Publications

2016

Wu H, Hu C, Wang A, Weisberg EL, Chen Y, Yun C-H, Wang W, Liu Y, Liu X, Tian B, Wang J, Zhao Z, Liang Y. Li B, Wang L, Wang B, Chen C, Buhrlage SJ, Qi Z, Zou F, Nonami A, Li Y, Fernandes SM,  Adamia S, Stone RM, Galinsky IA, Wang X, YangG, Griffin JD, Brown JR, Eck MJ, Liu J, Gray NS, Liu Q. Discovery of a BTK/MNK dual inhibitor for lymphoma and leukemia. Leukemia (2016) 30, 173–181

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Ferguson FM, Ni J, Zhang T, Tesar B, Sim T, Kim ND, Deng X, Brown JR, Zhao JJ, Gray NS. Discovery of a Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-δ/γ Inhibitors. ACS Med Chem Lett. 2016 Aug 2;7(10):908-912.

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Wein MN, Liang Y, Goransson O, Sundberg TB, Wang J, Williams EA, O'Meara MJ, Govea N, Beqo B, Nishimori S, Nagano K, Brooks DJ, Martins JS, Corbin B, Anselmo A, Sadreyev R, Wu JY, Sakamoto K, Foretz M, Xavier RJ, Baron R, Bouxsein ML, Gardella TJ, Divieti-Pajevic P, Gray NS, Kronenberg HM. SIKs control osteocyte responses to parathyroid hormone. Nat Commun. 2016 Oct 19;7:13176. doi: 10.1038/ncomms13176.

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Wang A, Yan XE, Wu H, Wang W, Hu C, Chen C, Zhao Z, Zhao P, Li X, Wang L, Wang B, Ye Z, Wang J, Wang C, Zhang W, Gray NS, Weisberg EL, Chen L, Liu J, Yun CH, Liu Q. Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation. Oncotarget. 2016 Oct 25;7(43):69760-69769.

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Zhang T, Kwiatkowski N, Olson CM, Dixon-Clarke SE, Abraham BJ, Greifenberg AK, Ficarro SB, Elkins JM, Liang Y, Hannett NM, Manz T, Hao M, Bartkowiak B, Greenleaf AL, Marto JA, Geyer M, Bullock AN, Young RA, Gray NS. Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors. Nat Chem Biol. 2016 Oct;12(10):876-84.

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Fan F, He Z, Kong LL, Chen Q, Yuan Q, Zhang S, Ye J, Liu H, Sun X, Geng J, Yuan L, Hong L, Xiao C, Zhang W, Sun X, Li Y, Wang P, Huang L, Wu X, Ji Z, Wu Q, Xia NS, Gray NS, Chen L, Yun CH, Deng X, Zhou D. Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration. Sci Transl Med. 2016 Aug 17;8(352):352ra108.

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Wang Y, Begley M, Li Q, Huang HT, Lako A, Eck MJ, Gray NS, Mitchison TJ, Cantley LC, Zhao JJ. Mitotic MELK-eIF4B signaling controls protein synthesis and tumor cell survival. Proc Natl Acad Sci U S A. 2016 Aug 30;113(35):9810-5.

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Williams CA, Fernandez-Alonso R, Wang J, Toth R, Gray NS, Findlay GM. Erk5 Is a Key Regulator of Naive-Primed Transition and Embryonic Stem Cell Identity. Cell Rep. 2016 Aug 16;16(7):1820-8.

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Miranda F, Mannion D, Liu S, Zheng Y, Mangala LS, Redondo C, Herrero-Gonzalez S, Xu R, Taylor C, Chedom DF, Karaminejadranjbar M, Albukhari A, Jiang D, Pradeep S, Rodriguez-Aguayo C, Lopez-Berestein G, Salah E, Abdul Azeez KR, Elkins JM, Campo L, Myers KA, Klotz D, Bivona S, Dhar S, Bast RC Jr, Saya H, Choi HG, Gray NS, Fischer R, Kessler BM, Yau C, Sood AK, Motohara T, Knapp S, Ahmed AA. Salt-Inducible Kinase 2 Couples Ovarian Cancer Cell Metabolism with Survival at the Adipocyte-Rich Metastatic Niche. Cancer Cell. 2016 Aug 8;30(2):273-89.

