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 Publications for the year 2005 |
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John S. Lazo, PhD
Zhou, B.-N., Tang, S., Johnson, R.K., Mattern, M.R., Lazo, J.S., Sharlow, E.R., Harich, K.C. and Kingston, D.G.I. New glycolipid inhibitors of Myt1 kinase. Tetrahedron 61:883-887, 2005.
Cao, S., Foster, C., Brisson, M., Lazo, J.S. and Kingston, D.G.I. Halenaquinone and xestoquinone derivatives, inhibitors of Cdc25B phosphatase from a Xestospongia sp. Bioorg. Med. Chem. 13:999-1003, 2005.
Koldamova, R.P., Lefterov, I.M., Staufenbiel, M., Wolfe, D., Huang, S., Glorioso, J.C., Walter, M., Roth, M.G. and Lazo, J.S. The LXR ligand T0901317 decreases amyloid beta production in vitro and in a mouse model of Alzheimer’s disease. J. Biol. Chem. 280:4079-4088, 2005.
Cao, S., Foster, C., Lazo, J.S., Kingston, D.G. Sesterterpenoids and an alkaloid from a Thorectandra sp. as inhibitors of the phosphatase Cdc25B. Bioorg Med Chem. 13:5094-8, 2005.
Vasudevan, S.A., Skoko, J., Wang, K., Burlingame, S.M., Patel, P.N., Lazo, J.S., Nuchtern, J.G., Yang, J. MKP-8, a novel MAPK phosphatase that inhibits p38 kinase. Biochem Biophys Res Commun. 330:511-8, 2005.
Vogt, A., Tamewitz, A., Skoko, J., Sikorski, R., Giuliano, K.A. and Lazo, J.S. The benzo[c]phenanthridine alkaloid, sanguinarine, is a selective, cell-active inhibitor of mitogen-activated protein kinase phosphatase-1. J. Biol. Chem. 280:19078-19086, 2005.
Vogt, A. and Lazo, J.S. Chemical complementation: a definitive phenotypic strategy for identifying small molecule inhibitors of elusive cellular targets. Pharmacol. Therap. 107:212-221, 2005.
Xiao, D., Antosiewicz, A.H., Antosiewicz, J., Xiao, H., Brisson, M., Lazo, J.S. and Singh, S.V. Diallyl trisulfide-induced G2-M phase cell cycle arrest in human prostate cancer cells is caused by reactive oxygen species-dependent destruction and hyperphosphorylation of Cdc25C. Oncogene 24:6256-6268, 2005.
Cao, S., Foster, C., Lazo, J.S. and Kingston, D.G.I. Four diterpenoid inhibitors of Cdc25B phosphatase from a marine anemone. Bioorg. Med. Chem. 13:5830-5834, 2005.
Giuliano, K.A., Cheung, W.S., Curran, D.P., Day, B.W., Kassick, A.J., Lazo, J.S., Nelson, S.G., Shin, Y. and Taylor, D.L. Systems cell biology knowledge created from high content screening. Assay Drug Develop. Technol. 3:501-514. 2005.
Brisson, M., Nguyen, T., Wipf, P., Joo, B., Day, B.W., Skoko, J.S., Schreiber, E.M., Foster, C., Bansal, P. and Lazo, J.S. Redox regulation of Cdc25B by cell active quinolinediones. Molec. Pharmacol. 68:1810-1820. 2005.
Paul Johnston, PhD
Pratt S, Shepard RL, Kandasamy RA, Johnston PA, Perry W 3rd, and Dantzig AH. The multidrug resistance protein 5 (ABCC5) confers resistance to 5-fluorouracil and transports its monophosphorylated metabolites. Molec. Cancer Ther. 4:855-63, 2005.
Razonable RR, Henault M, Lee LN, Laethem C, Johnston PA, Watson HL, Paya CV. Secretion of proinflammatory cytokines and chemokines during amphotericin B exposure is mediated by coactivation of toll-like receptors 1 and 2 Antimicrob Agents Chemother. 49:1617-21, 2005.
Barry Gold, PhD
Tentori, L., Forini, O., Fossile, E., Muzi, A., Vergati, M., Portarena, I., Amici, C., Gold, B., and Graziani, G. N3-Methyladenine induces early poly(ADP-ribosylation), reduction of NFkB DNA binding ability and nuclear up-regulation of telomerase activity. Molec. Pharmacol. 67:572-581, 2005.
Moulaei, T., Maehigashi, T., Lountos, G., Komeda, S., Watkins, D., Stone, M., Marky, L., Li, J.-S., Gold, B. and Williams, L.D. Structure of B-DNA with cations tethered in the major groove. Biochemistry 44:7458-7468, 2005.
Li, J.-S., Chen, F.-X., Shikiya, R., Marky, L.A. and Gold, B. Molecular recognition via triplex formation of mixed purine/pyrimidine DNA sequences using oligoTRIPs. J. Amer. Chem. Soc. 127:12657-12665, 2005.
