recent publications
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academic article
- Yang, Q., Liao, L., Deng, X., Chen, R., Gray, N. S., Yates, J. R., Lee, J. D. BMK1 is involved in the regulation of p53 through disrupting the PML-MDM2 interaction Oncogene 2013 32:3156-3164 DOI:10.1038/onc.2012.332 PMID:22869143 PMCID:PMC3493705
- Deng, X., Elkins, J. M., Zhang, J., Yang, Q., Erazo, T., Gomez, N., Choi, H. G., Wang, J., Dzamko, N., Lee, J. D., Sim, T., Kim, N., et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo e pyrimido- 5,4-b diazepine-6(11H)-ones European Journal of Medicinal Chemistry 2013 70:758-767 DOI:10.1016/j.ejmech.2013.10.052 PMID:24239623 PMCID:PMC3914206
- Zhang, T., Inesta-Vaquera, F., Niepel, M., Zhang, J. M., Ficarro, S. B., Machleidt, T., Xie, T., Marto, J. A., Kim, N., Sim, T., Laughlin, J. D., Park, H., et al. Discovery of potent and selective covalent inhibitors of JNK Chemistry & Biology 2012 19:140-154 DOI:10.1016/j.chembiol.2011.11.010 PMID:22284361 PMCID:PMC3270411
- Deng, X. M., Dzamko, N., Prescott, A., Davies, P., Liu, Q. S., Yang, Q. K., Lee, J. D., Patricelli, M. P., Nomanbhoy, T. K., Alessi, D. R., Gray, N. S. Characterization of a selective inhibitor of the parkinson's disease kinase lrrk2 Nature Chemical Biology 2011 7:203-205 DOI:10.1038/nchembio.538 PMID:21378983 PMCID:PMC3287420
- Deng, X., Yang, Q., Kwiatkowski, N., Sim, T., McDermott, U., Settleman, J. E., Lee, J. D., Gray, N. S. Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a potent and selective inhibitor of Big MAP Kinase 1 ACS Medicinal Chemistry Letters 2011 2:195-200 DOI:10.1021/ml100304b PMID:21412406 PMCID:PMC3055678
- Miduturu, C. V., Deng, X. M., Kwiatkowski, N., Yang, W. N. A., Brault, L., Filippakopoulos, P., Chung, E., Yang, Q. K., Schwaller, J., Knapp, S., King, R. W., Lee, J. D., et al. High-throughput kinase profiling: A more efficient approach toward the discovery of new kinase inhibitors Chemistry & Biology 2011 18:868-879 DOI:10.1016/j.chembiol.2011.05.010 PMID:21802008 PMCID:PMC3171802
- Patricelli, M. P., Nomanbhoy, T. K., Wu, J., Brown, H., Zhou, D., Zhang, J. M., Jagannathan, S., Aban, A., Okerberg, E., Herring, C., Nordin, B., Weissig, H., et al. In situ kinase profiling reveals functionally relevant properties of native kinases Chemistry & Biology 2011 18:699-710 DOI:10.1016/j.chembiol.2011.04.011 PMID:21700206 PMCID:PMC3142620
- Deng, X. M., Nagle, A., Wu, T., Sakata, T., Henson, K., Chen, Z., Kuhen, K., Plouffe, D., Winzeler, E., Adrian, F., Tuntland, T., Chang, J., et al. Discovery of novel 1h-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials Bioorganic & Medicinal Chemistry Letters 2010 20:4027-4031 DOI:10.1016/j.bmcl.2010.05.095 PMID:20610151
- Yang, Q. K., Deng, X. M., Lu, B. W., Cameron, M., Fearns, C., Patricelli, M. P., Yates, J. R., Gray, N. S., Lee, J. D. Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein Cancer Cell 2010 18:258-267 DOI:10.1016/j.ccr.2010.08.008 PMID:20832753 PMCID:PMC2939729
- Goldsmith, M., Avni, D., Levy-Rimler, G., Mashiach, R., Ernst, O., Levi, M., Webb, B., Meijler, M. M., Gray, N. S., Rosen, H., Zor, T. A ceramide-1-phosphate analogue, pcera-1, simultaneously suppresses tumour necrosis factor-alpha and induces interleukin-10 production in activated macrophages Immunology 2009 127:103-115 DOI:10.1111/j.1365-2567.2008.02928.x PMID:18793216 PMCID:PMC2678186
- Wu, T., Nagle, A., Sakata, T., Henson, K., Borboa, R., Chen, Z., Kuhen, K., Plouffe, D., Winzeler, E., Adrian, F., Tuntland, T., Chang, J., et al. Cell-based optimization of novel benzamides as potential antimalarial leads Bioorganic & Medicinal Chemistry Letters 2009 19:6970-6974 DOI:10.1016/j.bmcl.2009.10.050 PMID:19879133 PMCID:PMC3532596
