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(46) Direct Publications in 2007


bold indicates screening center PI

2007

1. Albanito, L., Madeo, A., Lappano, R., Vivacqua, A., Rago, V., Carpino, A., Oprea, T., Prossnitz, E., Musti, A., Ando, S., & Maggiolini, M. (2007). G Protein-Coupled Receptor 30 (GPR30) Mediates Gene Expression Changes and Growth Response to 17b -Estradiol and Selective GPR30 Ligand G-1 in Ovarian Cancer Cells. Cancer Res, 67:1859-1866.

2. Ariazi, E.A., Leitao, A., Oprea, T.I., Chen, B., Louis, T., Betucci, A.M., Sharma, C.G.N., Gill, S.D., Kim, H.R., Shupp, H.A., Pyle, J.R., Madrack, A., Donato A.L., Cheng, D., Paige, J.R., & Jordan, V.C. (2007). Exemestane’s 17-hydroxylated metabolite exerts biological effects as an androgen. Molecular Cancer Therapeutics, 11, 2817-2827.

3. Arnold, D. M., Foster, C., Huryn, D. M., Lazo, J. S., Johnston, P.A., &n Wipf, P. (2007). Synthesis and Biological Activity of a Focused Library of Mitogen-activated Protein Kinase Phosphatase Inhibitors. Chemical Biology & Drug Design, 69, 23-30.

4. Auld, D.S., Inglese, J., Jadhav, A., Austin, C.P., Sittampalam, G.S., Montrose-Rafizadeh, C., Mcgee, J.E., & Iversen, P.W. (2007). HTS technologies to facilitate chemical genomics. European Pharma. Review, 2: 53-63.

5. Buranda, T., Waller, A., Wu, Y., Simons, P.C., Biggs, S., Prossnitz, E.R., & Sklar, L.A. (2007). Some mechanistic insights into GPCR activation from detergent-solubilized ternary complexes on beads. Advanced Protein Chemistry, 74, 95-135.

6. Davis, R.E., Zhang, Y., Southall, N., Staudt, L.M., Austin, C.P., Inglese, J., & Auld, D.S. (2007). A Cell-Based Assay for IKBa Stabilization Using Two-Color Dual Luciferase-Based Sensor. Assay and Drug Development Technologies, 5: 85-103.

7. Diamond, S.L. (2007). Methods for mapping protease specificity. Current Opinion in Chemical Biology, 11, 46-51.

8. Don, A.S., Martinez-Lamenca, C., Webb, W.R., Proia, R.L., Roberts, E., & Rosen, H. (2007). Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY710 analogues. Biological Chemistry, 282, 15833-15842.

9. Du, Y., Moulick, K., Rodina, A., Aguirre, J., Felts, S., Dingledine, R., Fu, H. & Chiosis, G. (2007). High-throughput screening fluorescence polarization assay for tumor-specific Hsp90. Journal of Biomolecular Screening, 12, 915-924.

10. Edwards, B., Ivnitski-Steele, I., Young, S., Salas, V.,.Sklar, L. (2007). High Throughput Cytotoxicity Screening by Propidium Iodide Staining. Current Protocols in Cytometry, In press

11. Edwards, B., Young, S., Saunders, M., Bologa. C,, Oprea. T,, Ye, R., Prossnitz, E., Graves, S., & Sklar, L. (2007). High Throughput Flow Cytometry for Drug Discovery. Expert Opin Drug Discov 2, 685-696.

12. Edwards, B., Young, S., Ivnitski-Steele, I., Ye, R., Prossnitz, E., & Sklar, L. High content screening: flow cytometry analysis. In:P. A. Clemons, N. J. Tolliday, and B. K. Wagner (eds.), Cell Based Assays in High-Throughput Screening. Totowa, NJ: Humana Press, Inc., in press, 2007.

13. Feng, B.Y, Simeonov, A., Jadhav, A., Babaoglu, K., Inglese, J., Shoichet, B.K., & Austin, C.P. (2007). A High-throughput Screen for Aggregation-based inhibition in a Large Compound Library. J. Med. Chem, 50: 2385-2390.

14. Ganesh, T. (2007). Improved biochemical strategies for targeted delivery of taxoids, Bioorg Med Chem, 15, 3597-3623.

15. Gonzalez-Cabrera, P.J., Hla, T., & Rosen., H. (2007). Mapping Pathways Downstream of Sphingosine 1-Phosphate Subtype 1 by Differential Chemical Perturbation and Proteomics. Journal of Biological Chemistry, 282, 7254-7264.