Shikiya, R., Li, J.-S., Gold, B., Marky, L. A. Incorporation of a cationic 3-aminopropyl chain into the Dickerson-Drew dodecamer: Correlation of energetics, structure and hydration. Biochemistry 44:12582-12588, 2005.
Li, J.-S., Gold, B. Synthesis of C-Nucleosides designed to participate in triplex formation with native DNA: Specific recognition of an A:T base pair in DNA. J. Org. Chem. 70:8764-8771, 2005.
Tentori, L., Leonetti, C., Scarsella, M., Muzi, A., Vergati, M., Forini, O., Lacal, P.M. Ruffini, F. Gold, B., Li, W., Zhang, J. and Graziani, G. Poly (ADP-ribose) glycohydrolase inhibitor as chemosensitiser of malignant melanoma for temozolomide. Eur. J. Cancer 41:2948-2957, 2005.
Billy W. Day, PhD
Madiraju, C., Edler, M.C., Hamel, E., Raccor, B.S., Balachandran, R., Zhu, G., Giuliano, K.A., Vogt, A., Shin, Y., Fournier, J.-H., Fukui, Y., Brückner, A.M., Curran, D.P., Day, B.W. Tubulin assembly, taxoid site binding and cellular effects of the microtubule-stabilizing agent dictyostatin. Biochem. 44:15053-15063, 2005.
Nguyen, T.L., McGrath, C., Hermone, A.R., Burnett, J.C., Zaharevitz, D.W., Day, B.W., Wipf, P., Hamel, E., Gussio, R. A common pharmacophore for a diverse set of colchicine site inhibitors using a structure-based approach. J. Med. Chem. 48:6107-6116 [correction p. 7917], 2005.
Shin, Y., Fournier, J.H., Balachandran, R., Madiraju, C., Raccor, B.S., Zhu, G., Edler, M.C., Hamel, E., Day, B.W., Curran, D.P. Synthesis and biological evaluation of (–)-16-normethyldictyostatin: a potent analog of (–)-dictyostatin. Organic Ltrs. 7:2873-2876, 2005.
Mu, Y., Stephenson, C.R.J., Kendall, C., Saini, S.P.S., Toma, D., Ren, S., Cai, H., Strom, S.C., Day, B.W., Wipf, P., Xie, W. A pregnane X receptor agonist with unique species-dependent stereoselectivity and its implications in drug development. Molec. Pharmacol. 68:403-413, 2005.
Keohavong, P., Xi, L., Day, R.D., Zhang, L., Grant, S.G., Day, B.W., Ness, R.B., Bigbee, W.L. HPRT gene alterations in umbilical cord blood T-lymphocytes in newborns of mothers exposed to tobacco smoke during pregnancy. Mutation Res. 572:156-166, 2005.
Wipf, P., Coleman, C.M. Iyer, P.S., Fodor, M.D., Shafer, Y.A., Janjic, J.M., Stephenson, C.R.J., Kendall, C., Day, B.W. Microwave-assisted “libraries from libraries” approach toward the synthesis of allyl- and C-cyclopropylalkylamides. J. Combin. Chem. 7:322-330, 2005.
Beckner, M.E., Chen, X., An, J., Day, B.W., Pollack, I.F. Proteomic characterization of harvested pseudopodia with differential gel electrophoresis and specific antibodies. Lab. Invest. 85:316-327, 2005.
Cunningham, S.L., Cunningham, A.R., Day, B.W. CoMFA, HQSAR and molecular docking studies of butitaxel analogues with -tubulin. J. Molec. Model. 11:157-164, 2005.
Janjic, J.M., Mu, Y., Kendall, C., Stephenson, C.R.J., Balachandran, R., Raccor, B.S., Lu, Y., Zhu, G., Xie, W., Wipf, P., Day, B.W. New antiestrogens from a library screen of homoallylic amides, allylic amides and C-cyclopropylalkylamides. Bioorg. Med. Chem. 13:157-164, 2005.
Giuliano, K.A., Cheung, W.S., Curran, D.P., Day, B.W., Kassick, A.J., Lazo, J.S., Nelson, S.G., Shin, Y., Taylor, D.L. Systems cell biology knowledge created from high content screening. Assay Drug Develop. Tech. 3:501-514, 2005.
Brisson, M., Nguyen, T., Wipf, P., Joo, B., Day, B.W., Skoko, J.S., Schreiber, E.M., Foster, C., Bansal, P., Lazo, J.S. Redox regulation of Cdc25B by cell active quinolinediones. Molec. Pharmacol. 68;1810-1820, 2005
Marni Brisson, PhD
Cao, S., Foster, C., Brisson, M., Lazo, J.S., Kingston, D.G. Halenaquinone and xestoquinone derivatives, inhibitors of Cdc25B phosphatase from a Xestospongia sp. Bioorg. Med. Chem., 13:999-1003, 2005.
