mice. Blood 111, 5109-5117.
19. Elmore SA (2006). Enhanced histopathology of the bone marrow. Toxicol Pathol 34, 666-686.
20. Tefferi A and Pardanani A (2011). JAK inhibitors in myeloproliferative neoplasms: rationale, current data and perspective. Blood Rev 25, 229-237.
21. Santos FP, Kantarjian HM, Jain N, Manshouri T, Thomas DA, Garcia-Manero G, Kennedy D, Estrov Z, Cortes J, and Verstovsek S (2010). Phase 2 study of CEP-701, an orally available JAK2 inhibitor, in patients with primary or post-polycythemia vera/essential thrombocythemia myelofibrosis. Blood 115, 1131-1136.
22. Koppikar P, Abdel-Wahab O, Hedvat C, Marubayashi S, Patel J, Goel A, Kucine N, Gardner JR, Combs AP, Vaddi K, et al. (2010). Efficacy of the JAK2 inhibitor INCB16562 in a murine model of MPLW515L-induced thrombocytosis and myelofibrosis. Blood 115, 2919-2927.
23. Pardanani A, Lasho T, Smith G, Burns CJ, Fantino E, and Tefferi A (2009). CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia 23, 1441-1445.
24. Tyner JW, Bumm TG, Deininger J, Wood L, Aichberger KJ, Loriaux MM, Druker BJ, Burns CJ, Fantino E, and Deininger MW (2010). CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood 115, 5232-5240.
25. Larrosa M, Tomas-Barberan FA, and Espin JC (2003). Grape polyphenol resveratrol and the related molecule 4-hydroxystilbene induce growth inhibition, apoptosis, S-phase arrest, and upregulation of cyclins A, E, and B1 in human SK-Mel-28 melanoma cells. J Agric Food Chem 51, 4576-4584.
26. Le Corre L, Chalabi N, Delort L, Bignon YJ, and Bernard-Gallon DJ (2005). Resveratrol and breast cancer chemoprevention: molecular mechanisms. Mol Nutr Food Res 49, 462-471.
27. Kimura Y (2005). New anticancer agents: in vitro and in vivo evaluation of the antitumor and antimetastatic actions of various compounds isolated from medicinal plants. In Vivo 19, 37-60.
28. Pace-Asciak CR, Hahn S, Diamandis EP, Soleas G, and Goldberg DM (1995). The red wine phenolics trans-resveratrol and quercetin block human platelet aggregation and eicosanoid synthesis: implications for protection against coronary heart disease. Clin Chim Acta 235, 207-219.
29. Geahlen RL and McLaughlin JL (1989). Piceatannol (3,4,3′,5′-tetrahydroxytrans- stilbene) is a naturally occurring protein-tyrosine kinase inhibitor. Biochem Biophys Res Commun 165, 241-245.
30. Swanson-Mungerson M, Ikeda M, Lev L, Longnecker R, and Portis T (2003). Identification of latent membrane protein 2A (LMP2A) specific targets for treatment and eradication of Epstein-Barr virus (EBV)-associated diseases. J Antimicrob Chemother 52, 152-154.