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Items: 1 to 50 of 69

1.

Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.

Grimster NP, Anderson E, Alimzhanov M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Gero T, Harsch A, Huszar D, Kawatkar A, Kettle JG, Lyne P, Read JA, Rivard Costa C, Ruston L, Schroeder P, Shi J, Su Q, Throner S, Toader D, Vasbinder M, Woessner R, Wang H, Wu A, Ye M, Zheng W, Zinda M.

J Med Chem. 2018 Jun 28;61(12):5235-5244. doi: 10.1021/acs.jmedchem.8b00076. Epub 2018 Jun 13.

PMID:
29856615
2.

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
3.

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.

4.

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
5.

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.

6.

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.

7.

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
8.

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.

9.

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.

10.

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.

11.

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.

12.

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
13.

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.

14.

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.

15.

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.

16.

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
17.

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.

18.

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.

19.

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
20.

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.

21.

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.

22.

Therapeutic potential of AZD1480 for the treatment of human glioblastoma.

McFarland BC, Ma JY, Langford CP, Gillespie GY, Yu H, Zheng Y, Nozell SE, Huszar D, Benveniste EN.

Mol Cancer Ther. 2011 Dec;10(12):2384-93. doi: 10.1158/1535-7163.MCT-11-0480. Epub 2011 Oct 25.

23.

Antiangiogenic and antimetastatic activity of JAK inhibitor AZD1480.

Xin H, Herrmann A, Reckamp K, Zhang W, Pal S, Hedvat M, Zhang C, Liang W, Scuto A, Weng S, Morosini D, Cao ZA, Zinda M, Figlin R, Huszar D, Jove R, Yu H.

Cancer Res. 2011 Nov 1;71(21):6601-10. doi: 10.1158/0008-5472.CAN-11-1217. Epub 2011 Sep 15.

24.

Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent.

Theoclitou ME, Aquila B, Block MH, Brassil PJ, Castriotta L, Code E, Collins MP, Davies AM, Deegan T, Ezhuthachan J, Filla S, Freed E, Hu H, Huszar D, Jayaraman M, Lawson D, Lewis PM, Nadella MV, Oza V, Padmanilayam M, Pontz T, Ronco L, Russell D, Whitston D, Zheng X.

J Med Chem. 2011 Oct 13;54(19):6734-50. doi: 10.1021/jm200629m. Epub 2011 Sep 7.

PMID:
21899292
25.

A Phase I study to assess the safety, tolerability, and pharmacokinetics of AZD4877, an intravenous Eg5 inhibitor in patients with advanced solid tumors.

Infante JR, Kurzrock R, Spratlin J, Burris HA, Eckhardt SG, Li J, Wu K, Skolnik JM, Hylander-Gans L, Osmukhina A, Huszar D, Herbst RS.

Cancer Chemother Pharmacol. 2012 Jan;69(1):165-72. doi: 10.1007/s00280-011-1667-z. Epub 2011 Jun 3.

PMID:
21638123
26.

Phase I/II multicenter study to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of AZD4877 in patients with refractory acute myeloid leukemia.

Kantarjian HM, Padmanabhan S, Stock W, Tallman MS, Curt GA, Li J, Osmukhina A, Wu K, Huszar D, Borthukar G, Faderl S, Garcia-Manero G, Kadia T, Sankhala K, Odenike O, Altman JK, Minden M.

Invest New Drugs. 2012 Jun;30(3):1107-15. doi: 10.1007/s10637-011-9660-2. Epub 2011 Apr 15.

27.

Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.

Ioannidis S, Lamb ML, Wang T, Almeida L, Block MH, Davies AM, Peng B, Su M, Zhang HJ, Hoffmann E, Rivard C, Green I, Howard T, Pollard H, Read J, Alimzhanov M, Bebernitz G, Bell K, Ye M, Huszar D, Zinda M.