Xiao D., Herman-Antosiewicz, A., Antosiewicz, J., Xiao, H., Brisson, M., Lazo, J.S., Singh, S.V. Diallyl trisulfide-induced G(2)-M phase cell cycle arrest in human prostate cancer cells is caused by reactive oxygen species-dependent destruction and hyperphosphorylation of Cdc25C. Oncogene, 24:6256-6268, 2005.
Brisson, M., Nguyen, T., Wipf, P., Joo, B., Day, B.W., Skoko, J.S., Schreiber, E.M., Foster, C., Bansal, P., Lazo, J.S. Redox regulation of Cdc25B by cell-active quinolinediones. Molec. Pharmacol. 68:810-20, 2005.
Elizabeth Sharlow, PhD
Zhou B.N., Tang S, Johnson R.K., Mattern M.R., Lazo J,S,, Sharlow E.R., Harich K.C. and Kingston, D.G.I. New glycolipid inhibitors of Myt1 kinase. Tetrahedron 61:883-887, 2005.
Andreas Vogt, PhD
Wipf, P., Graham, T.H., Vogt, A., Sikorski, R.P., Ducruet, A.P., and Lazo, J.S. Cellular analysis of Disorazole C1 and structure-activity relationship of analogs of the natural product. Chem. Biol. Drug Design 67:66-73, 2005.
Madiraju, C., Edler, M.C., Hamel, E., Raccor, B.S., Balachandran, R., Zhu, G., Giuliano, K.A., Vogt, A., Shin, Y., Fournier, J.-H., Fukui, Y., Brücker, A.M., Curran, D.P., and Day, B.W. Tubulin aAssembly, taxoid site binding and cellular effects of the microtubule-stabilizing agent dictyostatin. Biochemistry 44:15053-15063, 2005.
Vogt, A., Tamewitz, A., Skoko, J., Sikorski, R.P., Giuliano, K.A., and Lazo, J.S. The benzo[c]phenanthridine alkaloid, sanguinarine, is a selective, cell-active inhibitor of mitogen-activated protein kinase phosphatase-1. J. Biol. Chem. 280:19078-09086, 2005.
Vogt, A., and Lazo, J.S. Chemical Complementation: A definitive phenotypic strategy for identifying small molecule inhibitors of elusive cellular targets. Pharmacol. Therap. 107:212-221, 2005.
Peter Wipf, PhD
Zuber, G., Goldsmith, M.-R., Hopkins, T.D., Beratan, D.N. and Wipf, P. Systematic assignment of the configuration of flexible natural products by spectroscopic & computational methods: The bistramide C analysis. Org. Lett. 7:5269-5272, 2005.
Wipf, P., Mahler, S.G. and Okumura, K. Metathesis reactions of pyrazolotriazinones generate dynamic combinatorial libraries. Org. Lett. 7:4483-4486, 2005.
Wipf, P., Lynch, S.M., Powis, G., Birmingham, A. and Englund, E.E. Synthesis and biological activity of prodrug inhibitors of the thioredoxin – thioredoxin reductase system. Org. Biomol. Chem. 3:3880-3882, 2005.
Brisson, M., Nguyen, T., Wipf, P., Joo, B., Day, B.W., Skoko, J.S., Schreiber, E.M., Foster, C., Bansal, P. and Lazo, J.S. Redox regulation of Cdc25B by cell active quinolinediones. Molec. Pharm. 2005, 68, 1810-20.
Ihle, N.T., Paine-Murrieta1, G., Berggren, M.I., Baker, A., Wipf, P., Abraham, R.T., Kirkpatrick, D.L. and Powis, G. The phosphoinositide-3-kinase inhibitor PX-866 overcomes resistance to the EGFR inhibitor Gefitinib in A-549 human non small cell lung cancer xenografts. Molec. Cancer Therap. 4:1349-1357, 2005.
Nguyen, T.L., McGrath, C., Hermone, A.R., Burnett, J.C., Zaharevitz, D.W., Day, B.W., Wipf, P., Hamel, E. and Gussio, R.J. A common pharmacophore for a diverse set of colchicine binding site inhibitors using a structure-based approach. Med. Chem. 48:6107-6116, 2005.
Wipf, P., Waller, D.L. and Reeves, J.T. Transition metal mediated cascade reactions: The water accelerated carboalumination-claisen rearrangement-carbonyl addition reaction. J. Org. Chem. 70:8096-8102, 2005.
Wipf, P., Xiao, J., Jiang, J., Belikova, N.A., Tyurin, V.A., Fink, M.P. and Kagan, V.E. Mitochondrial targeting of selective electron scavengers: Synthesis and biological analysis of hemigramicidin-TEMPO conjugates. J. Am. Chem. Soc. 127:12460-12461, 2005.