- Avni, D., Goldsmith, M., Ernst, O., Mashiach, R., Tuntland, T., Meijler, M. M., Gray, N. S., Rosen, H., Zor, T. Modulation of tnf alpha, il-10 and il-12p40 levels by a ceramide-1-phosphate analog, pcera-1, in vivo and ex vivo in primary macrophages Immunology Letters 2009 123:1-8 DOI:10.1016/j.imlet.2008.12.011 PMID:19185589
- Plouffe, D., Brinker, A., McNamara, C., Henson, K., Kato, N., Kuhen, K., Nagle, A., Adrian, F., Matzen, J. T., Anderson, P., Nam, T. G., Gray, N. S., et al. In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen Proceedings of the National Academy of Sciences of the United States of America 2008 105:9059-9064 DOI:10.1073/pnas.0802982105 PMID:18579783 PMCID:PMC2440361
- Hong, J. Y., Lee, J., Min, K. H., Walker, J. R., Peters, E. C., Gray, N. S., Cho, C. Y., Schultz, P. G. Identification and characterization of small-molecule inducers of epidermal keratinocyte differentiation ACS Chemical Biology 2007 2:171-175 DOI:10.1021/cb600435t PMID:17348628
- Galkin, A. V., Mellnick, J. S., Kim, S., Hood, T. L., Li, N. X., Li, L. T., Xia, G., Steensma, R., Chopiuk, G., Jiang, J. Q., Wan, Y. Q., Ding, P., et al. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK Proceedings of the National Academy of Sciences of the United States of America 2007 104:270-275 DOI:10.1073/pnas.0609412103 PMID:17185414 PMCID:PMC1765448
- Melnick, J. S., Janes, J., Kim, S., Chang, J. Y., Sipes, D. G., Gunderson, D., Jarnes, L., Matzen, J. T., Garcia, M. E., Hood, T. L., Beigi, R., Xia, G., et al. An efficient rapid system for profiling the cellular activities of molecular libraries Proceedings of the National Academy of Sciences of the United States of America 2006 103:3153-3158 DOI:10.1073/pnas.0511292103 PMID:16492761 PMCID:PMC1413928
- Luesch, H., Wu, T. Y. H., Ren, P. D., Gray, N. S., Schultz, P. G., Supek, F. A genome-wide overexpression screen in yeast for small-molecule target identification Chemistry & Biology 2005 12:55-63 DOI:10.1016/j.chembiol.2004.10.015 PMID:15664515
- Wignall, S. M., Gray, N. S., Chang, Y. T., Juarez, L., Jacob, R., Burlingame, A., Schultz, P. G., Heald, R. Identification of a novel protein regulating microtubule stability through a chemical approach Chemistry & Biology 2004 11:135-146 DOI:10.1016/j.chembiol.2003.12.019 PMID:15113003
- Wu, X., Ding, S., Ding, G., Gray, N. S., Schultz, P. G. Small molecules that induce cardiomyogenesis in embryonic stem cells Journal of the American Chemical Society 2004 126:1590-1591 DOI:10.1021/ja038950i PMID:14871063
- Ding, S., Wu, T. Y. H., Brinker, A., Peters, E. C., Hur, W., Gray, N. S., Schultz, P. G. Synthetic small molecules that control stem cell fate Proceedings of the National Academy of Sciences of the United States of America 2003 100:7632-7637 DOI:10.1073/pnas.0732087100 PMID:12794184 PMCID:PMC164638
- Ding, S., Gray, N. S., Wu, X., Ding, Q., Schultz, P. G. A combinatorial scaffold approach toward kinase-directed heterocycle libraries Journal of the American Chemical Society 2002 124:1594-1596 DOI:10.1021/ja0170302 PMID:11853431
- Wu, X., Ding, S., Ding, Q., Gray, N. S., Schultz, P. G. A small molecule with osteogenesis-inducing activity in multipotent mesenchymal progenitor cells Journal of the American Chemical Society 2002 124:14520-14521 DOI:10.1021/ja0283908 PMID:12465946
- Chang, Y. T., Choi, G., Bae, Y. S., Burdett, M., Moon, H. S., Lee, J. W., Gray, N. S., Schultz, P. G., Meijer, L., Chung, S. K., Choi, K. Y., Suh, P. G., et al. Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase ChemBioChem 2002 3:897-901 DOI:10.1002/1439-7633(20020902)3:9<897::aid-cbic897>3.0.co;2-b PMID:12210991
