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Items: 33

1.

BRD4 facilitates replication stress-induced DNA damage response.

Zhang J, Dulak AM, Hattersley MM, Willis BS, Nikkilä J, Wang A, Lau A, Reimer C, Zinda M, Fawell SE, Mills GB, Chen H.

Oncogene. 2018 Apr 11. doi: 10.1038/s41388-018-0194-3. [Epub ahead of print]

PMID:
29636547
2.

Comparative analysis of primary versus relapse/refractory DLBCL identifies shifts in mutation spectrum.

Greenawalt DM, Liang WS, Saif S, Johnson J, Todorov P, Dulak A, Enriquez D, Halperin R, Ahmed A, Saveliev V, Carpten J, Craig D, Barrett JC, Dougherty B, Zinda M, Fawell S, Dry JR, Byth K.

Oncotarget. 2017 Jun 15;8(59):99237-99244. doi: 10.18632/oncotarget.18502. eCollection 2017 Nov 21.

3.

Generation of stable PDX derived cell lines using conditional reprogramming.

Borodovsky A, McQuiston TJ, Stetson D, Ahmed A, Whitston D, Zhang J, Grondine M, Lawson D, Challberg SS, Zinda M, Pollok BA, Dougherty BA, D'Cruz CM.

Mol Cancer. 2017 Dec 6;16(1):177. doi: 10.1186/s12943-017-0745-1.

4.

Targeting KRAS-dependent tumors with AZD4785, a high-affinity therapeutic antisense oligonucleotide inhibitor of KRAS.

Ross SJ, Revenko AS, Hanson LL, Ellston R, Staniszewska A, Whalley N, Pandey SK, Revill M, Rooney C, Buckett LK, Klein SK, Hudson K, Monia BP, Zinda M, Blakey DC, Lyne PD, Macleod AR.

Sci Transl Med. 2017 Jun 14;9(394). pii: eaal5253. doi: 10.1126/scitranslmed.aal5253. Erratum in: Sci Transl Med. 2017 Jul 26;9(400):.

PMID:
28615361
5.

Target Deconvolution Efforts on Wnt Pathway Screen Reveal Dual Modulation of Oxidative Phosphorylation and SERCA2.

Casás-Selves M, Zhang AX, Dowling JE, Hallén S, Kawatkar A, Pace NJ, Denz CR, Pontz T, Garahdaghi F, Cao Q, Sabirsh A, Thakur K, O'Connell N, Hu J, Cornella-Taracido I, Weerapana E, Zinda M, Goodnow RA Jr, Castaldi MP.

ChemMedChem. 2017 Jun 21;12(12):917-924. doi: 10.1002/cmdc.201700028. Epub 2017 Apr 26.

PMID:
28371485
6.

AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies.

Rhyasen GW, Hattersley MM, Yao Y, Dulak A, Wang W, Petteruti P, Dale IL, Boiko S, Cheung T, Zhang J, Wen S, Castriotta L, Lawson D, Collins M, Bao L, Ahdesmaki MJ, Walker G, O'Connor G, Yeh TC, Rabow AA, Dry JR, Reimer C, Lyne P, Mills GB, Fawell SE, Waring MJ, Zinda M, Clark E, Chen H.

Mol Cancer Ther. 2016 Nov;15(11):2563-2574. Epub 2016 Aug 29.

7.

Effective combination therapies in preclinical endocrine resistant breast cancer models harboring ER mutations.

Ladd B, Mazzola AM, Bihani T, Lai Z, Bradford J, Collins M, Barry E, Goeppert AU, Weir HM, Hearne K, Renshaw JG, Mohseni M, Hurt E, Jalla S, Bao H, Hollingsworth R, Reimer C, Zinda M, Fawell S, D'Cruz CM.

Oncotarget. 2016 Aug 23;7(34):54120-54136. doi: 10.18632/oncotarget.10852.

8.

Acquired savolitinib resistance in non-small cell lung cancer arises via multiple mechanisms that converge on MET-independent mTOR and MYC activation.

Henry RE, Barry ER, Castriotta L, Ladd B, Markovets A, Beran G, Ren Y, Zhou F, Adam A, Zinda M, Reimer C, Qing W, Su W, Clark E, D'Cruz CM, Schuller AG.

Oncotarget. 2016 Sep 6;7(36):57651-57670. doi: 10.18632/oncotarget.10859.

9.

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
10.

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.

11.

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
12.

Tumors with AKT1E17K Mutations Are Rational Targets for Single Agent or Combination Therapy with AKT Inhibitors.

Davies BR, Guan N, Logie A, Crafter C, Hanson L, Jacobs V, James N, Dudley P, Jacques K, Ladd B, D'Cruz CM, Zinda M, Lindemann J, Kodaira M, Tamura K, Jenkins EL.