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Iorio F, Knijnenburg TA, Vis DJ, Bignell GR, Menden MP, Schubert M, Aben N, Gonçalves E, Barthorpe S, Lightfoot H, Cokelaer T, Greninger P, van Dyk E, Chang H, de Silva H, Heyn H, Deng X, Egan RK, Liu Q, Mironenko T, Mitropoulos X, Richardson L, Wang J, Zhang T, Moran S, Sayols S, Soleimani M, Tamborero D, Lopez-Bigas N, Ross-Macdonald P, Esteller M, Gray NS, Haber DA, Stratton MR, Benes CH, Wessels LF, Saez-Rodriguez J, McDermott U, Garnett MJ. A Landscape of Pharmacogenomic Interactions in Cancer. Cell. 2016 Jul 28;166(3):740-54.

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Brown W, Tan L, Smith A, Gray NS, Wendt M. Covalent targeting of fibroblast growth factor receptor inhibits metastatic breast cancer. Mol Cancer Ther. 2016 Sep;15(9):2096-106.

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Chong CR, Bahcall M, Capelletti M, Kosaka T, Ercan D, Sim T, Sholl LM, Nishino M, Johnson BE, Gray NS, Janne PA. Identification of existing drugs that effectively target NTRK1- and ROS1-rearrangements in lung cancer. Clin Cancer Res. 2017 Jan 1;23(1):204-213.

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Lee S, Shang Y, Redmond SA, Urisman A, Tang AA, Li KH, Burlingame AL, Pak RA, Jovicic A, Gitler AD, Wang J, Gray NS, Seeley WW, Siddique T, Bigio EH, Lee VM, Trojanowski JQ, Chan JR, Huang EJ. Activation of HIPK2 Promotes ER Stress-Mediated Neurodegeneration in Amyotrophic Lateral Sclerosis. Neuron. 2016 Jul 6;91(1):41-55.

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Sundberg TB, Liang Y, Wu H, Choi HG, Kim ND, Sim T, Johannessen L, Petrone A, Khor B, Graham DB, Latorre IJ, Phillips AJ, Schreiber SL, Perez J, Shamji AF, Gray NS, Xavier RJ. Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function In Vivo. ACS Chem Biol. 2016 11(8):2105-2111.

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Hatcher JM, Weisberg E, Sim T, Stone RM, Liu S, Griffin JD, Gray NS. Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor. ACS Med Chem Lett. 2016 Mar 8;7(5):476-81.

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Matthews JM, Bhatt S, Patricelli MP, Nomanbhoy TK, Jiang X, Natkunam Y, Gentles AJ, Martinez E, Zhu D, Chapman JR, Cortizas E, Shyam R, Chinichian S, Advani R, Tan L, Zhang J, Choi HG, Tibshirani R, Buhrlage SJ, Gratzinger D, Verdun R, Gray NS, Lossos IS. Pathophysiological significance and therapeutic targeting of germinal center kinase in diffuse large B-cell lymphoma. Blood. 2016 Jul 14;128(2):239-48.

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Yang G, Buhrlage S, Tan L, Liu X, Chen J, Xu L, Tsakmaklis N, Chen JG, Patterson CJ, Brown JR, Castillo JJ, Zhang W, Zhang X, Liu S, Cohen P, Hunter ZR, Gray N, Treon SP. HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib. Blood. 2016 Jun 23;127(25):3237-52.

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Udayakumar D, Pandita RK, Horikoshi N, Liu Y, Liu Q, Wong KK, Hunt CR, Gray NS, Minna JD, Pandita TK, Westover KD. Torin2 Suppresses Ionizing Radiation-Induced DNA Damage Repair. Radiat Res. 2016 May;185(5):527-38.