Wipf, P. and Pierce, J.G. Synthesis of homoallylic amines by hydrozirconation–imine addition of allenes. Org. Lett. 7:3537-3540, 2005.
Mu, Y., Stephenson, C.R.J., Kendall, C., Saini, S.P.S., Toma, D., Ren, S., Cai, H., Strom, S.C., Day, B.W., Wipf, P. and Xie, W. A pregnane X receptor agonist with unique species-dependent stereoselectivity and its implications in drug development. Molec. Pharmacol. 68:403-413, 2005.
Wipf, P., Werner, S., Woo, G.H.C., Stephenson, C.R.J., Walczak, M.A.A., Coleman, C.M. and Twining, L.A. Application of divergent multi-component reactions in the synthesis of a library of peptidomimetics based on γ-Amino-α,β-cyclopropyl acids. Tetrahedron (Symposium-in-Print No. 114 on Multicomponent Reactions) 61(48):11488-11500, 2005.
Wipf, P., Xiao, J. and Geib, S.J. Imine additions of internal alkynes for the synthesis of trisubstituted (E)-alkene and cyclopropane peptide isosteres. Adv. Synth. Catal. (Special Issue on C-C Bond Formation) 347:1605-1613.
Wipf, P. and Hopkins, T.D. Total synthesis and structure validation of (+)-bistramide C. Chem. Commun. 3421-3423, 2005.
Wipf, P. and Halter, R.J. Chemistry and biology of Wortmannin. Org. Biomol. Chem.3:2053-2061, 2005.
Wipf, P. and Xiao, J.J. Electrostatic vs steric effects in peptidomimicry. Synthesis and secondary structure analysis of gramicidin S analogs with (E)-alkene peptide isosteres. Amer. Chem. Soc. 127:5742-5743, 2005. |
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| Publications for the year 2006 |
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John S. Lazo, PhD
Wipf, P., Graham, T.H., Vogt, A. Sikorski, R., Ducruet, A., and Lazo, J.S. Cellular Analysis of disorazole C1 and structure-activity relationship of analogs of the natural product. Chemical Biol. Drug Design 67:66-73, 2006.
Vogt A., Lazo J.S. Discovery of protein kinase phosphatase inhibitors. Methods in Molecular Pharmacology 356:389-400, 2006.
Lazo, J.S., Nunes, R., Skoko, J.J., Queiroz de Oliveira, P.E., Vogt, A., and Wipf, P. Novel benzofuran inhibitors of human mitogen-activated protein kinase phosphatase-1. Bioorg. Med. Chem. 14:5643-5650, 2006.
Billy W. Day, PhD
Fan, Y., Schreiber, E.M., Giorgianni, A., Yalowich, J.C., Day, B.W. Myeloperoxidase-catalyzed metabolism of etoposide to its uinine and glutathione adduct forms in HL60 cells. Chem. Res.Toxicol. 19:937-943, 2006.
Atkins, J.L., Day, B.W., Handrigan, M.T., Zhang, Z., Pamnani, M.B., Gorbunov, N.V. Brisk production of nitric oxide and associated formation of S-nitrosothiols in early hemorrhage. J. Applied Physiol. 100:1267-1277, 2006.
Zhu, G., Yang, F., Balachandran, R., Höök, P., Vallee, R., Curran, D.P., Day, B.W. Synthesis and biological evaluation of purealin and analogues as cytoplasmic dynein heavy chain inhibitors. J. Med. Chem. 49:2063-2076, 2006.
Gong, H., Singh, S.V., Singh, S.P., Mu, Y., Saini, S.P.S., Toma, D. Ren, S. Kagan, V.E., Day, B.W. Zimniak, P., Xie, W. Orphan nuclear receptor PXR sensitizes oxidative stress responses in transgenic mice and cancerous cells. Molec. Endocrinol. 20:279-290, 2006.
Balasubramani, M., Day, B.W., Schoen, R.E., Getzenberg, R.H. Altered expression and localization of creatine kinase B, heterogenous nuclear ribonucleoprotein F and high mobility group box 1 protein in the nuclear matrix associated with colon cancer. Cancer Res. 66:763-769, 2006.
Fukui, Y., Brückner, A.M., Shin, Y., Balachandran, R., Day, B.W., Curran, D.P. Fluorous mixture synthesis of (–)-dictyostatin and three stereoisomers. Organic Ltrs. 8:301-304, 2006.
Khanday, F.A., Yamamori, T., Mattagajasingh, I., Zhang, Z., Bugayenko, A., Naqvi, A., Santhanam, L., Nabi, N., Kasuno, K., Day, B.W., Irani, K. Rac1 leads to phosphorylation-dependent increase in stability of the p66shc adaptor protein: role in Rac1-induced oxidative stress. Molec. Biol. Cell. 17:122-129, 2006.
