(64) Direct Publications in 2008
Direct Manuscripts
(From MLSCN Funded Grants)
2008 (64 total)
Characterization of chemical libraries for luciferase inhibitory activity.
Auld, D.S., Southall, N., Jadhav, A., Johnson R.L., Diller D., Simeonov A., Austin, C.P, & Inglese, J.
Journal of Medicinal Chemistry, 2008, 10.1021/jm701302v
Specific Mechanism for Nonspecific Activation in Reporter-Gene Assays.
Auld, D.S., Thorne, N., Nguyen, D.T. & Inglese, J.A.
Chemical Biology, 2008, 3(8), 463-470.
Bagaoglu, K., Simeonov, A., Irwin, J., Nelson, M., Feng, B.Y., Thomas, C., Cancian, L., Costi, MP., Maltby, D., Jadhav, A., Inglese, A., Austin, C.P., & Shoichet. B.K.
Journal of Medicinal Chemistry, 2008, in press.
Bakan, A, Lazo, J., Wipf, P., Brummond K., & Bahar, I.
Current Med. Chem., 2008, in press.
Molecular docking of cathepsin L inhibitors in the binding site of papain.
Beavers, M., Myers, M., Shaw, P., Diamond, S., & Smith, A.
J. Chem. Information & Modeling, 2008, 48(7), 1464-1472.
COPI complex is a regulator of lipid homeostasis.
Beller, M., Sztalryd, C., Southall, N., Bell, M., Jackle, H., Auld, D.S. & Oliver, B. PLoS Biol, 2008, 6(11): e292. doi:10.1371/journal.pbio.0060292
A comparative analysis of standard microtiter plate reading versus imaging in cellular assays.
Bushway, P., Mercola, M. & Price, J.
Assay and Drug Development Technologies, 2008, 6(4), 557-567.
deAlmeida, R.A., Burgess, D., Shema, R., Motlekar, N., Napper, A.D., Diamond, S.L. & Pavitt., G.D.
Yeast, 2008, 25, 71-76.
Dennis, M., Bowles, H., MacKenzie, D., Burchiel, S., Edwards, B., Sklar, L., Prossnitz, E., & Thompson, T.
Cytometry, 2008, 7, 390-9
Dai, S., Chalmers, M., Bruning, J., Bramlett, K., Osborne, H., Montrose-Rafizadeh, C., Barr, R., Wang, Y., Wang, M., Burris, T., Dodge, J., & Griffin, P.
Proc. Natl. Acad. Sci. USA, 2008, 105, 7171-7176.
Comprehensive Survey of Chemical Libraries for Drug Discovery and Chemical Biology: 2007.
Dolle, R.E., Bourdonnec, B., Goodman, A., Morales, G., Thomas, C. & Zhang W.
Journal of Combinatorial Chemistry, 2008, 10(6), 753-802.
A fluorescent plate reader assay for ceramide kinase.
Don, A.S., & Rosen, H.
Analytical Biochemistry, 2008, 375(2), 265-271.
Gonzalez-Cabrera, P.J., Jo, E., Sanna, M.G., Brown, S., Leaf, N., Marsolais, D., Schaeffer, M.T., Chapman, J., Cameron, M., Guerrero, M., Roberts, E. & Rosen, H.
Mol Pharmacol, 2008, 74(5), 1308-1318.
Guha, R., & Schurer, S.
Comp. Aided. Mol. Des., 2008, 22, 367-384.
Hsieh, J-H., Wang, X.S., Teotico, D., Golbraikh, A. & Tropsha, A.
J. Comput Aided Mol Des, 2008, DOI 10.1007/s10822-008-9199-2
Huang, R., Southall, N., Cho, M.H., Xia, M., Inglese, J., & Austin, C.P.
Chem. Res. Toxicol., 2008, 21(3), 659–667.
Ivnitski-Steele, I., Lawson, R.S., Lovato, D.M., Khawaja, H.M., Winter, S.S., Oprea, T.I., Sklar L.A., & Edwards, B.S.
Assay and Drug Development Technologies, 2008, 6(2), 263-276.
