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(106) Direct Publications in 2009


  1. Triple hybrids of steroids, spiroketals, and oligopeptides as new biomolecular chimeras. Banerjee, A., Sergienko, E., Vasile, S., Gupta, V., Vuori, K., Wipf, P. Org. Lett., 2009, 11(1): 65-8.
  2. Small molecule DnaK modulators targeting the beta-domain. Cellitti, J., Zhang, Z., Wang, S., Wu, B., Yuan, H., Hasegawa, P., Guiney, D.G., Pellecchia, M. Chem Biol Drug Des., 2009, 74(4):349-57.
  3. Discovery and validation of a series of aryl sulfonamides as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP). Dahl, R., Sergienko, E.A., Su, Y., Mostofi, Y.S., Yang, L., Simao, A.M., Narisawa, S., Brown, B., Mangravita-Novo, A., Vicchiarelli, M., Smith, L.H., O’Neill, W.C., Millán, J.L., Cosford, N. J Med Chem, 2009, 52(21):6919-25.
  4. Versatile Assays for High Throughput Screening for Activators or Inhibitors of Intracellular Proteases and their Cellular Regulators. Hayashi, H., Cuddy, M., Yip, K.W., Madiraju, C., Diaz, P., Vasile, S., Sergienko, E., Reed, J.C. PLoS One, 2009, 4(10):e7655.
  5. Chemical biology investigation of cell death pathways activated by endoplasmic reticulum stress reveals cytoprotective modulators of ASK1 Kim, I., Shu, C.W., Xu, W., Shiau, C.W., Grant, D., Vasile, S., Cosford, N.D., & Reed, J.C. J Biol Chem, 2009, 284(3):1593-1603.
  6. Lentiviral Vectors and Protocols for Creation of Stable hESC Lines for Fluorescent Tracking and Drug Resistance Selection of Cardiomyocytes. Kita-Matsu, H., Barcova, M., Prighozhina, N., Salomonis, N., Wei, K., Jacot, J.G., Nelson, B., Spiering, S., Haverslag, R., Kim, C., Talantova, M., McCulloch, A.D., Conklin, B.R., Price, J.H., Chen, H.S.V., Mercola, M. PLoS ONE, 2009, 4(4):e5046.
  7. XIAP mediates NOD signaling via interaction with RIP2. Krieg, A., Correa, R.G., Garrison, J.B., Le Negrate, G., Welsh, K., Huang, Z., Knoefel, W.T., Reed, J.C. Proc Natl Acad Sci USA, 2009, 106(34):14524-9.
  8. Engineering a leucine zipper-TRAIL homotrimer with improved cytotoxicity in tumor cells. Rozanov, D., Savinov, A., Golubkov, V., Rozanova, O., Postnova, T., Sergienko, E., Vasile, S., Aleshin, A., Rega, M., Pellecchia, M., Strongin, A. Mol. Cancer. Ther., 2009, 6:1515-25.
  9. Identification and Characterization of Novel Tissue-Nonspecific Alkaline Phosphatase Inhibitors with Diverse Modes of Action. Sergienko, E., Su, Y., Chan, X., Brown, B., Hurder, A., Narisawa, S., Millán, J.L. J Biomol Screen, 2009, 14(7):824-37.
  10. Design and synthesis of pyrazole derivatives as potent and selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP). Sidique, S., Ardecky, R., Su, Y., Narisawa, S., Brown, B., Millan, J.L., Sergienko, E., & Cosford, N.D. Bioorg Med Chem Lett, 2009, 19(1):222-225.
  11. Structure-activity relationship and improved hydrolytic stability of pyrazole derivatives that are allosteric inhibitors of West Nile Virus NS2B-NS3 proteinase. Sidique, S., Shiryaev, S., Ratnikov, B., Herath, A., Su, Y., Strongin, A., Cosford, N. Bioorg Med Chem Lett., 2009, 19(19):5773-7.
