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Items: 1 to 20 of 110

1.

LS104, a non-ATP-competitive small-molecule inhibitor of JAK2, is potently inducing apoptosis in JAK2V617F-positive cells.

Lipka DB, Hoffmann LS, Heidel F, Markova B, Blum MC, Breitenbuecher F, Kasper S, Kindler T, Levine RL, Huber C, Fischer T.

Mol Cancer Ther. 2008 May;7(5):1176-84. doi: 10.1158/1535-7163.MCT-07-2215.

2.

TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations.

Pardanani A, Hood J, Lasho T, Levine RL, Martin MB, Noronha G, Finke C, Mak CC, Mesa R, Zhu H, Soll R, Gilliland DG, Tefferi A.

Leukemia. 2007 Aug;21(8):1658-68. Epub 2007 May 31.

PMID:
17541402
3.

Combined inhibition of Janus kinase 1/2 for the treatment of JAK2V617F-driven neoplasms: selective effects on mutant cells and improvements in measures of disease severity.

Liu PC, Caulder E, Li J, Waeltz P, Margulis A, Wynn R, Becker-Pasha M, Li Y, Crowgey E, Hollis G, Haley P, Sparks RB, Combs AP, Rodgers JD, Burn TC, Vaddi K, Fridman JS.

Clin Cancer Res. 2009 Nov 15;15(22):6891-900. doi: 10.1158/1078-0432.CCR-09-1298. Epub 2009 Nov 3.

4.

A potential role for HSP90 inhibitors in the treatment of JAK2 mutant-positive diseases as demonstrated using quantitative flow cytometry.

Bareng J, Jilani I, Gorre M, Kantarjian H, Giles F, Hannah A, Albitar M.

Leuk Lymphoma. 2007 Nov;48(11):2189-95.

PMID:
17926180
5.

The kinase inhibitor LS104 induces apoptosis, enhances cytotoxic effects of chemotherapeutic drugs and is targeting the receptor tyrosine kinase FLT3 in acute myeloid leukemia.

Kasper S, Breitenbuecher F, Hoehn Y, Heidel F, Lipka DB, Markova B, Huber C, Kindler T, Fischer T.

Leuk Res. 2008 Nov;32(11):1698-708. doi: 10.1016/j.leukres.2008.05.003. Epub 2008 Jun 16.

PMID:
18556063
6.

mTOR inhibitors alone and in combination with JAK2 inhibitors effectively inhibit cells of myeloproliferative neoplasms.

Bogani C, Bartalucci N, Martinelli S, Tozzi L, Guglielmelli P, Bosi A, Vannucchi AM; Associazione Italiana per la Ricerca sul Cancro AGIMM Gruppo Italiano Malattie Mieloproliferative..

PLoS One. 2013;8(1):e54826. doi: 10.1371/journal.pone.0054826. Epub 2013 Jan 31.

7.
8.

Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805.

Baffert F, Régnier CH, De Pover A, Pissot-Soldermann C, Tavares GA, Blasco F, Brueggen J, Chène P, Drueckes P, Erdmann D, Furet P, Gerspacher M, Lang M, Ledieu D, Nolan L, Ruetz S, Trappe J, Vangrevelinghe E, Wartmann M, Wyder L, Hofmann F, Radimerski T.

Mol Cancer Ther. 2010 Jul;9(7):1945-55. doi: 10.1158/1535-7163.MCT-10-0053. Epub 2010 Jun 29.

9.

AT9283, a potent inhibitor of the Aurora kinases and Jak2, has therapeutic potential in myeloproliferative disorders.

Dawson MA, Curry JE, Barber K, Beer PA, Graham B, Lyons JF, Richardson CJ, Scott MA, Smyth T, Squires MS, Thompson NT, Green AR, Wallis NG.

Br J Haematol. 2010 Jul;150(1):46-57. doi: 10.1111/j.1365-2141.2010.08175.x. Epub 2010 May 7.

PMID:
20507304
10.

SOCS2: inhibitor of JAK2V617F-mediated signal transduction.

Quentmeier H, Geffers R, Jost E, Macleod RA, Nagel S, Röhrs S, Romani J, Scherr M, Zaborski M, Drexler HG.

Leukemia. 2008 Dec;22(12):2169-75. doi: 10.1038/leu.2008.226. Epub 2008 Sep 4.

PMID:
18769447
11.