Jiang, J.K., Ghoreschi, K., Deflorian, F., Chen, Z., Perreira, M., Pesu, M., Smith, J., Nguyen, D.T., Liu, E.H., Leister, W., Costanzi, S., O’Shea, J.J., Thomas, C.J.
Journal of Medicinal Chemistry, 2008, In press.
A quantitative high-throughput screen identifies potential epigenetic modulators of gene expression.
Johnson, R., Huang, W., Jadhav, A., Austin, C.P., Inglese, J., & Martinez, E.D. Analytical Biochemistry, 2008, 375, 237-248.
Tetracycline-Inducible Gene Expression in Conditionally Immortalized Mouse Podocytes.
Kajiyama, H., Titus, S., Austin, C., Chiotos, K., Matsumoto, T., Sakairi, T. & Kopp, J.
American Journal of Nephrology, 2008, 29, 153-163.
Kim, I., Shu, C., Xu, W., Shiau, C.W., Grant, D., Vasile, S., Cosford, N., Reed, J.
J. Biol Chem., 2008, In press.
Lauer-Fields, J.L., Minond, D., Chase, P., Baillargeon, P., Saldanha, S., Stawikowska, R., Hodder, P., & Fields, G.
Bioorg. & Med. Chem. Letters, 2008, In press.
Lauer-Fields, J.L., Spicer, T.P., Chase, P.S., Cudic, M., Burstein, G.D., Nagase, H., Hodder, P. & Fields, GB.
Analytical Biochemistry, 2008, 373, 43-51.
Is Cdc25 a druggable target?
Lazo, J., & Wipf P.
Anti-cancer Agents Med Chem., 2008, In press.
Lea, W.A., Jadhav, A., Rai, G., Sayed, A., Cass, C., Inglese, J., Williams, D., Austin, C,P. & Simeonov, A.
Assay and Drug Development Technologies, 2008, 6, 551-555.
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.
Lewis, M., Sheffler, D., Williams, R., Bridges, T., Kennedy, J.P., Brogan, J.T., Mulder, M.J., Williams, L., Nalywajko, N.T., Niswender, C., Weaver, C., Conn, P.J., Lindsley, C.W.
Bioorg. & Med. Chem. Lett, 2008, 885-890.
Potent, selective and cell penetrant inhibitors of SF-1 by functional uHTS.
Madoux, F., Li, X., Chase, P., Zastrow, G., Cameron, M.D., Conkright, J.J., Griffin, P.R., Thacher, S. & Hodder, P.
Molecular Pharmacology, 2008, 73(6), 1776-1784.
Marchand, C., Lea, W., Jadhav, A., Dexheimer, T., Austin, C.P., Inglese, J., Pommier, Y. & Simeonov, A.
Molecular Cancer Therapeutics, 2008, In press.
Marinello, J., Marchand, C., Mott, B.T., Bain, A., Thomas, C.J., Pommier, Y. Biochemistry, 2008, 27(36), 9345-9354.
Marsolais, D., Hahm,B., Edelmann, K.H., Walsh, K.B., Guerrero, M., Hatta, Y., Kawaoka, Y., Roberts, E., Oldstone, M.B. & Rosen, H.
Mol Pharmacol., 2008, 74(3), 896-903.
A robotics platform for quantitative high-throughput screening.
Michael, S., Auld, D., Klumpp, C., Jadhav, A., Zheng, W., Thorne, N., Austin, C.P., Inglese, J. & Simeonov A.
Assay and Drug Development Technologies, 2008, 6(5), 637-657.
Evaluation of an orthogonal pooling strategy for rapid high throughput screening of proteases.
Moltekar, N., Diamond, S.L., & Napper, A.
Assay & Drug Dev. Tech., 2008, 6(3), 395-405.
Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor.
Myers, M.C., Shah, P.P., Diamond, S.L., Huryn, D.M., & Smith, A.B.
Bioorganic and Medicinal Chemistry Letters, 2008, 18, 210-214.
Nakai, R., Salisbury, C.M., Rosen, H., & Cravatt, B.F.
