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(49) Publications in 2009


Burnham

  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. 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.
  3. 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.

Columbia

  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.

NCGC

  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. 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.
  5. HTS β-Lactamase transcriptional reporter gene assay for interrogating heat shock response signaling pathway. Hancock, M., Xia, M., Frey, E., Sakamuru, S., & Bi, K. Current Chemical Genomics, 2009, 3: 1-6.
  6. High Throughput Screening (HTS) Techniques- Applications in Chemical Biology. Inglese, J., Auld, D. Wiley Encyclopedia of Chemical Biology., 2009.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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: 7-12.
  20. 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.
  21. 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.

New Mexico

  1. In vivo effects of a GPR30 antagonist. Dennis, M., Burai, R., Ramesh, C., Petrie, W., Alcon, S., Nayak, T., Bologa, C., Leitao, A., Brailoiu, E., Deliu, E., Dun, N., Sklar, S., Hathaway, H., Arterburn, J., Oprea, T., & Prossnitz, E. Nature Chemical Biology, 2009, 5: 421-427.
  2. A Novel Fluorescent Cross-Reactive Formylpeptide Receptor/Formylpeptide Receptor-Like 1 Hexapeptide Ligand. Strouse, J.J., Young, S.M., Mitchell, H.D., Ye, R.D., Prossnitz, E.R., Sklar, L.A., & Edwards, B.S. Cytometry A, 2009, 75(3): 264-270.
  3. Duplex high throughput flow cytometry screen identifies two Novel Formylpeptide Receptor Family Ligands.Young, S.M., Bologa, C.M., Fara, D., Bryant, B.K., Strouse, J.J., Arterburn, J.B., Ye, R.D., Oprea, T.I., Prossnitz, E.R., Sklar, L.A., & Edwards, B.S. Cytometry A, 2009, 75(3): 253-263.

Penn

  1. Toward the development of a potent and selective organoruthenium mammalian sterile 20 kinase inhibitor. Anand, R., Maksimoska, J., Pagano, N., Wong, E., Gimotty, P., Diamond, S., Meggers, E., & Marmorstein, R. J. Med. Chem., 2009, 52(6):1602-1611.
  2. Advancing microarray assembly with acoustic dispensing technology. Wong, E., & Diamond, S. Anal. CHem., 2009, 81(1):509-514.

Scripps

  1. MAOS protcols for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines. Aldrich, L., Lebois, E., Lewis, M., Nalywajko, N., Niswender, C., Weaver, C.D., Conn, P.J., & Lindsley, C. Tetrahedron Letters, 2009, 50:212-215.
  2. Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes. Bachovchin, D., Brown, S., Rosen, H., Cravatt, B. Nat Biotechnol, 2009, 27(4):387-94.
  3. S1P1 signaling just keeps going and going and going… Calahan, S., & Rosen, H. Nat. Chem. Biol. 2009, 5(6): 377-378.
  4. A lipid binding domain in sphingosine kinase 2. Don, A., Rosen, H. Biochem Biophys Res Commun., 2009, 380(1): 87-92.
  5. The function of follicular helper T cells is regulated by the strength of T cell antigen receptor binding. Fazilleau, N., McHeyzer-Williams, L., Rosen, H., McHeyzer-Williams, M. Nat Immunol 2009, 10(4):375-84.
  6. Chemical modulators of sphingosine-1-phosphate receptors as barrier-oriented therapeutic molecules. Marsolais, D., Rosen, H. Nat Rev Drug Discov., 2009, 8(4):297-307.
  7. A critical role for the sphingosine analog AAL-R in dampening the cytokine response during influenza virus infection. Marsolais, D., Hahm, B., Walsh, K., Edelmann, K., McGavern, D., Hatta, Y., Kawaoka, Y., Rosen, H., Oldstone, M. Proc Natl Acad Sci USA, 2009, 106(5): 1560-5.
  8. Endogenous EPCR/aPC-PAR1 signaling prevents inflammation-induced vascular leakage and lethality. Niessen, F., Furlan-Freguia, C., Fernandez, J.A., Mosnier, L.O., Castellino, F.J., Weiler, H., Rosen, H., Griffin, J.H., & Ruf, W. Blood, 2009, 113(12):2859-2866.
  9. HD Desktop: An Integrated Platform for the Analysis and Visualization of H/D Exchange Data. Pascal, B.D., Chalmers, M.J., Busby, S.A., Griffin, P.R. J of the Am Soc for Mass Spec, 2009, 20(4):601-610.
  10. Potent inhibitors of Huntingtin protein aggregation in a cell-based assay. Rinderspacher, A., Cremona, M.L., Lui, Y., Deng, S.-X., Xie, Y., Gong, G., Aulner, N., Tobben, U., Myers, K., Chung, C., Anderson, M., Vidovic, D., Schurer, S., Branden, L., Yamamoto, A., Landry, D. Bioorg Med Chem Lett., 2009, 19(6):1715-1717.
  11. Sphingosine 1-phosphate receptor signaling. Rosen, H., Gonzalez-Cabrera, P.J., Sanna, M.G., & Brown, S. Annual Rev Biochem, 2009, 78: 743-768.
  12. S1P1-selective agonist SEW2871 exacerbates reperfusion arrhythmias. Tsukada, Y., Sanna, M., Rosen, H., Gottlieb, R. J Cardiovasc Pharmacol, 2007, 50(6):660-9.

SRI

  1. Southern Research Institute: A Molecular Libraries Screening Center Program. Screening Trends in Drug Discovery, 2009, 10.

Vanderbilt

  1. A Novel Selective Muscarinic Acetylcholine Receptor Subtype 1 Antagonist Reduces Seizures without Impairing Hippocampus-Dependent Learning. Sheffler, D., Williams, R., Bridges, T., Xiang, Z., Kane, A., Byun, N., Jadhav, S., Mock, M., Zheng, F., Lewis, M., Jones, C., Niswender, C., Weaver, C., Lindsley, C., & Conn, J. Molec. Pharm., 2009, 76(2): 356-368.
  2. Discovery of the First Highly M5-Preferring Muscarinic Acetylcholine Receptor Ligand, an M5 Positive Allosteric Modulator Derived from a Series of 5-Trifluoromethoxy N-Benzyl Isatins. Bridges, T., Marlo, J., Niswender, C., Jones. C., Jadhav, S., Gentry, P., Plumley, H., Weaver, D., Conn, P. J., & Lindsley, C. J. Med. Chem, 2009, 52(11):3445-8.

Other

  1. Perfecting Probes. Editorial. Nature Chemical Biology, 2009, 5(7): 435.
  2. A crowdsourcing evaluation of the NIH chemical probes Oprea, T., Bologa, C., Boyer, S., Curpan, R., Glen, R., Hopkins, A., Lipinski, C., Marshall, G., Martin, Y., Ostopovici-Halip, L., Rishton, G., Ursu, O., Vaz, R., Waller, C., Waldmann, H., & Sklar, L. Nature Chemical Biology, 2009, 5(7): 441-447.
  3. Chemoinformatic analysis of combinatorial libraries, drugs, natural products, and molecular libraries small molecule repository. Singh, N., Guha, R., Giulianotti, M., Pinilla, C., Houghten, R., & Medina-Franco, J. J. Chem. Inf. Model., 2009, 49(4): 1010-1024.