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  • Related References Published by Members of the PMLSC
  • HCS Related References
  • HTS Related References
    bullet point  Related References Published by Members of the PMLSC
  • Arnold, D.M., et al., Synthesis and biological activity of a focused library of mitogen-activated protein kinase phosphatase inhibitors. Chem Biol Drug Des, 2007. 69: p. 23-30.
    Johnston, An interview with Paul A. Johnston, Ph.D., by Vicki Glaser. Assay Drug Dev Technol., 2007. 5(3): p. 289-97.
  • Johnston, P.A., et al., 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 Drug Dev Technol, 2007. 5: p. 319-32.
  • Johnston, P.A., et al., High throughput screening (HTS) identifies novel and specific uncompetitive inhibitors of the two-componenet NS2B-NS3 proteinase of West Nile virus. Assay Drug Dev Technol. 5: p 737-750
  • Lazo, J.S., Roadmap or roadkill: a pharmacologist's analysis of the NIH Molecular Libraries Initiative. Mol Interv, 2006. 6: p. 240-3.
  • Lazo, J.S., L.S. Brady, and R. Dingledine, Building a pharmacological lexicon: small molecule discovery in academia. Mol Pharmacol, 2007. 72: p. 1-7.
  • Sharlow, E.R., et al., Development and Implementation of a Miniaturized High Throughput Timed-Resolved – Fluorescence Energy Transfer Assay to Identify Small Molecule Inhibitors of Polo-like Kinase I. Assay Drug Dev Technologies, 2007. 5: p. 723-735.
  • Tierno, M.B., et al., Development and optimization of high-throughput in vitro protein phosphatase screening assays. Nat Protoc, 2007. 2: p. 1134-44.
  • Vogt, A. and J.S. Lazo, Discovery of protein kinase phosphatase inhibitors. Methods Mol Biol, 2007. 356: p. 389-400.
  • Vogt, A. and J.S. Lazo, Implementation of high-content assay for inhibitors of mitogen-activated protein kinase phosphatases. Methods, 2007. 42: p. 268-77.
  • Guo, J., Parise, R., Joseph, E., Egorin, M. Lazo, J.S., Prochownik, E., and Eiseman, J. Efficacy, pharmacokinetics, tissue distribution, and metabolism of the Myc-Max disruptor, 10058-F4 [Z,E]-5-[4-ethylbenzylidine]-2-thioxothiazolidin-4-one, in mice. Cancer Chemother Pharmacol. In Press
  • Sharlow, E.R., Leimgruber, S., Yellow-Duke, A., Barrett, R., Wang, Q.J., and Lazo, J.S. Development, validation and implementation of immobilized metal affinity for phosphochemicals (IMAP)-based high-throughput screening assays for low-molecular-weight compound libraries. Nature Protocols. In Press
  • Lazo, J.S. Speaking of Pharmacology, Rear-view mirrors and crystal balls: A brief reflection on drug discovery. Mol Interv. 8:60-63, 2008.
  • Queiroz de Oliveira, P.E., Tomko, R.J. Jr, and Lazo, J.S. Is a step backwards in s-phase-targeted chemotherapy a step forward? Mol Interv. 8:137-40, 2008. PMID: 18693192
  • Hermone, A. R., Burnett, J. C., Nuss, J. E., Tressler, L. E., Nguyen, T. L., Solaja, B. A., Vennerstrom, J. L., Schmidt, J. J., Wipf, P., Bavari, S., and Gussio, R. Three-Dimensional Database Mining Identifies a Unique Chemotype that Unites Structurally Diverse Botulinum Neurotoxin Serotype A Inhibitors in a Three-Zone Pharmacophore. Chem Med Chem. In Press, 2008.
  • Timmons, C.; Wipf, P. J. DFT Calculation of 13C NMR Shifts of Phenanthrenoid Alkaloids: Reinvestigation of the Structure of Samoquasine A. Org Chem. In Press, 2008.
    Rabu, C., Wipf, P. and Brodsky, J. L. High, S. J. A Precursor Specific Role for Hsp40/Hsc70 during Tail-Anchored Protein Integration at the Endoplasmatic Reticulum. Biol Chem. In Press, 2008.
  • Gu, L.; Wang, B., Kulkarni, A., Geders, T. W., Grindberg, R. V., Gerwick, L., Hakansson, K., Wipf, P., Smith, J. L., Gerwick, W. H., and Sherman, D. H. Nature Metamorphic Enzyme Assembly in Polyketide Diversification. Chem Biol. Submitted, 2008,
  • Pierce, J. G., Kasi, D., Fushimi, M., Cuzzupe, A., and Wipf, P. Synthesis of Hydroxylated Bicyclic Amino Acids from L-Tyrosine: Octahydro-1H-indole Carboxylates. Org Chem. In Press, 2008.