Bioorganic & Medicinal Chemistry, 2008, doi: 10.1016/j.bmc.2008.03.018
Neumann, S., Kleinau, G., Costanzi, S., Moore, S., Jiang, J.K., Raaka , B.M., Thomas, C.J., Krause, G., & Gershengorn, M.C.
Endocrinology, 2008, 149(12), 5945-5950.
Dendritic cell PAR1-S1P3 signalling couples coagulation and inflammation.
Niessen, F., Schaffner, F., Furlan-Freguia, C., Pawlinski, R., Bhattacharjee, G., Chun, J., Derian, C. K., Andrade-Gordon, P., Rosen, H., Ruf, W.
Nature, 2008, 452, 654-658.
Niswender, C.M., Johnson, K.A., Luo, Q., Ayala, J., Kim, C., Conn, P.J., & Weaver, D.
Molec. Pharmacology, 2008, In press.
Estrogen Signaling through the Transmembrane G protein-coupled Receptor GPR30.
Prossnitz, E., Arterburn, J., Smith, H., Oprea, T., Sklar, L. & Hathaway H.
Ann. Rev. Physiol., 2008, 70, 165-190.
GPR30: a novel therapeutic target in estrogen-related disease
Prossnitz, E., Arterburn, J., Oprea, T., & Sklar, L.
TIPS, 2008, 29, 116-123.
Modulating tone: the overture of S1P receptor immunotherapeutics.
Rosen, H., Gonzalez-Cabrera, P., Marsolais, D., Cahalan, S., Don, A. S., Sanna, M. G. Immunol. Rev., 2008, 223, 221-235.
Roth, J., Madoux, F., Hodder, P. & Roush, W.
Bioorg. Med Chem Lett., 2008, 18(8), 2628-2632.
Advances in Multiple Analyte Profiling.
Salas, V., Edwards, B., & Sklar, L.
Adv Clin Chem, 2008, 45, 47-74
Identification of oxadiazoles as new drug leads for control of schistosomiasis.
Sayed, A.A., Simeonov, A., Thomas, C.J., Inglese, J., Austin, C.P., & Williams, D.L. Nature Medicine, 2008, 14, 407-412.
Schröter, T., Minond, D., Weiser, A., Dao, C., Habel, J., Spicer, T., Chase, P., Baillargeon, P., Scampavia, L., Schürer, S., Chung, C., Mader, C., Southern, M., Tsinoremas, N., LoGrasso, P., & Hodder, P.
J. Biomolecular Screening, 2008, In press.
Schürer, S., Brown, S., Gonzales Cabrera, P., Schaeffer, M-T., Chapman, J., Jo, E., Chase, P., Spicer, T., Hodder, P. & Rosen, H.
ACS Chem Biol,, 2008, 3(8), 486-498.
Shah, P., Myers, M., Beavers, M., Pruvis, J., Huryn, D., Smith, A., & Diamond, S. Molec. Pharmacol., 2008, In press.
Potent and selective disruption of protein kinase d functionality by a benzoxoloazepinolone.
Sharlow, E.R., Giridhar, K., Lavelle, C., Chen, J., Leimgruber, S., Barrett, R., Bravo-Altamirano, K., Wipf, P., Lazo, J., & Wang, Q.
J. Biol Chem., 283(48), 33516-33526.
Sharlow, E., Leimgruber, S., Yellow-Duke, A., Barrett, R., Wang, Q., & Lazo, J.S. Nature Protocols, 2008, In Press.
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.
Shirey, J.K., Xiang, Z., Orten, D., Brady, A.E., Johnson, K.A., Williams, R., Ayala, J.E., Rodriquez, A.L., Wess, J., Weaver, D., Niswender, C., & Conn, J.P.
Nature Chemical Biology, 2008, 4, 42-50.
Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade.
Simeonov, A., Jadhav, A., Sayed, A.A., Wang, Y., Nelson, M.E., Thomas, C.J., Inglese, J., Williams, D.L., & Austin, C.P.
PLoS Negl Trop Dis, 2008, 2, e127.
Simeonov, A., Yasgar, A., Jadhav, A., Lokesh, G.L., Klumpp, C., Michael, S., Austin, C.P., Natarajan, A., & Inglese, J.
