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Items: 1 to 20 of 68

1.

Concurrent Inhibition of Pim and FLT3 Kinases Enhances Apoptosis of FLT3-ITD Acute Myeloid Leukemia Cells through Increased Mcl-1 Proteasomal Degradation.

Kapoor S, Natarajan K, Baldwin PR, Doshi KA, Lapidus RG, Mathias TJ, Scarpa M, Trotta R, Davila E, Kraus M, Huszar D, Tron AE, Perrotti D, Baer MR.

Clin Cancer Res. 2018 Jan 1;24(1):234-247. doi: 10.1158/1078-0432.CCR-17-1629. Epub 2017 Oct 26.

PMID:
29074603
2.

Pim kinase inhibition sensitizes FLT3-ITD acute myeloid leukemia cells to topoisomerase 2 inhibitors through increased DNA damage and oxidative stress.

Doshi KA, Trotta R, Natarajan K, Rassool FV, Tron AE, Huszar D, Perrotti D, Baer MR.

Oncotarget. 2016 Jul 26;7(30):48280-48295. doi: 10.18632/oncotarget.10209.

3.

Next-generation sequencing identifies a novel ELAVL1-TYK2 fusion gene in MOLM-16, an AML cell line highly sensitive to the PIM kinase inhibitor AZD1208.

Tron AE, Keeton EK, Ye M, Casas-Selves M, Chen H, Dillman KS, Gale RE, Stengel C, Zinda M, Linch DC, Lai Z, Khwaja A, Huszar D.

Leuk Lymphoma. 2016 Dec;57(12):2927-2929. Epub 2016 May 17. No abstract available.

PMID:
27189703
4.

JAK2 inhibition sensitizes resistant EGFR-mutant lung adenocarcinoma to tyrosine kinase inhibitors.

Gao SP, Chang Q, Mao N, Daly LA, Vogel R, Chan T, Liu SH, Bournazou E, Schori E, Zhang H, Brewer MR, Pao W, Morris L, Ladanyi M, Arcila M, Manova-Todorova K, de Stanchina E, Norton L, Levine RL, Altan-Bonnet G, Solit D, Zinda M, Huszar D, Lyden D, Bromberg JF.

Sci Signal. 2016 Mar 29;9(421):ra33. doi: 10.1126/scisignal.aac8460.

5.

Differential regulation of mTOR signaling determines sensitivity to AKT inhibition in diffuse large B cell lymphoma.

Ezell SA, Wang S, Bihani T, Lai Z, Grosskurth SE, Tepsuporn S, Davies BR, Huszar D, Byth KF.

Oncotarget. 2016 Feb 23;7(8):9163-74. doi: 10.18632/oncotarget.7036.

6.

Identification of azabenzimidazoles as potent JAK1 selective inhibitors.

Vasbinder MM, Alimzhanov M, Augustin M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Goodwin K, Huszar D, Kawatkar A, Kawatkar S, Read J, Shi J, Steinbacher S, Steuber H, Su Q, Toader D, Wang H, Woessner R, Wu A, Ye M, Zinda M.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):60-7. doi: 10.1016/j.bmcl.2015.11.031. Epub 2015 Nov 12.

PMID:
26614408
7.

The PIM inhibitor AZD1208 synergizes with ruxolitinib to induce apoptosis of ruxolitinib sensitive and resistant JAK2-V617F-driven cells and inhibit colony formation of primary MPN cells.

Mazzacurati L, Lambert QT, Pradhan A, Griner LN, Huszar D, Reuther GW.

Oncotarget. 2015 Nov 24;6(37):40141-57. doi: 10.18632/oncotarget.5653.

8.

Targeted Blockade of JAK/STAT3 Signaling Inhibits Ovarian Carcinoma Growth.

Gritsina G, Xiao F, O'Brien SW, Gabbasov R, Maglaty MA, Xu RH, Thapa RJ, Zhou Y, Nicolas E, Litwin S, Balachandran S, Sigal LJ, Huszar D, Connolly DC.

Mol Cancer Ther. 2015 Apr;14(4):1035-47. doi: 10.1158/1535-7163.MCT-14-0800. Epub 2015 Feb 2.

9.

PIM kinase inhibitor AZD1208 for treatment of MYC-driven prostate cancer.

Kirschner AN, Wang J, van der Meer R, Anderson PD, Franco-Coronel OE, Kushner MH, Everett JH, Hameed O, Keeton EK, Ahdesmaki M, Grosskurth SE, Huszar D, Abdulkadir SA.

J Natl Cancer Inst. 2014 Dec 13;107(2). pii: dju407. doi: 10.1093/jnci/dju407. Print 2015 Feb.

10.

Partial inhibition of gp130-Jak-Stat3 signaling prevents Wnt-β-catenin-mediated intestinal tumor growth and regeneration.

Phesse TJ, Buchert M, Stuart E, Flanagan DJ, Faux M, Afshar-Sterle S, Walker F, Zhang HH, Nowell CJ, Jorissen R, Tan CW, Hirokawa Y, Eissmann MF, Poh AR, Malaterre J, Pearson HB, Kirsch DG, Provero P, Poli V, Ramsay RG, Sieber O, Burgess AW, Huszar D, Vincan E, Ernst M.