  12. Multidentate small-molecule inhibitors of vaccinia H1-related (VHR) phosphatase decrease proliferation of cervix cancer cells. Wu, S., Vossius, S., Rahmouni, S., Miletic, A.V., Vang, T., Vazquez-Rodriguez, J., Cerignoli, F., Arimura, Y., Williams, S., Hayes, T., Moutschen, M., Vasile, S., Pellecchia, M., Mustelin, T., Tautz, L. J. Med. Chem., 2009, 52(21):6716-23.


  1. Potent inhibitors of Huntingtin protein aggregation in a cell-based assay. Rinderspacher, A., Cremona, M., Liu, Y., Deng, S., Xie, Y., Gong, G, Aulner, N., Tobben, U., Myers, K., Chung, C., Andersen, M., Vidovic, D., Schurer, S., Branden, L., Yamamoto, A., & Landry, D. Bioorg. Med. Chem. Lett., 2009, 19(6):1715-1717.
  2. Convenient preparation of N-8-quinolinyl benzemesultams as novel NK-kB inhibitors. Xie, Y., Gong, G., Liu, L., Deng, S., Rinderspacher, A., Branden, L., & Landry, D. Tetrahedron Letters, 2009, 49(14):2320-2323.


  1. Interrogation of phosphor-specific interaction on a high-throughput label-free optical biosensor system-Epic System. Wu, M., Long, S., Frutos, A.G., Eichelberger, M., Li, M., Fang, Y. J Recept Signal Transduct Res., 2009, 29(3-4):202-210.


  1. A Basis for Reduced Chemical Library Inhibition of Firefly Luciferase Obtained from Directed Evolution. Auld, D., Zhang, Y., Southall, N., Rai, G., Landsman, M., Maclure, J., Langevin, D., Thomas, C., Austin, C., & Inglese, J. J Med Chem, 2009, 52(5):1450-1458.
  2. Mechanism of PTC124 activity in cell-based luciferase assays of nonsense codon suppression. Auld, D., Thorne, N., Maguire, W., & Inglese, J. Proc Natl Acad Sci USA, 2009, 106(9): 3585-3590.
  3. A dual-fluorescence high-throughput cell line system for probing multidrug resistance. Brimacombe, K., Hall, M., Auld, D.S.; Inglese, J., Austin, C., Gottesman, M., & Fung, K-L. Assay and Drug Development Technologies, 2009, 7(3):233-249.
  4. PubChem as a Source of Polypharmacology. Chen, B., Wild, D., Guha, R. Journal of Chemical Information and Modeling., 2009, 49(9): 2044-2055.
  5. Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening. Crowe, A., Huang, W., Ballatore, C., Johnson, R., Hogan, A., Huang, R., Wichterman, J., McCoy, J., Huryn, D., Auld, D., Smith, A., Inglese, J., Troganowski, J., Austin, C., Brunden, K., & Lee, V. Biochemistry, 48(32):7732-7745.
  6. Comprehensive Survey of Chemical Libraries for Drug Discovery and Chemical Biology: 2008. Dolle, R.E., Le Bourdonnec, B., Goodman, A.J., Morales, G.A., Thomas, C.J., Zhang, W. Journal of Combinatorial Chemistry, 2009, 11(5): 739-790.
  7. A Real-time Fluorescence Method for Enzymatic Characterization of Specialized Human DNA Polymerases. Dorjsuren, D., Wilson, D.M., Beard, W.A., McDonald, J.P., Austin, C.P., Woodgate, R., Wilson, S.H., Simeonov, A. Nucleic Acids Research, 2009, 37(19):e128.
  8. Proteasome Inactivation Promotes p38 Mitogen-activated Protein Kinase-dependent Phosphatidylinositol 3-kinase Activation and Increases Interleukin-8 Production in Retinal Pigment Epithelial Cells. Fernandes, A.F., Bian, Q., Jiang, J-K., Thomas, C.J., Taylor, A., Pereira, P., Shang, F. Molecular Biology of the Cell, 2009, 20(16): 3690-3699.