Peter Wipf, PhD
Chen, Z., Yang, Y., Werner, S., Wipf, P. and Weber, S.G. A dcreening method for chiral Selectors that does not require covalent attachment. J. Am. Chem. Soc. 128:2208-2209, 2006.
Wipf, P., Graham, T.H., Vogt, A., Sikorski, R., Ducruet, A.P. and Lazo, J.S. Cellular analysis of disorazole C1 and structure-activity relationship of analogs of the natural product. Chem. Biol. Drug Design 67:66-73, 2006.
Chen, Z., Yang, Y., Werner, S., Wipf, P. and Weber, S.G. A screening method for chiral selectors that does not require covalent attachment. J. Am. Chem. Soc. 128:2208-2209, 2006.
Goldsmith, M.-R., George, C.B., Zuber, G, Naaman, R., Waldeck, D.H., Wipf, P. and Beratan, D.N. The chiroptical signature from achiral metal clusters induced by dissymmetric adsorbates. Phys. Chem. Chem Phys. 8:63-67, 2006. |
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| Publications for the year 2007 |
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Billy W. Day, PhD
Thomas, C.A., Grant, S.G., Pflug, B.R., Getzenberg, R.H., Day, B.W. Z-1,1-Dichloro-2-(4-methoxyphenyl)-3-phenylcyclopropane induces concentration-dependent growth inhibition, apoptosis and upregulation of apoptotic genes in TRAMP cells. Urol. Oncol. 25, in press, 2007.
Wipf, P., Gong, H., Janjic, J.M., Li, S., Day, B.W., Xie, W. New opportunities for pregnane X receptor (PXR) targeting in drug development. Lessons from enantio- and species-specific PXR ligands identified from a discovery library of amino acid analogues. Mini-Rev. Med. Chem. 7, in press 2007.
Heussner, A.H., Moeller, I., Day, B.W., Dietrich, D.R., O'Brien, E. Production and characterization of monoclonal antibodies against ochratoxin B. Food Chem. Toxicol. 45, in press,2007.
Escobar, P.A., Olivero, O.A., Wade, N.A., Abrams, E.J., Nesel, C.J., Ness, R.B., Day, R.D., Day, B.W., Meng, Q., O'Neill, J.P., Walker, D.M., Poirier, M.C., Walker, V.E., Bigbee, W.L. Genotoxicity assessed by the comet and GPA assays following in vitro exposure of human lymphoblastoid cells (H9) or perinatal exposure of mother-child pairs to AZT or AZT-3TC. Environ. Mol. Mutagen. 48, 330-343, 2007.
Buey, R.M., Calvo, E., Barasoain, I., Pineda, O., Edler, M.C., Matesanz, R., Cerezo, G., Vanderwal, C.D., Day, B.W., Sorensen, E.J., López, J.A., Andreu, J.M., Hamel, E., Díaz, J.F. Cyclostreptin binds covalently to microtubule pores and lumenal taxoid binding sites. Nature Chem. Biol. 3, 117-125, 2007.
Marni Brisson, PhD
Brisson, M., Foster, C., Wipf, P., Beomjun, J., Tomko, R.J., Jr., Nguyen, T., Lazo, J.S. “Independent mechanistic inhibition of Cdc25 phosphatases by a natural product caulibugulone” Molecular Pharmacology 71, 184-192, 2007.
Tierno, M.B., Johnston, P.A., Foster, C., Skoko, J.J., Shinde, S.N., Shun, T. Y., and Lazo, J.S. Development and optimization of high-throughput in vitro protein phosphatase screening assays. Nature Protocols. 2:1134-1144, 2007. [Cover Article]
Andreas Vogt, PhD
Vogt, A., and Lazo, J.S. Discovery of protein kinase phosphatase inhibitors. IN: Methods in Molecular Biology: High Content Screening. Eds. Giuliano, K., Taylor, D.L., and Haskins J.R. Humana Press, New Jersey. 356:389-400, 2007.
Vogt, A., and Lazo, J.S. Implementation of high-content assay for inhibitors of mitogen-activated protein kinase phosphatases. Methods 42, 268-277 (2007)
Wang, Z., McPherson, P.A., Day, B.W., Vogt, A., Raccor, B., and Wipf. P., Structure-Activity and High-Content Imaging Analyses of Novel Tubulysins. Chemical Biology and Drug Design 70 (2), 75-86 (2007)
Jung, W.-H., Harrison, C., Shin, Y., Fournier, J.-H., Balachandran, R., Raccor, B.S., Sikorski, R.P., Vogt, A., Curran, D.P. and Day, B.W. Total synthesis and biological evaluation of C16 analogs of (–)-dictyostatin J. Med. Chem. 50 (13), 2951-2966 (2007)
Shin, Y., Fournier, J.-H., Brückner, A.M., Madiraju, C., Balachandran, R., Raccor, B.S., Edler, M.D., Hamel, E., Sikorski, R.P., Vogt, A., Day, B.W. and Curran, D.P. Synthesis and biological evaluation of (–)-dictyostatin and stereoisomers. Tetrahedron 63, 8537-8562 (2007)
Elizabeth Sharlow, PhD
Ramanathan RK, Kirkpatrick DL, Egorin MJ, Friedland D, Belani CP, Green SB, Chow HH S, Cordova CA, Stratton SP, Sharlow ER, Baker A, and T Dragovich. 2007. A Phase I, Pharmacokinetic and Pharmacodynamic Study of PX-12, a Novel Inhibitor of Thioredoxin-1, in Patients with Advanced Solid Tumors. Clinical Cancer Research 13: 2109 – 2014.