Mol Cancer Ther. 2015 Nov;14(11):2441-51. doi: 10.1158/1535-7163.MCT-15-0230. Epub 2015 Sep 8.

13.

The MET Inhibitor AZD6094 (Savolitinib, HMPL-504) Induces Regression in Papillary Renal Cell Carcinoma Patient-Derived Xenograft Models.

Schuller AG, Barry ER, Jones RD, Henry RE, Frigault MM, Beran G, Linsenmayer D, Hattersley M, Smith A, Wilson J, Cairo S, Déas O, Nicolle D, Adam A, Zinda M, Reimer C, Fawell SE, Clark EA, D'Cruz CM.

Clin Cancer Res. 2015 Jun 15;21(12):2811-9. doi: 10.1158/1078-0432.CCR-14-2685. Epub 2015 Mar 16.

14.

Resistance to everolimus driven by epigenetic regulation of MYC in ER+ breast cancers.

Bihani T, Ezell SA, Ladd B, Grosskurth SE, Mazzola AM, Pietras M, Reimer C, Zinda M, Fawell S, D'Cruz CM.

Oncotarget. 2015 Feb 10;6(4):2407-20.

15.

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.

16.

Discovery of 6-aryl-azabenzimidazoles that inhibit the TBK1/IKK-ε kinases.

Johannes JW, Chuaqui C, Cowen S, Devereaux E, Gingipalli L, Molina A, Wang T, Whitston D, Wu X, Zhang HJ, Zinda M.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1138-43. doi: 10.1016/j.bmcl.2013.12.123. Epub 2014 Jan 13.

PMID:
24462666
17.

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
18.

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.

19.

Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.

Guan H, Lamb ML, Peng B, Huang S, Degrace N, Read J, Hussain S, Wu J, Rivard C, Alimzhanov M, Bebernitz G, Bell K, Ye M, Zinda M, Ioannidis S.

Bioorg Med Chem Lett. 2013 May 15;23(10):3105-10. doi: 10.1016/j.bmcl.2013.02.111. Epub 2013 Mar 7.

PMID:
23562594
20.

Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKε kinases.

Wang T, Block MA, Cowen S, Davies AM, Devereaux E, Gingipalli L, Johannes J, Larsen NA, Su Q, Tucker JA, Whitston D, Wu J, Zhang HJ, Zinda M, Chuaqui C.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):2063-9. doi: 10.1016/j.bmcl.2012.01.018. Epub 2012 Jan 14.

PMID:
22305584
21.

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.

22.

In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.

Wang T, Ioannidis S, Almeida L, Block MH, Davies AM, Lamb ML, Scott DA, Su M, Zhang HJ, Alimzhanov M, Bebernitz G, Bell K, Zinda M.

Bioorg Med Chem Lett. 2011 May 15;21(10):2958-61. doi: 10.1016/j.bmcl.2011.03.053. Epub 2011 Mar 21.

PMID:
21493067
23.

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
24.

Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors.

Ioannidis S, Lamb ML, Almeida L, Guan H, Peng B, Bebernitz G, Bell K, Alimzhanov M, Zinda M.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1669-73. doi: 10.1016/j.bmcl.2010.01.091. Epub 2010 Jan 25.

PMID:
20144546
25.

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.

26.

Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.

Ioannidis S, Lamb ML, Davies AM, Almeida L, Su M, Bebernitz G, Ye M, Bell K, Alimzhanov M, Zinda M.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6524-8. doi: 10.1016/j.bmcl.2009.10.054. Epub 2009 Oct 24.

PMID:
19857966
27.

Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase.

Scott DA, Balliet CL, Cook DJ, Davies AM, Gero TW, Omer CA, Poondru S, Theoclitou ME, Tyurin B, Zinda MJ.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):697-700. doi: 10.1016/j.bmcl.2008.12.046. Epub 2008 Dec 24.

PMID:
19112018
28.

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.

29.

AKT-1, -2, and -3 are expressed in both normal and tumor tissues of the lung, breast, prostate, and colon.

Zinda MJ, Johnson MA, Paul JD, Horn C, Konicek BW, Lu ZH, Sandusky G, Thomas JE, Neubauer BL, Lai MT, Graff JR.

Clin Cancer Res. 2001 Aug;7(8):2475-9.

31.

Ceramide induces the dephosphorylation and inhibition of constitutively activated Akt in PTEN negative U87mg cells.

Zinda MJ, Vlahos CJ, Lai MT.

Biochem Biophys Res Commun. 2001 Feb 2;280(4):1107-15.

PMID:
11162641
32.
33.

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