Sci Signal. 2014 Sep 30;7(345):ra92. doi: 10.1126/scisignal.2005411.

11.

PIM and AKT kinase inhibitors show synergistic cytotoxicity in acute myeloid leukaemia that is associated with convergence on mTOR and MCL1 pathways.

Meja K, Stengel C, Sellar R, Huszar D, Davies BR, Gale RE, Linch DC, Khwaja A.

Br J Haematol. 2014 Oct;167(1):69-79. doi: 10.1111/bjh.13013. Epub 2014 Jun 30.

PMID:
24975213
12.

Pharmacologic suppression of JAK1/2 by JAK1/2 inhibitor AZD1480 potently inhibits IL-6-induced experimental prostate cancer metastases formation.

Gu L, Talati P, Vogiatzi P, Romero-Weaver AL, Abdulghani J, Liao Z, Leiby B, Hoang DT, Mirtti T, Alanen K, Zinda M, Huszar D, Nevalainen MT.

Mol Cancer Ther. 2014 May;13(5):1246-58. doi: 10.1158/1535-7163.MCT-13-0605. Epub 2014 Feb 27.

13.

Therapeutic inhibition of Jak activity inhibits progression of gastrointestinal tumors in mice.

Stuart E, Buchert M, Putoczki T, Thiem S, Farid R, Elzer J, Huszar D, Waring PM, Phesse TJ, Ernst M.

Mol Cancer Ther. 2014 Feb;13(2):468-74. doi: 10.1158/1535-7163.MCT-13-0583-T. Epub 2014 Jan 7.

14.

AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia.

Keeton EK, McEachern K, Dillman KS, Palakurthi S, Cao Y, Grondine MR, Kaur S, Wang S, Chen Y, Wu A, Shen M, Gibbons FD, Lamb ML, Zheng X, Stone RM, Deangelo DJ, Platanias LC, Dakin LA, Chen H, Lyne PD, Huszar D.

Blood. 2014 Feb 6;123(6):905-13. doi: 10.1182/blood-2013-04-495366. Epub 2013 Dec 20.

15.

Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.

Su Q, Ioannidis S, Chuaqui C, Almeida L, Alimzhanov M, Bebernitz G, Bell K, Block M, Howard T, Huang S, Huszar D, Read JA, Rivard Costa C, Shi J, Su M, Ye M, Zinda M.

J Med Chem. 2014 Jan 9;57(1):144-58. doi: 10.1021/jm401546n. Epub 2013 Dec 20.

PMID:
24359159
16.

Pharmacologic inhibition of Jak2-Stat5 signaling By Jak2 inhibitor AZD1480 potently suppresses growth of both primary and castrate-resistant prostate cancer.

Gu L, Liao Z, Hoang DT, Dagvadorj A, Gupta S, Blackmon S, Ellsworth E, Talati P, Leiby B, Zinda M, Lallas CD, Trabulsi EJ, McCue P, Gomella L, Huszar D, Nevalainen MT.

Clin Cancer Res. 2013 Oct 15;19(20):5658-74. doi: 10.1158/1078-0432.CCR-13-0422. Epub 2013 Aug 13.

17.

The IL-6/JAK/Stat3 feed-forward loop drives tumorigenesis and metastasis.

Chang Q, Bournazou E, Sansone P, Berishaj M, Gao SP, Daly L, Wels J, Theilen T, Granitto S, Zhang X, Cotari J, Alpaugh ML, de Stanchina E, Manova K, Li M, Bonafe M, Ceccarelli C, Taffurelli M, Santini D, Altan-Bonnet G, Kaplan R, Norton L, Nishimoto N, Huszar D, Lyden D, Bromberg J.

Neoplasia. 2013 Jul;15(7):848-62.

18.

A Phase I trial of the kinesin spindle protein (Eg5) inhibitor AZD4877 in patients with solid and lymphoid malignancies.

Gerecitano JF, Stephenson JJ, Lewis NL, Osmukhina A, Li J, Wu K, You Z, Huszar D, Skolnik JM, Schwartz GK.

Invest New Drugs. 2013 Apr;31(2):355-62. doi: 10.1007/s10637-012-9821-y. Epub 2012 May 22.

PMID:
22615058
19.

p63 expression correlates with sensitivity to the Eg5 inhibitor ZD4877 in bladder cancer cells.

Marquis L, Tran M, Choi W, Lee IL, Huszar D, Siefker-Radtke A, Dinney C, McConkey DJ.

Cancer Biol Ther. 2012 May;13(7):477-86. doi: 10.4161/cbt.19590. Epub 2012 May 1.

20.

Comparisons of the efficacy of a Jak1/2 inhibitor (AZD1480) with a VEGF signaling inhibitor (cediranib) and sham treatments in mouse tumors using DCE-MRI, DW-MRI, and histology.

Loveless ME, Lawson D, Collins M, Nadella MV, Reimer C, Huszar D, Halliday J, Waterton JC, Gore JC, Yankeelov TE.

Neoplasia. 2012 Jan;14(1):54-64.

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