Analytical Biochemistry, 2008, 375, 60-70.
Fluorescence Spectroscopic Profiling of Compound Libraries.
Simeonov, A., Jadhav, A., Thomas, C.J., Wang, Y., Huang, R., Southall, N., Shinn, P., Smith, J., Austin, C.P., & Inglese, J.
Journal of Medicinal Chemisty, 2008, in press.
Identification of a potent new chemotype for the selective inhibition of PDE4.
Skoumbourdis, A.P., Huang, R., Southall, N., Leister, W., Guo, V., Cho, M.H., Inglese, J., Nirenberg, M., Austin, C.P., Xia, M., & Thomas, C.J.
Bioorganic and Medicinal Chemistry Letters, 2008, 18 (4),1297-1303.
Titus, S., Neumann, S., Zheng, W., Southall, N., Michael, S., Klumpp, C., Yasgar, A., Shinn, P., Thomas, C.J., Inglese, J., Gershengorn, M.C., & Austin, C.P.
Journal of Biomolecular Screening, 2008, 13(2), 120-127.
A Cell-Based PDE4 Assay in 1536-Well Plate Format for High-Throughput Screening.
Titus, S., Xiao, L., Southall, N., Lu, J., Inglese, J., Brasch, M., Austin , C. P. & Zheng, W.
Journal of Biomolecular Screening, 2008, In press.
Urban, D.J., Zheng, W., Goker-Alpan, O., Jadhav, A., LaMarca, M.E., Inglese, J., Sidransky, E. & Austin, C.P.
Combinatorial Chemistry & High Throughput Screening, 2008, In press.
Vogt, A., McDonald, P.R., Tamewitz, A., Sikorski, R., Wipf, P., Skoko, J.J., & Lazo, J.S.
Molecular Cancer Therapeutics, 2008, In press.
Identification of Off-Patent Drugs That Reverse Daunorubicin Efflux Mediated by ABCB1 in T-ALL Cells.
Winter, S,. Lovato, D., Khawaja, H., Edwards, B., Ivnitski-Steele. I., Young, S., Estes, D., Oprea, T., Sklar, L., & Larson, R.
SBS, 2008, 15, 185-193.
Compound cytotoxicity profiling using quantitative high-throughput screening.
Xia, M., Huang, R., Witt, K.L., Southall, N., Fostel, J., Cho, M.H., Jadhav, A., Smith, C.S., Inglese, J., Portier, C.J., Tice, R.R., & Austin, C.P.
Environmental Health Prospectives, 2008, In press.
Data mining a small molecule drug screening representative subset from NIH PubChem.
Xie, X.-Q. & Chen, J.-Z.
Journal of Chemical Information and Modeling, 48(3), 465-475.
Xie, Y., Deng, S., Thomas, C.J., Liu, Y., Zhang, Y-Q., Rinderspacher, A., Huang, W., Gong, G., Wyler, M., Cayanis, E., Aulner, N., Tobben, U., Chung, C., Pampou, S., Southall, N., Vidovic, D., Schurer, S., Branden, L., Davis, R. E., Staudt, L. M., Inglese, J., Austin, C.P., Landry, D.W., Smith, D.H., & Auld, D.S.
Bioorganic and Medicinal Chemistry Letters, 2008, 18, 329-335.
Compound management for quantitative high-throughput screening.
Yasgar, A., Shinn, P., Jadhav, A., Auld, D.S., Michael, S., Zheng, W., Austin, C.P., Inglese, J., & Simeonov, A.
Journal of the Association for Laboratory Automation, 2008, 12(2), 79-89.
Zhu, H., Rusyn, I., Richard, A. & A. Tropsha
Environmental Health Perspectives, 2008, 116, 4, 506-513.
Zhu, P.J., Zheng, W., Auld, D.S., Jadhav, A., Macarthur, R., Olson , K.R., Peng, K., Dotimas, H., Austin, C.P., Inglese, J.
Combinatorial Chemistry & High Throughput Screening, 2008, 11(7), 545-559.