Selective reduction of JAK2V617F-dependent cell growth by siRNA/shRNA and its reversal by cytokines.

Jedidi A, Marty C, Oligo C, Jeanson-Leh L, Ribeil JA, Casadevall N, Galy A, Vainchenker W, Villeval JL.

Blood. 2009 Aug 27;114(9):1842-51. doi: 10.1182/blood-2008-09-176875. Epub 2009 Jul 9.

12.

JAK2 kinase inhibitors and myeloproliferative disorders.

Chen AT, Prchal JT.

Curr Opin Hematol. 2010 Mar;17(2):110-6. doi: 10.1097/MOH.0b013e3283366b91. Review.

PMID:
20087176
13.

Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitors.

Geron I, Abrahamsson AE, Barroga CF, Kavalerchik E, Gotlib J, Hood JD, Durocher J, Mak CC, Noronha G, Soll RM, Tefferi A, Kaushansky K, Jamieson CH.

Cancer Cell. 2008 Apr;13(4):321-30. doi: 10.1016/j.ccr.2008.02.017.

14.

R723, a selective JAK2 inhibitor, effectively treats JAK2V617F-induced murine myeloproliferative neoplasm.

Shide K, Kameda T, Markovtsov V, Shimoda HK, Tonkin E, Fang S, Liu C, Gelman M, Lang W, Romero J, McLaughlin J, Bhamidipati S, Clough J, Low C, Reitsma A, Siu S, Pine P, Park G, Torneros A, Duan M, Singh R, Payan DG, Matsunaga T, Hitoshi Y, Shimoda K.

Blood. 2011 Jun 23;117(25):6866-75. doi: 10.1182/blood-2010-01-262535. Epub 2011 Apr 29.

15.

An inhibitor of Janus kinase 2 prevents polycythemia in mice.

Mathur A, Mo JR, Kraus M, O'Hare E, Sinclair P, Young J, Zhao S, Wang Y, Kopinja J, Qu X, Reilly J, Walker D, Xu L, Aleksandrowicz D, Marshall G, Scott ML, Kohl NE, Bachman E.

Biochem Pharmacol. 2009 Aug 15;78(4):382-9. doi: 10.1016/j.bcp.2009.04.025. Epub 2009 May 3.

PMID:
19413997
16.

WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation.

Verstovsek S, Manshouri T, Quintás-Cardama A, Harris D, Cortes J, Giles FJ, Kantarjian H, Priebe W, Estrov Z.

Clin Cancer Res. 2008 Feb 1;14(3):788-96. doi: 10.1158/1078-0432.CCR-07-0524.

17.

In vitro and in vivo characterization of SGI-1252, a small molecule inhibitor of JAK2.

Ahmed KB, Warner SL, Chen A, Gourley ES, Liu X, Vankayalapati H, Nussenzveig R, Prchal JT, Bearss DJ, Parker CJ.

Exp Hematol. 2011 Jan;39(1):14-25. doi: 10.1016/j.exphem.2010.09.013. Epub 2010 Oct 8.

PMID:
20934482
18.

WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells.

Ferrajoli A, Faderl S, Van Q, Koch P, Harris D, Liu Z, Hazan-Halevy I, Wang Y, Kantarjian HM, Priebe W, Estrov Z.

Cancer Res. 2007 Dec 1;67(23):11291-9.

19.

Efficacy of the JAK2 inhibitor INCB16562 in a murine model of MPLW515L-induced thrombocytosis and myelofibrosis.

Koppikar P, Abdel-Wahab O, Hedvat C, Marubayashi S, Patel J, Goel A, Kucine N, Gardner JR, Combs AP, Vaddi K, Haley PJ, Burn TC, Rupar M, Bromberg JF, Heaney ML, de Stanchina E, Fridman JS, Levine RL.

Blood. 2010 Apr 8;115(14):2919-27. doi: 10.1182/blood-2009-04-218842. Epub 2010 Feb 12.

20.

Preferential nuclear accumulation of JAK2V617F in CD34+ but not in granulocytic, megakaryocytic, or erythroid cells of patients with Philadelphia-negative myeloproliferative neoplasia.

Rinaldi CR, Rinaldi P, Alagia A, Gemei M, Esposito N, Formiggini F, Martinelli V, Senyuk V, Nucifora G, Pane F.

Blood. 2010 Dec 23;116(26):6023-6. doi: 10.1182/blood-2010-08-302265. Epub 2010 Sep 22.

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