  • Bakan, A., Lazo, J. S., Wipf, P., Brummond, K. M., and Bahar, I. Toward a Molecular Understanding of the Interaction of Dual Specificity Phosphatases with Substrates: Insights from Structure-Based Modeling and High Throughput Screening. Curr. Med. Chem. In Press, 2008.
  • Johnston, P. A., Soares, K. M., Shinde, S. N., Foster, C. A., Shun, T. Y., Takyi, H. K., Wipf, P., and Lazo, J. S. Development of a 384-well Colorimetric Assay to Quantify Hydrogen Peroxide Generated by the Redox Cycling of Compounds in the Presence of Reducing Agents. Assay Drug Dev Technol. In Press, 2008.
  • Faraji, A. H.; Wipf, P. Nanoparticles in Cellular Drug Delivery. Comb Chem High Throughput Screen. In Press, 2008.
  • Keinan, S., Paquette, W. D., Skoko, J. J., Beratan, D. N., Yang, W., Shinde, S., Johnston, P. A., Lazo, J. S., and Wipf, P. Computational Design, Synthesis and Biological Evaluation of para-Quinone-Based Inhibitors for Redox Regulation of the Dual-Specificity Phosphatase Cdc25B. Org Biomol Chem. 6:3256-3263, 2008.
  • Lazo, J. S.; Wipf, P. Is Cdc25 a Druggable Target? Anti-Cancer Agents Med Chem. In Press, 2008.
  • Wipf, P. Sixteen Semesters of Chemistry at the University of Zürich: A Retrospective on a Formative Time. Chimia 62:150-151, 2008.
  • Walczak, M. A. A., and Wipf, P. J. Rhodium(I)-Catalyzed Cycloisomerizations of Bicyclobutanes. Am Chem Soc. 130:6924-6925, 2008.
  • Ihle, N. T., Lemos, R., Wipf, P., Yacoub, A., Mitchell, C., Siwak, D., Mills, G. B., Dent, P., Kirkpatrick, D. L., and Powis, G. Identification of Oncogenic Ras as a Marker for Intrinsic in vivo Resistance to Single Agent Activity of the Specific PI-3-Kinase Inhibitor, PX-866. xxx. Submitted, 2008.
  • Braunstein, M. J., Scott, C. M., Behrman, S., Walter, P., Wipf, P., Smith, E. L. P., Brodsky, J. L., Batuman, O. Inhibitors of the Hsp70 Molecular Chaperone and the Proteasome Show Synergistic Antimyeloma Effects. Cancer Res. Submitted, 2008.
  • A Vogt, A., McDonald, P. R., Tamewitz, A., Sikorski, R. P., Wipf, P., Skoko, J. J., and Lazo, J. S. Cell-Active Inhibitor of Mitogen-Activated Protein Kinase Phosphatases Restores Paclitaxel-Induced Apoptosis in Dexamethasone-Protected Cancer Cells. Mol Cancer Ther. 7: 330-340, 2008.
  • Jiang, J., Belikova, N., Hoye, A. T., Zhao, Q., Epperly, M. W., Greenberger, J. S., Wipf, P., and Kagan, V. E. A Mitochondria-Targeted Nitroxide/Hemigramicidin S Conjugate Protects Mouse Embryonic Cells Against Gamma Irradiation. Int J Radiat Oncol Biol Phys. 70: 816-825, 2008.
  • Feng, L., Du, D., Fuller, A. A., Davoren, J. E., Wipf, P., Kelly, J. W., and Gruebele, M. An Experimental Survey of the Transition between Two-State and Downhill Protein Folding Scenarios. Proc Natl Acad Sci USA. 105:2369-2374, 2008.
  • Balachandran, R., Hopkins, T. D., Thomas, C. A., Wipf, P., and Day, B. W. Tubulin-Perturbing Naphthoquinone Spiroketals. Chem Biol Drug Desig. 71:117-124, 2008.
  • Zuber, G., Wipf, P., and Beratan, D. N. Exploring the Optical Activity Tensor by Anisotropic Rayleigh Optical Activity Scattering. ChemPhysChem. 9: 265-271, 2008.