Sharlow E, Leimgruber S, Shun T and Lazo J. (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 & Drug Development Technologies 5(6): 723 – 735.
Paul Johnston
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.
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
Tierno, M.B., Johnston, P.A., Foster, C., Skoko, J.J., Shinde, S.N., Shun, T. Y., and Lazo, J.S. Development and optimization of high-throughput in vitro protein phosphatase screening assays. Nature Protocols. 2:1134-1144, 2007. [Cover Article]
Peter Wipf, PhD
"Mitochondrial Targeting of Radioprotectants Using Peptidyl Conjugates." Kanai, A.; Zabbarova, I.; Amoscato, A.; Epperly, M.; Xiao, J.; Wipf, P. Org. Biomol. Chem. 5(2), 307-309, 2007.
"Treatment with a Novel Hemigramicidin-TEMPO Conjugate Prolongs Survival in a Rat Model of Lethal Hemorrhagic Shock." Macias, C. A.; Chiao, J. W.; Xiao, J.; Arora, D. S.; Tyurina, Y. Y.; Delude, R. L.; Wipf, P.; Kagan, V. E.; Fink, M. P. Ann. Surg. 245(2), 305-314, 2007.
"Spiroketals via Oxidative Rearrangement of Enol Ethers." Waller, D. L.; Stephenson, C. R. J.; Wipf, P. Org. Biomol. Chem. 5, 58-60, 2007.
"HPLC Determinations of Enantiomeric Ratios." Wipf, P.; Werner, S.; Twining, L. A.; Kendall, C. Chirality
19, 5-9, 2007.
John Lazo, PhD
Lazo, J.S. In the forefront of basic and translational cancer research – 7th AACR-JCA Joint International Conference. IDrugs. 10:224-6, 2007.
Lazo, J.S. Pharmacology goes phlat: Molecular Interventions feels the impact. Mol Interv. 7:178, 2007.
Lazo, J.S., Skoko, J.S., Werner, S., Mitasev, B., Bakan, A., Koizumi, F., Yellow-Duke, A. Bahar, I., and Brummond, K.M. Structurally unique inhibitors of human mitogen-activated protein kinase phosphatase-1 identified in a pyrrole carboxamide library. J Pharmacol Exp Ther. 322:940-947, 2007. [Cover Article]
Guo, J., Parise, R.A., Joseph, E., Lan, J., Pan, S., Joo, B., Egorin, M.J., Wipf, P., Lazo, J.S., and Eiseman, J.L. Pharmacology and antitumor activity of a quinolinedione Cdc25phosphatase inhibitors DA3003-1 (NSC 663284). Anticancer Res. 27:3067-73, 2007.
Wang, H., Hammoudeh, D.I., Follis, A.V., Reese, B.E., Lazo, J.S., Metallo, S.J., and Prochownik, E.V. Improved low molecular weight myc-max inhibitors. Molec Cancer Ther. 6:2399-2408, 2007.
Giuliano, K.A., Cheung, W.S., Curran, D.P., Day, B.W., Kassick, A.J., Lazo, J.S., Nelson, S.G., Shin, Y., and Taylor, D.L. Systems cell biology knowledge created from high content screening. Assay Drug Dev Technol. 3:501-514, 2007.
Srivastava, S.K., Bansal, P., Oguri, T., Lazo, J.S., and Singh, S.V. Cell division cycle 25B phosphatase is essential for benzo(a)pyrene-7,8-diol-9,10-epoxide–induced neoplastic transformation. Cancer Res. 67:9150-9157, 2007.
Bansal, P., and Lazo, J.S. Induction of Cdc25B regulates cell cycle resumption after genotoxic stress. Cancer Res. 67:3356-3363, 2007.
Montoya, S.E., Thiels, E., Card, J.P., and Lazo, J.S. Astrogliosis and behavioral changes in mice lacking the neutral cysteine protease bleomycin hydrolase. Neuroscience. 146:890-900, 2007.
Panchal, R.G., Ruthel, G., Brittingham, K.C., Lane, D., Kenny, T.A., Gussio, R., Lazo, J.S., and Bavari, S. Chemical genetic screening identifies critical pathways in anthrax lethal toxin-induced pathogenesis. Chem Biol, 14:245-55, 2007. [Cover Article]
Towne, C.F., York, I.A., Watkin, L.B., Lazo, J.S., and Rock, K.L. Analysis of the role of bleomycin hydrolase in antigen presentation and the generation of CD8 T cell responses. J Immunol. 178:6923-30, 2007.