J Med Chem. 2011 Jan 13;54(1):262-76. doi: 10.1021/jm1011319. Epub 2010 Dec 7.

PMID:
21138246
28.

Cooperation among non-relatives evolves by state-dependent generalized reciprocity.

Barta Z, McNamara JM, Huszár DB, Taborsky M.

Proc Biol Sci. 2011 Mar 22;278(1707):843-8. doi: 10.1098/rspb.2010.1634. Epub 2010 Sep 22.

29.

The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors.

Hedvat M, Huszar D, Herrmann A, Gozgit JM, Schroeder A, Sheehy A, Buettner R, Proia D, Kowolik CM, Xin H, Armstrong B, Bebernitz G, Weng S, Wang L, Ye M, McEachern K, Chen H, Morosini D, Bell K, Alimzhanov M, Ioannidis S, McCoon P, Cao ZA, Yu H, Jove R, Zinda M.

Cancer Cell. 2009 Dec 8;16(6):487-97. doi: 10.1016/j.ccr.2009.10.015.

30.

Kinesin motor proteins as targets for cancer therapy.

Huszar D, Theoclitou ME, Skolnik J, Herbst R.

Cancer Metastasis Rev. 2009 Jun;28(1-2):197-208. doi: 10.1007/s10555-009-9185-8. Review.

PMID:
19156502
31.

Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2.

Gozgit JM, Bebernitz G, Patil P, Ye M, Parmentier J, Wu J, Su N, Wang T, Ioannidis S, Davies A, Huszar D, Zinda M.

J Biol Chem. 2008 Nov 21;283(47):32334-43. doi: 10.1074/jbc.M803813200. Epub 2008 Sep 4.

32.

Mice deficient in fractalkine are less susceptible to cerebral ischemia-reperfusion injury.

Soriano SG, Amaravadi LS, Wang YF, Zhou H, Yu GX, Tonra JR, Fairchild-Huntress V, Fang Q, Dunmore JH, Huszar D, Pan Y.

J Neuroimmunol. 2002 Apr;125(1-2):59-65.

PMID:
11960641
33.

Establishment and chimera analysis of 129/SvEv- and C57BL/6-derived mouse embryonic stem cell lines.

Auerbach W, Dunmore JH, Fairchild-Huntress V, Fang Q, Auerbach AB, Huszar D, Joyner AL.

Biotechniques. 2000 Nov;29(5):1024-8, 1030, 1032.

PMID:
11084865
34.

Increased LDL cholesterol and atherosclerosis in LDL receptor-deficient mice with attenuated expression of scavenger receptor B1.

Huszar D, Varban ML, Rinninger F, Feeley R, Arai T, Fairchild-Huntress V, Donovan MJ, Tall AR.

Arterioscler Thromb Vasc Biol. 2000 Apr;20(4):1068-73.

35.

A role for smad6 in development and homeostasis of the cardiovascular system.

Galvin KM, Donovan MJ, Lynch CA, Meyer RI, Paul RJ, Lorenz JN, Fairchild-Huntress V, Dixon KL, Dunmore JH, Gimbrone MA Jr, Falb D, Huszar D.

Nat Genet. 2000 Feb;24(2):171-4.

PMID:
10655064
36.

Targeted deletion of the tub mouse obesity gene reveals that tubby is a loss-of-function mutation.

Stubdal H, Lynch CA, Moriarty A, Fang Q, Chickering T, Deeds JD, Fairchild-Huntress V, Charlat O, Dunmore JH, Kleyn P, Huszar D, Kapeller R.

Mol Cell Biol. 2000 Feb;20(3):878-82.

37.

Hepatic scavenger receptor BI promotes rapid clearance of high density lipoprotein free cholesterol and its transport into bile.

Ji Y, Wang N, Ramakrishnan R, Sehayek E, Huszar D, Breslow JL, Tall AR.

J Biol Chem. 1999 Nov 19;274(47):33398-402.

38.