  • Wright, C. M., Chovatiya, R. J., Jameson, N. E., Turner, D. M., Zhu, G., Werner, S., Huryn, D. M., Pipas, J. M., DayB. W., Wipf, P., and Brodsky, J. L. Pyrimidinone-Peptoid Hybrid Molecules with Distinct Effects on Molecular Chaperone Function and Breast Cancer Cell Proliferation. Bioorg Med Chem. 16:3291-3301, 2008.
  • Hoye, A. T., Davoren, J., Wipf, P., Fink, M. P., and Kagan, V. E. Targeting Mitochondria. Acc Chem Res. 41:87–97, 2008.
  • Ihle, N. T., Lemos, R., Schwartz, D., Oh, J., Halter, R. J., Wipf, P., Kirkpatrick, D. L., and Powis, G. The PPARg Agonist Pioglitazone Prevents the Increase in Blood Glucose Caused by Phosphoinositide-3-kinase Pathway Inhibition without Blocking Antitumor Activity. Clin Cancer Res. Submitted, 2008.
  • Wipf, P. and Jayasuriya, N. Chiral Ligand Optimization in the Asymmetric Zirconium-Zinc Transmetalation Aldehyde Addition Reaction. Chirality. 20:425-430, 2008.
  • Shrivastava IH, Jiang J, Amara SG and Bahar I. Time-resolved mechanism of extracellular gate opening and substrate binding in glutamate transporter. J Biol Chem, 2008. PMID: 18678877.
  • Engen JR, Wales TE, Hochrein JM, Meyn MA III, Ozkan SB, Bahar I and Smithgall TE. Structure and dynamic regulation of Src-family kinases. Cell Mol Life Sci, 2008. PMID: 18563293.
  • Bagci EZ, Vodovotz Y, Billiar TR, Ermentrout B and Bahar I. Computational Insights on the Competing Effects of Nitric Oxide in Regulating Apoptosis. PLoS ONE 3, e2249, 2008.
  • Isin B, Schulten K, Tajkhorshid E, Bahar I. Mechanism of Signal Propagation upon Retinal Isomerization: Insights from Molecular Dynamics Simulations of Rhodopsin Restrained by Normal Modes. Biophysical J. 95: 789-803, 2008. PMID: 18390613
  • Liu Y, Eyal E, Bahar I. Analysis of correlated mutations in HIV-1 protease using spectral clustering. Bioinformatics. 24:1243-50, 2008. PMID: 18375964
  • C. Chennubhotla, Z. Yang and Bahar I. Coupling between global dynamics and signal transduction pathways: a mechanism of allostery for chaperonin GroEL. Mol. BioSyst. 4:287-292, 2008.
  • Eyal E, Bahar I. Toward a molecular understanding of the anisotropic response of proteins to external forces: insights from elastic network models. Biophys J. 94:3424-35, 2008.
  • Johnston PA, Soares KM, Shinde SN, Foster CA, Shun TY, Takyi HK, Wipf P, and Lazo JS. Development of a 384-well Colorimetric Assay to Quantify Hydrogen Peroxide Generated by the Redox Cycling of Compounds in the Presence of Reducing Agents. Assay and Drug Development Technologies. In Press, 2008.
  • Keinan S, Paquette WD, Skoko JJ, Beratan DN, Yang W, Shinde S, Johnston PA, Lazo JS, and Wipf P. Computational design, synthesis and biological evaluation of para-quinone-based inhibitors for redox regulation of the dual-specificity phosphatase Cdc25B. Org Biomol Chem. In Press, 2008.
  • Raccor,B.S., Vogt,A., Sikorski,R.P., Madiraju,C., Balachandran,R., Montgomery,K., Shin,Y., Fukui,Y., Jung,W.H., Curran,D.P., and Day,B.W. (2008). Cell-based and biochemical structure-activity analyses of analogs of the microtubule stabilizer dictyostatin. Mol. Pharmacol. 73, 718-726.
  • Vogt,A., McDonald,P.R., Tamewitz,A., Sikorski,R.P., Wipf,P., Skoko,J.J., III, and Lazo,J.S. (2008). A cell-active inhibitor of mitogen-activated protein kinase phosphatases restores paclitaxel-induced apoptosis in dexamethasone-protected cancer cells. Mol. Cancer Ther. 7, 330-340.
  • Zou,H., Thomas,S.M., Yan,Z.W., Grandis,J.R., Vogt,A., and Li,L.Y. (2008). Human rhomboid family-1 gene RHBDF1 participates in GPCR-mediated transactivation of EGFR growth signals in head and neck squamous cancer cells. FASEB J [epub ahead of print]

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    bullet point  HCS Related References
  • Gough, A.H. and P.A. Johnston, Requirements, features and performance of high content screening platforms, in high content screening: a powerful approach to systems cell biology and drug discovery. Methods in Molecular Biology, 2006. 356: p. 41-61.