16. Honson, N. S., Johnson, R. L., Huang, W., Inglese, J., Austin, C.P., & Kuret, J. (2007). Differentiating Alzheimer disease-associated aggregates with small molecules. Neurobiology of Disease, 28(3), 251-260.

17. Hristozov, D. P., Oprea, T.I., & Gasteiger, J. (2007). Ligand-based virtual screening by novelty detection with self-organizing maps. J. Chem. Inf. Model., 47, 2044-2062.

18. Huang, W., Zheng, W., Urban, D.J., Inglese, J., Sidransky, E., Austin, C.P., & Thomas, C.J. (2007). N4-Phenyl modifications of N2-(2-hydroxyl)ethyl-6(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease. Bioorganic and Medicinal Chemistry Letters, 17, 5783-5789.

19. Huryn, D. M., & Cosford, N. D. P. (2007). Chapter 26 the molecular libraries screening center network (MLSCN): Identifying chemical probes of biological systems. Annual Reports in Medicinal Chemistry 42, 401-416

20. Inglese, J., Johnson, R.L., Simeonov, A., Xia, M., Austin, C.P., & Auld, D.S. (2007). High-throughput screening assays for the identification of chemical probes. Nature Chemical Biology, 3: 466-479.

21. Inglese, J., Shamu, C.E., & Guy, R.K. (2007). Reporting data from high-throughput screening of small-molecule libraries. Nature Chemical Biology, 3: 438-441.

22. Johnston, P.A., Foster, C.A., Shun, T.Y., Skoko, J.J., Shinde, S., Wipf, P., & Lazo, J.S. (2007). Development and implementation of a 384-well homogeneous fluorescence intensity high-throughput screening assay to identify mitogen-activated protein kinase phosphatase-1 dual-specificity protein phosphatase inhibitors. Assay and Drug Development Technologies, 5: 319-332.

23. Johnston, P.A., Phillips, J., Shun, T.Y., Shinde, S., Lazo, J.S., Huryn, D. M., Myers, M. C., Ratnikov, B.I., Smith, J.W., Su, Y., Dahl, R., Cosford, N., Shiryaev, S.A., & Strongin, A.Y. (2007). HTS identifies novel and specific uncompetitive inhibitors of the two-component NS2B-NS3 proteinase of West Nile virus. Assay and Drug Development Technologies, 5, 737-750.

24. Lazo, J. S., Brady, L., & Dingledine, R. (2007). Building a pharmacological lexicon: small molecule discovery in academia. Molecular Pharmacoogy, 72 , 1-17.

25. Lazo, J.S., Skoko, J.J., Werner, S., Mitasev, B., Bakan, A., Koizumi, F., Yellow-Duke, A., Bahar, I., & Brummond, K.M. (2007).Structurally unique inhibitors of human mitogen-activated protein kinase phosphatase-1 identified in a pyrrole carboamide library. Journal of Pharmacology and Experimental Therapeutics, 322, 940-947.

26. Lee, H-K., Brown, S.J., Rosen, H., & Tobias, P.S. (2007). Application of B-lactamase enzyme complementation to the high-throughput screening of toll-like receptor signaling inhibitors. Molecular Pharmacology, 72, 868-875.

27. Myers, M. C., Napper, A.D., Motlekar, N., Shah, P.P., Chiu, C.H., Beavers, M.P., Diamond, S.L., Huryn, D.M., & Smith, III., A.B. (2007). Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: The confounding effects of DTT and cysteine in biological assays. Bioorg Med Chem Lett, 17, 4761-4766.

28. Naivar, M.A., Parson, J.D., Wilder, M.E., Habbersett, R.C., Edwards, B.S., Sklar, L., Nolan, J.P., Graves, S.W., Martin, J.C., Jett, J.H., & Freyer, J.P. (2007). Open, reconfigurable cytometic acquisition system: ORCAS. Cytometry Part A, 71, 915-924.

29. Oprea, T. I., Allu, T.K, Fara, D.C., Rad, R.F., Ostopovici, L., & Bologa, C.G. (2007).Lead-like, drug-like or “Pub-like”: how different are they? J Comput Aided Mol Des, 21.

30. Oprea, T. I., Tropsha, A., Faulon, J.L., Rintou, M.D. (2007). Systems chemical biology. Nat Chem Biol, 3, 447-450.

31. Prossnitz, E. R., Arterburn, J.B., & Sklar, L.A. (2007). GPR30: A G protein-coupled receptor for estrogen. Mol Cell Endocrinol, 265-266.