  9. HTS-Compatible Beta-Lactamase Transcriptional Reporter GeneAssay for Interrogating the Heat Shock Response Pathway. Hancock, M., Xia, M., Frey, E., Sakamuru, S., & Bi, K. Current Chemical Genomics, 2009, 3: 1-6.
  10. Weighted Feature Significance (WFS): A Simple, Interpretable Model of Compound Toxicity Based on the Statistical Enrichment of Structural Features. Huang, R., Southall, N., Xia, M., Cho, M.H., Jadhav, A., Nguyen, D.T., Inglese, J., Tice, R.R., Austin, C.P. ToxSci, 2009, 112(2):385-393.
  11. High Throughput Screening (HTS) Techniques- Applications in Chemical Biology. Inglese, J., Auld, D. Wiley Encyclopedia of Chemical Biology., 2009.
  12. Reply to Peltz et al: Post-translational stabilization of the firefly luciferase reporter by PTC124 (Ataluren). Inglese, J., Thorne, N., Auld, D.S. 2009 PNAS, 2009, 106(25): E65.
  13. Enabling the Large-Scale Analysis of Qunatitative High-Throughput Screening Data. Jadhav, A. Handbook of Drug Screening, Second Edition, 2009, ed. Seethala R & Zhang L. (Informa Healthcare): 442-465.
  14. A quantitative high-throughput screen for modulators of IL-6 signaling: a model for interrogating biological networks using chemical libraries. Johnson, R., Huang, R., Jadhav, A., Southall, N., Wichterman, J., MacArthur, R., Xia, M., Bi, K., Printen, J., Austin, C., & Inglese, J. Mol. Biosyst., 2009, 5(9): 1039-1050.
  15. Tetracycline-inducible gene expression in conditionally immortalized mouse podocytes. Kajiyama, H., Titus, S., Austin, C.P., Chiotos, K., Matsumoto, T., Sakairi, T., Kopp, J.B. American Journal of Nephrology., 2009, 29(3):153-63.
  16. Toxicity Testing in the 21st Century: Implications for Human Health Risk Assessment. Kavlock, R.J., Austin, C.P., Tice, R.R. Risk Analysis, 2009, 29(4): 485-487.
  17. A High-throughput Approach for Identification of Novel General Anesthetics. Lea, W.A., Xi, J., Jadhav, A., Lu, L., Austin, C.P., Simeonov, A., Eckenhoff, R.G. PLoS One, 2009, 4(9):e7150.
  18. Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a.Liu, F., Chen, X., Allali-Hassani, A., Quinn, A.M., Wasney, G.A., Dong, A., Barsyte, D., Kozieradzki, I., Senisterra, G., Chau, I., Siarheyeva, A., Kireev, D.B., Jadhav, A., Herold, J.M., Frye, S.V., Arrowsmith, C.H., Brown, P.J., Simeonov, A., Vedadi, M., Jin, J. Journal of Medicinal Chemistry, 2009, 52(24): 7950-7953.
  19. Monitoring compound integrity with cytochrome P450 assays and qHTS. MacArthur, R., Leister, W., Veith, H., Shinn, P., Southall, N., Austin, C., Inglese, J., & Auld, D. J Biomol Screen., 2009, 14(5): 538-546.
  20. Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay. Marchand, C., Lee, W.A., Jadhav, A., Dexheimer, T.S., Austin, C.P., Inglese, J., Pommier, Y., & Simeonov, A. Molecular Cancer Therapeutics, 2009, 8:240-248.
  21. A new resorufin-based alpha-glucosidase assay for high-throughput screening. Motabar, O., Shi, Z., Goldin, E., Liu, K., Southall, N., Sidranksy, E., Austin, C., Griffiths, G., & Zheng, W. Anal Biochem., 2009, 390(1): 79-84.