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Pacold ME, Brimacombe KR, Chan SH, Rohde JM, Lewis CA, Swier LJ, Possemato R, Chen WW, Sullivan LB, Fiske BP, Cho S, Freinkman E, Birsoy K, Abu-Remaileh M, Shaul YD, Liu CM, Zhou M, Koh MJ, Chung H, Davidson SM, Luengo A, Wang AQ, Xu X, Yasgar A, Liu L, Rai G, Westover KD, Vander Heiden MG, Shen M, Gray NS, Boxer MB, Sabatini DM. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol. 2016 Jun;12(6):452-8.

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Clark MJ, Miduturu C, Schmidt AG, Zhu X, Pitts JD, Wang J, Potisopon S, Zhang J, Wojciechowski A, Hann Chu JJ, Gray NS, Yang PL. GNF-2 Inhibits Dengue Virus by Targeting Abl Kinases and the Viral E Protein. Cell Chem Biol. 2016 Apr 21;23(4):443-52.

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Liu F, Wang J, Yang X, Li B, Wu H, Qi S, Chen C, Liu X, Yu K, Wang W, Zhao Z, Wang A, Chen YF, Wang L, Gray NS, Liu J, Zhang X, Liu Q. Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem Biol. 2016 Jun 17;11(6):1537-43.

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Liu X, Hunter ZR, Xu L, Chen J, Chen JG, Tsakmaklis N, Patterson CJ, Castillo JJ, Buhrlage S, Gray N, Treon SP, Yang G. Targeting Myddosome Assembly in Waldenstrom Macroglobulinaemia. Br J Haematol. 2016 Apr 13. doi: 10.1111/bjh.14103.

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Ho CM, Donovan-Banfield IZ, Tan L, Zhang T, Gray NS, Strang BL. Inhibition of IKKa by BAY61-3606 Reveals IKKa-Dependent Histone H3 Phosphorylation in Human Cytomegalovirus Infected Cells. PLoS One. 2016 Mar 1;11(3):e0150339.

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Nishikawa JL, Boeszoermenyi A, Vale-Silva LA, Torelli R, Posteraro B, Sohn YJ, Ji F, Gelev V, Sanglard D, Sanguinetti M, Sadreyev RI, Mukherjee G, Bhyravabhotla J, Buhrlage SJ, Gray NS, Wagner G, Näär AM, Arthanari H. Inhibiting fungal multidrug resistance by disrupting an activator-Mediator interaction. Nature. 2016 Feb 25;530(7591):485-9.

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Amato KR, Wang S, Tan L, Hastings AK, Song W, Lovly CM, Meador CB, Ye F, Lu P, Balko JM, Colvin DC, Cates JM, Pao W, Gray NS, Chen J. EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer. Cancer Res. 2016 Jan 15;76(2):305-18.

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Neel VA, Todorova K, Wang J, Kwon E, Kang M, Liu Q, Gray N, Lee SW, Mandinova A. Sustained Akt activity is required to maintain cell viability in seborrheic keratosis, a benign epithelial tumor. J Invest Dermatol. 2015 Dec 28.

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Maxson JE, Abel ML, Wang J, Deng X, Reckel S, Luty SB, Sun H, Gorenstein J, Hughes SB, Bottomly D, Wilmot B, McWeeney SK, Radich J, Hantschel O, Middleton RE, Gray NS, Druker BJ, Tyner JW. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis. Cancer Res. 2015 Dec 17.

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Ye S, Zhang J, Shen J, Gao Y, Li Y, Choy E, Cote G, Harmon D, Mankin H, Gray NS, Hornicek FJ, Duan Z. NVP-TAE684 reverses multidrug resistance (MDR) in human osteosarcoma by inhibiting P-glycoprotein (Pgp) function. Br J Pharmacol. 2015 Nov 25.

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