Decreased selective uptake of high density lipoprotein cholesteryl esters in apolipoprotein E knock-out mice.

Arai T, Rinninger F, Varban L, Fairchild-Huntress V, Liang CP, Chen W, Seo T, Deckelbaum R, Huszar D, Tall AR.

Proc Natl Acad Sci U S A. 1999 Oct 12;96(21):12050-5.

39.

The mahogany protein is a receptor involved in suppression of obesity.

Nagle DL, McGrail SH, Vitale J, Woolf EA, Dussault BJ Jr, DiRocco L, Holmgren L, Montagno J, Bork P, Huszar D, Fairchild-Huntress V, Ge P, Keilty J, Ebeling C, Baldini L, Gilchrist J, Burn P, Carlson GA, Moore KJ.

Nature. 1999 Mar 11;398(6723):148-52.

PMID:
10086355
40.

Response of melanocortin-4 receptor-deficient mice to anorectic and orexigenic peptides.

Marsh DJ, Hollopeter G, Huszar D, Laufer R, Yagaloff KA, Fisher SL, Burn P, Palmiter RD.

Nat Genet. 1999 Jan;21(1):119-22.

PMID:
9916804
41.

Targeted mutation reveals a central role for SR-BI in hepatic selective uptake of high density lipoprotein cholesterol.

Varban ML, Rinninger F, Wang N, Fairchild-Huntress V, Dunmore JH, Fang Q, Gosselin ML, Dixon KL, Deeds JD, Acton SL, Tall AR, Huszar D.

Proc Natl Acad Sci U S A. 1998 Apr 14;95(8):4619-24.

42.

Induction of neuropeptide Y gene expression in the dorsal medial hypothalamic nucleus in two models of the agouti obesity syndrome.

Kesterson RA, Huszar D, Lynch CA, Simerly RB, Cone RD.

Mol Endocrinol. 1997 May;11(5):630-7.

PMID:
9139806
43.

Targeted disruption of the melanocortin-4 receptor results in obesity in mice.

Huszar D, Lynch CA, Fairchild-Huntress V, Dunmore JH, Fang Q, Berkemeier LR, Gu W, Kesterson RA, Boston BA, Cone RD, Smith FJ, Campfield LA, Burn P, Lee F.

Cell. 1997 Jan 10;88(1):131-41.

44.

Phenotypic analysis of mice expressing exclusively apolipoprotein B48 or apolipoprotein B100.

Farese RV Jr, Véniant MM, Cham CM, Flynn LM, Pierotti V, Loring JF, Traber M, Ruland S, Stokowski RS, Huszar D, Young SG.

Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6393-8.

45.
46.

Gene-targeted B-deficient mice reveal a critical role for B cells in the CD4 T cell response.

Liu Y, Wu Y, Ramarathinam L, Guo Y, Huszar D, Trounstine M, Zhao M.

Int Immunol. 1995 Aug;7(8):1353-62.

PMID:
7495742
47.

The site and stage of anti-DNA B-cell deletion.

Chen C, Nagy Z, Radic MZ, Hardy RR, Huszar D, Camper SA, Weigert M.

Nature. 1995 Jan 19;373(6511):252-5.

48.

Human antibodies from transgenic mice.

Lonberg N, Huszar D.

Int Rev Immunol. 1995;13(1):65-93. Review.

PMID:
7494109
49.

Antibody response elicited by T-dependent and T-independent antigens in gene targeted kappa-deficient mice.

Pricop L, Brumeanu T, Elahi E, Moran T, Wang BS, Troustine M, Huszar D, Alt F, Bona C.

Int Immunol. 1994 Dec;6(12):1839-47.

PMID:
7535094
50.

Light chain editing in kappa-deficient animals: a potential mechanism of B cell tolerance.

Prak EL, Trounstine M, Huszar D, Weigert M.

J Exp Med. 1994 Nov 1;180(5):1805-15.

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