- Ding, S., Gray, N. S., Ding, Q., Wu, X., Schultz, P. G. Resin-capture and release strategy toward combinatorial libraries of 2,6,9-substituted purines Journal of Combinatorial Chemistry 2002 4:183-186 DOI:10.1021/cc010080i PMID:11886295
- Ding, S., Gray, N. S., Ding, Q., Schultz, P. G. A concise and traceless linker strategy toward combinatorial libraries of 2,6,9-substituted purines Journal of Organic Chemistry 2001 66:8273-8276 DOI:10.1021/jo016010f PMID:11722241
- Lin, Q., Jiang, F. Y., Schultz, P. G., Gray, N. S. Design of allele-specific protein methyltransferase inhibitors Journal of the American Chemical Society 2001 123:11608-11613 DOI:10.1021/ja011423j PMID:11716715
- Ding, S., Gray, N. S., Ding, Q., Schultz, P. G. Expanding the diversity of purine libraries Tetrahedron Letters 2001 42:8751-8755 DOI:10.1016/s0040-4039(01)01925-6
- Wu, T. Y. H., Ding, S., Gray, N. S., Schultz, P. G. Solid-phase synthesis of 2,3,5-trisubstituted indoles Organic Letters 2001 3:3827-3830 DOI:10.1021/ol016525t PMID:11720546
- Chang, Y. T., Wignall, S. M., Rosania, G. R., Gray, N. S., Hanson, S. R., Su, A. I., Merlie, J., Moon, H. S., Sangankar, S. B., Perez, O., Heald, R., Schultz, P. G. Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors Journal of Medicinal Chemistry 2001 44:4497-4500 DOI:10.1021/jm010451+ PMID:11741468
- Bishop, A. C., Ubersax, J. A., Petsch, D. T., Matheos, D. P., Gray, N. S., Blethrow, J., Shimizu, E., Tsien, J. Z., Schultz, P. G., Rose, M. D., Wood, J. L., Morgan, D. O., et al. A chemical switch for inhibitor-sensitive alleles of any protein kinase Nature 2000 407:395-401 PMID:11014197
- Armstrong, J. I., Portley, A. R., Chang, Y. T., Nierengarten, D. M., Cook, B. N., Bowman, K. G., Bishop, A., Gray, N. S., Shokat, K. M., Schultz, P. G., Bertozzi, C. R. Discovery of carbohydrate sulfotransferase inhibitors from a kinase-directed library Angewandte Chemie-International Edition 2000 39:1303-1306 DOI:10.1002/(sici)1521-3773(20000403)39:7<1303::aid-anie1303>3.0.co;2-0 PMID:10767039
- Chang, Y. T., Gray, N. S., Rosania, G. R., Sutherlin, D. P., Kwon, S., Norman, T. C., Sarohia, R., Leost, M., Meijer, L., Schultz, P. G. Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors Chemistry & Biology 1999 6:361-375 DOI:10.1016/s1074-5521(99)80048-9 PMID:10375538
- Gray, N. S., Wodicka, L., Thunnissen, Amwh, Norman, T. C., Kwon, S. J., Espinoza, F. H., Morgan, D. O., Barnes, G., LeClerc, S., Meijer, L., Kim, S. H., Lockhart, D. J., et al. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors Science 1998 281:533-538 DOI:10.1126/science.281.5376.533 PMID:9677190
- Brooks, E. E., Gray, N. S., Joly, A., Kerwar, S. S., Lum, R., Mackman, R. L., Norman, T. C., Rosete, J., Rowe, M., Schow, S. R., Schultz, P. G., Wang, X. B., et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation Journal of Biological Chemistry 1997 272:29207-29211 DOI:10.1074/jbc.272.46.29207 PMID:9360999
- Gray, N. S., Kwon, S., Schultz, P. G. Combinatorial synthesis of 2,9-substituted purines Tetrahedron Letters 1997 38:1161-1164 DOI:10.1016/s0040-4039(97)00014-2
- Norman, T. C., Gray, N. S., Koh, J. T., Schultz, P. G. A structure-based library approach to kinase inhibitors Journal of the American Chemical Society 1996 118:7430-7431 DOI:10.1021/ja9614934
- Patten, P. A., Gray, N. S., Yang, P. L., Marks, C. B., Wedemayer, G. J., Boniface, J. J., Stevens, R. C., Schultz, P. G. The immunological evolution of catalysis Science 1996 271:1086-1091 DOI:10.1126/science.271.5252.1086 PMID:8599084