Lazo, J.S., Brady, L.S., and Dingledine, R.J. Building a pharmacological lexicon: small molecule discovery in academia. Mol Pharmacol. 72:1-7, 2007.
Montoya, S.E., Thiels, E., Card, J.P., and Lazo, J.S. Astrogliosis and behavioral changes in mice lacking the neutral cysteine protease bleomycin hydrolase. Neuroscience. 146:890-900, 2007.
Panchal, R.G., Ruthel, G., Brittingham, K.C., Lane, D., Kenny, T.A., Gussio, R., Lazo, J.S., and Bavari, S. Chemical genetic screening identifies critical pathways in anthrax lethal toxin-induced pathogenesis. Chem Biol, 14:245-55, 2007. [Cover Article]
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| Publications for the year 2008 |
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John S. Lazo, PhD
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
Barry Gold, PhD.
Wang, F., Li, F., Ganguly, M., Marky, L. A., Gold, B., Egli, M. and Stone, M. P. A bridging water anchors the tethered 5-(3-aminopropyl)-2-deoxyuridine amine in the DNA major groove proximate to the N+2 C•G base pair: Implications for formation of interstrand 5’-GNC-3’ cross-links by nitrogen mustards. Biochemistry. 47:7147-7157, 2008.
Monti, P., Ciribilli, Y., Russo, D., Bisio, A., Perfumo, C., Andreotti, V., Menichini, P., Inga, A., Huang, X., Gold, B. and Fronza, G. REV1 and Polζ influence toxicity and mutagenicity of Me-lex, a sequence selective N3-adenine methylating agent. DNA Repair. 7:431-438, 2008.
Peter Wipf, Ph.D.
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.
Ivet Bahar, Ph.D.
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.
Kay M. Brummond, Ph.D.
Werner, S., David T.M., Chambers, P.G., and Brummond, K.M. Skeletal and Appendage Diversity as Design Elements in the Synthesis of a Discovery Library of Nonaromatic Polycyclic 5-Iminooxazolidin-2-ones, Hydantoins, and Acylureas. Tetrahedron Symposia-in-Print, Synthetic Advances in Transition Metal-Catalyzed Bond-Forming Reactions. 64:6997-7007, 2008.
Brummond, K.M., Chen, D., and Davis, M.M. A General Synthetic Route to Differentially Functionalized Angularly and Linearly Fused [6-7-5] Ring Systems: A Rh(I)-Catalyzed Cyclocarbonylation Reaction. J Org Chem. 73:5064-5068, 2008.
Mao, S., Probst, D.A., Werner, S., Chen, J., Xie, X., and Brummond, K.M. Diverging Rh(I)-Catalyzed Carbocyclization Strategy to Prepare a Library of Unique Cyclic Ethers. J Comb Chem. 10: 235-246, 2008.
Dennis Curran, Ph.D.
Raccor, B.S., Vogt, A., Sikorski, R.P., Madiraju, C., Balanchandran, R., Montgomery, K., Shin, Y., Fukui, Y., Jung, W.-H., Curran, D.P, and Day, B.W. Cell-based and biochemical structure-activity analyses analogs of the microtubule stabilizer dictyostatin. Mol Pharmacol. 73:718, 2008.
Jung, W.-H., Guyenne, S., Riesco-Fagundo, C., Mancuso, J., Nakamura, S., and Curran, D.P., Confirmation of the stereostructure of (+)-Cytostatin by fluorous mixture synthesis of four candidate stereoisomers. Angew Chem Int Ed. 47:1130, 2008
Tonoi, T., Zhang, W., Curran, D.P., and Mikami, K. Fluorous “Racemic” mixture synthesis:
polysaccharide-based chiral columns for simultaneious demix and enantioseparation of racemic fluorous tagged compounds. Chirality. 20:597, 2008.
Billy W. Day, Ph.D.
Gibson, F., Anderson, L., Babnigg, G., Baker, M., Berth, M., Binz, P.-A., Borthwick, A., Phil Cash, P., Day, B.W., Friedman, D.B., Garland, D., Gutstein, H.B., Hoogland, C., Jones, N.A., Jones, A.R., Khan, A., Klose, J., Lamond, A.I., Lemkin, P.F., Lilley, K.S., Minden, J., Morris, N.J., Paton, N.W., Pisano, M.R., Prime, J.E., Rabilloud, T., Stead, D.A., Taylor, C.F., Voshol, H., and Wipat, A. Guidelines for reporting the use of gel electrophoresis in proteomics. Nature Biotechnology. 26:863-864, 2008.