  • Williams, R.G., et al., Generation and characterization of a stable MK2-EGFP cell line and subsequent development of a high-content imaging assay on the Cellomics ArrayScan platform to screen for p38 mitogen-activated protein kinase inhibitors. Methods Enzymol, 2006. 414: p. 364-89.
  • Trask, O.J., Jr., et al., Assay development and case history of a 32K-biased library high-content MK2-EGFP translocation screen to identify p38 mitogen-activated protein kinase inhibitors on the ArrayScan 3.1 imaging platform. Methods Enzymol, 2006. 414: p. 419-39.
  • Nickischer, D., et al., Development and implementation of three mitogen-activated protein kinase (MAPK) signaling pathway imaging assays to provide MAPK module selectivity profiling for kinase inhibitors: MK2-EGFP translocation, c-Jun, and ERK activation. Methods Enzymol, 2006. 414: p. 389-418.
  • Madiraju, C., et al., Tubulin assembly, taxoid site binding, and cellular effects of the microtubule-stabilizing agent dictyostatin. Biochemistry, 2005. 44: p. 15053-63.
  • Vogt, A., et al., Cell-active dual specificity phosphatase inhibitors identified by high-content screening. Chem Biol, 2003. 10: p. 733-42.
  • Vogt, A., E.N. Kalb, and J.S. Lazo, A scalable high-content cytotoxicity assay insensitive to changes in mitochondrial metabolic activity. Oncol Res, 2004. 14: p. 305-14.
  • Vogt, A. and J.S. Lazo, Chemical complementation: a definitive phenotypic strategy for identifying small molecule inhibitors of elusive cellular targets. Pharmacol Ther, 2005. 107: p. 212-21.
  • Vogt, A. and J.S. Lazo, Discovery of protein kinase phosphatase inhibitors. Methods Mol Biol, 2007. 356: p. 389-400.
  • Vogt, A. and J.S. Lazo, Implementation of high-content assay for inhibitors of mitogen-activated protein kinase phosphatases. Methods, 2007. 42: p. 268-77.
  • Vogt, A., et al., Spatial analysis of key signaling proteins by high-content solid-phase cytometry in Hep3B cells treated with an inhibitor of Cdc25 dual-specificity phosphatases. J Biol Chem, 2001. 276: p. 20544-50.
  • Vogt, A., et al., The benzo[c]phenanthridine alkaloid, sanguinarine, is a selective, cell-active inhibitor of mitogen-activated protein kinase phosphatase-1. J Biol Chem, 2005. 280: p. 19078-86.
  • Vogt, A., et al., The antisignaling agent SC-alpha alpha delta 9, 4-(benzyl-(2-[(2,5-diphenyloxazole-4-carbonyl)amino]ethyl)carbamoyl)- 2-decanoylaminobutyric acid, is a structurally unique phospholipid analogue with phospholipase C inhibitory activity. Mol Cancer Ther, 2002. 1: p. 885-92.
  • P. A. Johnston. (2007) “Automated High Content Screening Microscopy” Chapter 2, p25-42, in High Content Screening: Science, Technology and Applications. John Wiley & Sons, Inc; Edited by: Stephen A. Haney.
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    bullet point  HTS Related References
  • Carpenter, J; C. Laethem, F. R. Hubbard, T. K. Eckols, M. Baez, D. McClure, D. L. G. Nelson, and P. A. Johnston. (2002). Configuring Radioligand receptor Binding Assays for HTS using Scintillation Proximity Assay Technology. High Throughput Screening: Methods and Protocols, in Methods in Molecular Biology, 190: 31-49. The Humana Press, Inc. Edited by W. P. Janzen.
  • Johnston, P. A. and P. A. Johnston (2002). Cellular Platforms for HTS: three case studies. Drug Discovery Today 7: 353-363.
  • Pratt S, Shepard RL, Kandasamy RA, Johnston PA, Perry W 3rd, and Dantzig AH. (2005). The multidrug resistance protein 5 (ABCC5) confers resistance to 5-fluorouracil and transports its monophosphorylated metabolites. Mol. Cancer Ther. 4:855-63.
  • Razonable RR, Henault M, Lee LN, Laethem C, Johnston PA, Watson HL, Paya CV. (2005) Secretion of proinflammatory cytokines and chemokines during amphotericin B exposure is mediated by coactivation of toll-like receptors 1 and 2 Antimicrob Agents Chemother. 49(4):1617-21.
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