32. Revankar, C.M., Mitchell, H.D., Field, A.S., Burai, R., Corona, C., Ramesh, C., Sklar, L.A., Arterburn, J.B., & Prossnitz, E.R. (2007). Synthetic estrogen derivatives demonstrate the functionality of intracellular GPR30. ACS Chemical Biology, 2: 536-544.

33. Rosen, H., Sanna, M.G., Calahan, S.M., & Gonzalez-Cabrera, P.J. (2007). Tipping the gatekeeper: S1P regulation of endothelial barrier function. Trends in Immunology, 28, 102-107.

34. Sharlow, E.R., Leimgruber, S., Shung, T.Y., & Lazo, J.S. (2007). Development and implementation of a miniaturized high-throughput time-resolved fluorescence energy transfer assay to identify small molecule inhibitors of polo-like kinase 1. Assay and Drug Development Technologies, 5, 723-735.

35. Simeonov, A., Yasgar, A., Klumpp, C., Zheng, W., Shafqat, N., Oppermann, U., Austin, C.P., & Inglese, J. (2007). Evaluation of micro-parallel liquid chromatography as a method for HTS-coupled actives verification. Assay and Drug Development Technologies, 5, 815-824.

36. Simons, P.C., Young, S.M., Gibaja, V., Lee, W-C., Josiah, S., Edwards, B.S., & Sklar, L.A. (2007). Duplexed, bead-based competitive assay for inhibitors of protein kinases. Cytometry Part A, 71, 451-459.

37. Sklar. L.A., Carter, M.B., Edwards, B.S. (2007). Flow cytometry for drug discovery, receptor pharmacology and high-throughput screening. Current Opinion in Pharmacology, 7, 527-534.

38. Skoumbourdis, A.P., Moore, S., Landsman, M., & Thomas, C.J. (2007). Synthesis of substituted 2-phenylhistamines via a microwave promoted Suzuki coupling. Tetrahedron Letters, 48, 9140-9143.

39. Sun, A., Chandrakumar, N., Yoon, J-J., Plemper, R.K., & Snyder, J.P. (2007). Non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex activity: Synthesis and in vitro evaluation. Bioorganic and Medicinal Chemistry Letters, 17, 5199-5203.

40. Thepchatri, P., Eliseo, T., Cicero, D.O., Myles, D., & Snyder, J.P. (2007). Relationship among ligand conformations in solution, in the solid state, and at the Hsp90 binding site: geldanamycin and radicicol. J Am Chem Soc, 129, 3127-3134.

41. Tran, T.C., Sneed, B., Haider, J., Blavo, D., White, A., Aiyejorun, T., Baranowski, T.C., Rubinstein, A.L., Doan, T.N., Dingledine, R., & Sandberg, E.M. (2007). Automated, quantitative screening assay for antiangiogenic compounds using transgenic zebrafish. Cancer Research, 67, 11386-11392.

42. Vogt, A., & Lazo, J.S. (2007). Implementation of high-content assay for inhibitors of mitogen-activated protein kinase phosphatases, Methods, 42, 268-277.

43. Wu, Y., Buranda, T., Simons, P.C., Lopez, G.P., McIntire, W.E., Garrison, J.C., Prossnitz, E.R., & Sklar, L.A. (2007). Rapid-mix flow cytometry measurements of subsecond regulation of G protein-coupled receptor ternary complex dynamics by guanine nucleotides. Analytical Biochemistry, 371: 10-20.

44. Wu, Y., Campos, S.K., Lopez, G.P., Ozbun, M.A., Sklar, L.A., & Buranda, T. (2007). The development of quantum dot calibration beads and quantitative multicolor bioassays in flow cytometry and microscopy. Anal Biochem, 364, 180-192.

45. Wu, Y., Lopez, G.P., Sklar, L.A., & Buranda, T. (2007). Spectroscopic characterization of streptavidin functionalized quantum dots. Anal Biochem, 364, 194-203.

46. Zheng, W., Padla, K., Urban, D.J., Jadhav, A., Goker-Alpan, O., Simeonov, A., Goldin, E., Auld, D., LeMarca, M.E., Inglese, J., Austin, C.P., & Sidransky, E. (2007). Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease. Proceedings of the National Academy of Sciences of the United States of America, 104: 13192-13197.

Edited by CR: 06/16/08