Thomas, C.A., Grant, S.G., Pflug, B.R., Getzenberg, R.H., and Day, B.W. Z-1,1-Dichloro-2-(4-methoxyphenyl)-3-phenylcyclopropane induces concentration-dependent growth inhibition, apoptosis and upregulation of apoptotic genes in TRAMP cells. Urologic Oncology. 25: 378-385, 2008.
Thomas, C.A., Grant, S.G., Pflug, B.R., Getzenberg, R.H., and Day, B.W. Z-1, 1-Dichloro-2-(4-methoxyphenyl)-3-phenylcyclopropane induces concentration-dependent growth inhibition, apoptosis and upregulation of apoptotic genes in TRAMP cells. Urologic Oncology. In Press, 2008.
Wright, C.M., Chovatiya, R.J., Jameson, N.E., Turner, D.M., Zhu, G., Werner, S., Huryn, D.M., Pipas, J.M., Day, B.W., Wipf, P., and Brodsky, J.L. Pyrimidinone-peptoid hybrid molecules with distinct effects on molecular chaperone function and cell proliferation. Bioorganic & Medicinal Chemistry. 16:3291-3301, 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., Day, B.W. Cell-based and biochemical structure-activity analyses of analogues of the microtubule stabilizer dictyostatin. Moler Pharmacol. 73:718-726, 2008.
Balachandran, R., Hopkins, T.D., Thomas, C.A., Wipf, P., Day, B.W. Tubulin-perturbing naphthoquinone spiroketals. Chem Biol & Drug Design. 71:117-124, 2008
Kangani, C.O., Day, B.W., Kelley, D.E. Controlled conversion of phenylacetic acids to
phenylacetonitriles or benzonitriles using bis(2-methoxyethyl)aminosulfur trifluoride. Tetrahedron Letters. 49:914-918, 2008.
Donald B. DeFranco, Ph.D.
Ho Y, Knoch M, Samarasinghe R, Aizenman E, DeFranco DB. (2008) Selective inhibition of MAPK phosphatases by zinc accounts for ERK1/2-dependent oxidative neuronal cell death. Molecular Pharmacology. In Press, 2008.
Gong H, Jarzynka MJ, Cole TJ, Wada T, Lee J-H, Zhai Y, Song W-C, DeFranco DB, Cheng S, Xie W. (2008) Glucocorticoids antagonize estrogens by glucocorticoid receptor-mediated activation of estrogen sulfotransferase. Cancer Research. In Press, 2008.
Reiko Ishima, Ph.D.
Sayer JM, Liu F, Ishima R, Weber IT, Louis JM. Effect of the active-site D25N mutation on the structure, stability and ligand binding of the mature HIV-1 protease. J Biol Chem. 283: 13459-13470, 2008.
Paul A. Johnston, Ph.D.
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.
Paul D. Robbins, Ph.D.
Montecalvo, A., Shufesky, W. J., Beer Stolz, D., Sullivan, M. G., Wang, Z., Divito, S., Papworth, G. D., Watkins, S. C., Robbins, P. D., Laregina, A. T., and Morelli, A. E. Exosomes as a short-range mechanism to spread allopeptides between lymphoid organ dendritic cells to amplify the effector T cell response. J Immunol. 180:3081-90, 2008.
Sun, F., Mi, Z., Condiffe, S. B., Bertrand, C. A., Gong, X., Li, X., Zhang, R., Latouche, J. D. Pilewski, J. M., Robbins, P. D. and Frizzell, R. A. Chaperone displacement from mutant cystic fibrosis transmembrane conductance regulator restores its function in human airway epithelia. FASEB J. 22:3255-63, 2008.
Levicoff, E.A., Kim, J.S., Sobajima, S, Wallach, C.J., Larson, J.W., Robbins, P.D., Xiao, X., Juan, L., Vadala, G., Gilbertson, L. G. and Kang, J.D. Safety assessment of intradiscal gene therapy II: effect of dosing and vector choice. Spine. 33:1509-16, 2008.
Moon, S. H., Nishida, K., Gilbertson, L. G., Lee, H. M., Kim, H., Hall, R. A., Robbins, P. D and Kang, J. D. Biologic response of human intervertebral disc cells to gene therapy cocktail. Spine. 33:1850-5, 2008.
Rehman, K. K., Xiao, X., Trucco, M. and Robbins, P. D. AAV8-mediated gene transfer of interleukin-4 to adenogenous ß cells prevents the onset of diabetes in NOD mice. Mol Ther. 6:1409-16, 2008.
Andreas Vogt, PhD
Vogt, A., McDonald, P.M., Tamewitz, A., Sikorski, R.P., Wipf, P., John J. Skoko, 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. Molecular Cancer Therapeutics 7 (3), 330-340 (2008)
Raccor, B.S., Vogt, A., Sikorski, R.P., 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 analogues of the microtubule stabilizer dictyostatin. Molecular Pharmacology 73 (3), 718-726 (2008)
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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