  22. Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk). Mott, B.T., Tanega, C., Shen, M., Maloney, D.J., Shinn, P., Leister, W., Marugan, J.J., Inglese, J., Austin, C.P., Misteli, T., Auld, D.S., Thomas, C.J. Bioorganic & Medicinal Chemistry Letters, 2009, 19(23): 6700-6705.
  23. Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice. Neumann, S., Huang, W., Titus, S., Krause, G., Kleinau, G., Alberobello, A., Zheng, W., Southall, N., Inglese, J., Austin, C., Celi, F., Gavrilova, O., Thomas, C., Raaka, B., & Gershengorn, M. Proc Natl Acad Sci USA, 2009, 106(30): 12471-12476.
  24. Automated high-content screening for compounds that disassemble the perinucleolar compartment. Norton, J.T., Titus, S.A., Dexter, D., Austin, C.P., Zheng, W., Huang, S. J Biomol Screen., 2009, 14(9):1045-53.
  25. Multi-gram scale synthesis of FR180204. Patnaik, S., Dietz, H.C., Zheng, W., Austin, C., Marugan, J.J. J Org Chem., 2009, 74(22):8870-3.
  26. Synthesis of Oxadiazole-2-oxide Analogues as Potential Antischistosomal Agents. Rai, G., Thomas, C. J., Leister, W., & Maloney, D. J. Tett Lett, 2009, 50(15): 1710-1713.
  27. Structure Mechanism Insights and the Role of Nitric Oxide Donation Guide the Development of Oxadiazole-2-Oxides as Therapeutic Agents against Schistosomiasis. Rai, G., Sayed, A.A., Lea, W.A., Luecke, H.F., Chakrapani, H., Prast-Nielsen, S., Jadhav, A., Leister, W., Shen, M., Inglese, J., Austin, C.P., Keefer, L., Arner, E.S., Simeonov, A., Maloney, D.J., Williams, D.L., Thomas, C.J. J Med Chem., 2009, 52(20):6474-6483.
  28. Synthesis and characterization of a new fluorogenic substrate for alpha-galactosidase. Shi, Z., Motabar, O., Goldin, E., Liu, K., Southall, N., Sidranksy, E., Austin, C., Griffiths, G., Zheng, W. Anal Bioanal Chem., 2009, 394(7): 1903-1909.
  29. Identification of pregnane X receptor ligands using time-resolved fluorescence resonance energy transfer and quantitative high-throughput screening. Shukla, S., Nguyen, D., Macarthur, R., Simeonov, A., Frazee, W., Hallis, T., Marks, B., Singh, U., Eliason, H., Printen, J., Austin, C., Inglese, J., & Auld, D. Assay Drug Dev Technol., 2009, 7(2): 143-169.
  30. Identification and characterization of inhibitors of human apurinic/apyrimidinic endonuclease APE1. Simeonov, A., Kulkarni, A., Dorjsuren, D., Jadhav, A., Shen, M., McNeill, D., Austin, C., & Wilson, D. PLoS One, 2009, 4(6):e5740.
  31. Exploration and Optimization of Substituted Triazolothiadiazines and Triazolopyridazines as PDE4 Inhibitors. Skoumbourdis, A. P., LeClair, C. A., Stefan, E., Turjanski, A. G., Maguire, W., Titus, S. A., Huang, R., Auld, D. S., Inglese, J., Austin, C. P., Michnick, S. W., Xia, M., & Thomas, C. J. Bioorg Med Chem Lett, 2009, epub.
  32. Comparison of a Bioluminescent Kinase Assays using Substrate Depletion and Product Formation. Tanega, C., Shen, M., Mott, B.T., Thomas, C.J., MacArthur, R., Inglese, J., Auld. D.S. Assay Drug Dev Technol., 2009, 7(6):606-14.
  33. Chemical safety: preparation and use of nitroacetonitrile. Thomas, C.J. Chemical & Engineering News, 2009, 87(32): 4-6.
  34. The Pilot Phase of the NIH Chemical Genomics Center: Paradigms, Profiles and Probes. Thomas, C.J., Auld, D.S., Huang, R., Huang, W., Jadhav, A., Johnson, R.L., Leister, W., Maloney, D.J., Marugan, J.J., Michael, S., Simeonov, A., Southall, N., Xia, M., Zheng, W., Inglese, J., Austin, C.P. Current Topics in Medicinal Chemistry, 2009, 9(13): 1181-1193.
  35. A new homogenous high-throughput screening assay for profiling compound activity on the human ether-a-go-go related gene channel. Titus, S., Beacham, D., Shashane, S., Southall, N., Xia, M., Huang, R., Hooten, E., Zhao, Y., Austin, C., & Zheng, W. Anal Biochem., 2009, 394(1): 30-38.
  36. Comprehensive characterization of cytochrome P450 isozyme selectivity across chemical libraries. Veith, H., Southall, N., Huang, R., James, T., Fayne, D., Artemenko, N., Shen, M., Inglese, J., Austin, C.P., Lloyd, D.G., Auld, D.S. Nat Biotechnol., 2009, 27(11):1050-5.
  37. Cardiac glycosides inhibit p53 synthesis by a mechanism relieved by Src or MAPK inhibition. Wang, Z., Zheng, M., Li, Z., Li, R., Jia, L., Xiong, X., Southall, N., Wang, S., Xia, M., Austin, C.P., Zheng, W., Xie, Z., Sun, Y. Cancer Res., 2009, 69(16):6556-64.
  38. Identification of Compounds that Potentiate CREB Signaling as Possible Enhancers of Long-Term Memory. Xia, M., Huang, R., Vicky Gou, V., Southall, N., Cho, M., Inglese, J., Austin, C.P., Nirenberg, M. Proc Natl Acad Sci USA, 2009,106(7): 2412-2417.
  39. Identification of small molecule compounds that inhibit the HIF-1 signaling pathway. Xia, M., Bi, K., Huang, R., Cho, M., Sakamuru, S., Miller, S.C., Printen, J., Austin, C.P., Inglese, J. Molecular Cancer, 2009, 8:117.
  40. A Cell-based Beta-Lactamase Reporter Gene Assay for the CREB Signaling Pathway. Xia, M., Guo, V., Huang, R., Inglese, J., Nirenberg, M., Austin, C.P. Current Chemical Genomics, 2009, 3(1): 7-12.
  41. Identification of Chemical Compounds that Induce HIF-1{alpha} Activity. Xia, M., Huang, R., Sun, Y., Semenza, G.L., Aldred, S.F., Witt, K.L., Inglese, J., Tice, R.R., Austin, C.P. Toxicol Sci., 2009, 112(1): 153-163.
  42. An AlphaScreen Based High-throughput Screen to Identify Inhibitors of Hsp90 and Cochaperone Interaction. Yi, F., Zhu, P., Southall, N., Inglese, J., Austin, C., Zheng, W., & Regan, L. Journal of Biomolecular Screening, 2009, 14(3):273-281.
  43. Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. Yuan, J., Johnson, R.L., Huang, R., Wichterman, J., Jiang, H., Hayton, K., Fidock, D.A., Wellems, T.E., Inglese, J., Austin, C.P., Su, X.-Z. Nat. Chem. Bio, 2009, 5(10):765-771.
  44. Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death. Zhu, P., Hobson, J., Southall, N., Qiu, C., Thomas, C., Lu, J., Inglese, J., Zheng, W., Leppla, S., Bugge, T., Austin, C., & Liu, S. Bioorg Med Chem., 2009, 17(14): 5139-5145.
  45. Practical Approach to Quantitative High Throughput Screening. Zheng, W., Liu, K., Inglese, J. In Seethala R and Zhang L (Eds.), Handbook of Drug Screening, second edition, Drugs and the Pharmaceutical Sciences (pp.432-441) , Informa Healthcare USA, New York (2009).