The Fiske Drug Discovery lab works closely with The Virginia Center for Translational and Regulatory Sciences
George Bloom
David Brautigan
James Larner
Peter Wipf
Publications
Sharlow, E.R., Koseoglu, M.M., Bloom, G.S.,and Lazo, J.S. The promise and perils of compound discovery screening with inducible pluripotent cell-derived neurons. Assay Drug Dev Technol. 18:97-103, 2020.
Porterfield, V., Khan, S., Foff, E., Koseoglu, M.M., Blanco, I.K., Jayaraman, S. Lien, E., McConnell, M.J., Bloom, G.S., Lazo, J.S., and Sharlow, E.R. A three-dimensional dementia model reveals spontaneous cell cycle reentry and a senescence-associated secretory phenotype. Neurobiol Aging. 90:125-134, 2020.
Aguilar-Sopeña, O., Hernández-Pérez, S., Alegre-Gómez, S., Castro-Sánchez, P., Iglesias-Ceacero, A., Lazo, J.S., and Roda-Navarro, P. Effect of pharmacological inhibition of the catalytic activity of phosphatases of regenerating liver in early T cell receptor signaling dynamics and IL-2 production. Int J Mol Sci. 5:21, 2020.
Tasker, N.R., Rastelli, E.J., Blanco, I.K., Burnett, J.C., Sharlow, E.R.,Lazo, J.S., and Wipf, P. In-flow photooxygenation of aminothienopyridinones generates iminopyridinedione PTP4A3 phosphatase inhibitors. Org Biomol Chem. 17:2448-2466, 2019.
Koseoglu, M.M., Norambuena, A., Sharlow, E.R.,Lazo, J.S., and Bloom, G.S. Aberrant neuronal cell cycle re-entry: The pathological confluence of Alzheimer’s Disease and brain insulin resistance, and Its relation to cancer. J Alzheimer’s Dis. 67:1-11, 2019.
Lazo, J.S., Blanco, I.K., Tasker, N.R., Rastelli, E.J., Burnett, J.C., Garrott, S.R., Hart, D.J., McCloud, R.L., Hsu, K.-L., Wipf, P. and Sharlow, E.R. Next-generation cell-active inhibitors of the undrugged oncogenic PTP4A3 phosphatase. J Pharmacol Exptl Therap. 371:652-662, 2019.
Sharlow, E.R., Koseoglu, M.M., Bloom, G.S.,and Lazo, J.S. The promise and perils of compound discovery screening with inducible pluripotent cell-derived neurons. Assay Drug Dev Technol. In Press. doi: 10.1089/adt.2019.914.
Lazo, J.S. and Lau, A.F. What snaps your socks – A tribute to Dr. Raymond (Ray) W. Ruddon. The Pharmacologist. 61:184, 2019.
Lazo, J.S. The hubris and humility of cancer pharmacology in the post-immuno-oncology era. Pharmacol Res Perspec. 7:e00527, 2019
McQueeney, K.E., Salamoun, J.E., Anh, J., Pekic, P., Blanco, I.K., Struckman, H., Sharlow, E.R., Wipf, P., and Lazo, J.S. PTP4A3 phosphatase regulates colorectal cancer cell migration, adhesion and Emilin 1 gene expression. FASEB J. 32: 5661-5673, 2018.
Johnston, P.A., Sen, M., Hua, Y., Camarco, D.P., Shun, T.Y., Lazo, J.S., and Grandis, J.R. High content imaging assays for IL-6-induced STAT3 pathway activation in Head and Neck cancer cell lines. Methods Mol Biol.1683:229-244, 2018.
Lazo, J.S. Refining radiation in the next century. Mol Cancer Therap. 17:332-335, 2018.
Lazo, J.S. Cutting down the time to identify challenging tumor therapeutic targets and drug combinations using synthetic lethal approaches. F1000Res. 7:308, 2018
McQueeney, K.E., Salamoun, J.M., Burnett, J.C., Barabutis, N., Pekic, P., Lewandowski, S.L., Llaneza, D.C., Cornelison, R., Bai, Y., Zhang, Z.-Y., Catravas, J.D., Landen Jr., C.N., Wipf, P., Lazo, J.S., and Sharlow, E.R. Targeting ovarian cancer and endothelium with an allosteric PTP4A3 phosphatase inhibitor. Oncotarget. 9:8223-8240.
Lazo, J.S., McQueeney, K.E. and Sharlow, E.R. New approaches to difficult drug targets: The phosphatase story. SLAS Discovery, 2472555217721142, 2017.
Bloom, G., Lazo, J.S. and Norambuena, A. Reduced brain insulin signaling: a seminal process in Alzheimer’s disease pathogenesis. Neuropharmacology. S0028-3908:30433-1, 2017.
Lazo, J.S., McQueeney, K.E., Birnett, J.C., Wipf, P., and Sharlow, E.R. Small targeting of PTPs in cancer. Int J Biochem Cell Biol S1357-2725:30237-6, 2017
Sharlow, E.R., Leimgruber, S., Lira, A., McConnell, M.J., Norambuena, A., Bloom, G.S., Epperly, M.W., Greenberger, J.S., and Lazo, J.S. A small molecule screen exposes mTOR signaling pathway involvement in radiation-induced apoptosis. ACS Chem Biol. 11:1428-1437, 2016.
Johnston, P.A., Nguyen, M.M., Dar, J.A., Ai, J., Wang, Y., Masoodi, K.Z., Shun, T., Shinde, S., Camarco, D.P., Hua, Y., Huryn, D.M., Wilson, G.M., Lazo, J.S., Nelson, J.B., Wipf, P., and Wang Z. Development and implementation of a high-throughput high-content screening assay to identify inhibitors of androgen receptor nuclear localization in castration-resistant prostate cancer cells. Assay Drug Dev Technol. 14:226-239, 2016.
Salamoun, J.M., McQueeney, K.E., Patil, K., Geib, S.J., Sharlow, E.R., Lazo, J.S., and Wipf, P. Photooxygenation of an amino-thienopyridone yields a more potent PTP4A3 inhibitor. Org Biomol Chem. 14:6398-6402, 2016.
LaPorte, M.G., Wang, Z., Colombo, R., Garzan, A., Peshkov, V.A., Liang, M., Johnston, P.A., Schurdak, M.E., Sen, M., Camarco, D.P., Hua, Y., Pollock, N.I., Lazo, J.S., Grandis, J.R., Wipf, P., and Huryn, D.M. Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors. Bioorg Med Chem Lett. 26: 3581-3585. 2016.
Lazo, J.S. and Sharlow, E.R. Drugging Undruggable Molecular Cancer Targets. Annu Rev Pharmacol Toxicol. 56: 23-40, 2016
George Rosenker, K.M., Paquette, W.D., Johnston, P.A., Sharlow, E.R., Vogt, A., Bakan, A., Lazo, J.S., and Wipf, P. Synthesis and biological evaluation of 3-aminoisoquinolin-1(2H)-one based inhibitors of the dual-specificity phosphatase Cdc25B. Bioorg Med Chem. 23:2810-2818, 2015.
Johnston, P.A., Sen, M., Hua, Y., Camarco, D.P., Shun, T.Y., Lazo, J.S., Wilson, G.M., Resnick, L.O., LaPorte, M.G., Wipf, P., Huryn, D.M., and Grandis, J.R. HCS campaign to identify selective inhibitors of IL-6-induced STAT3 pathway activation in head and neck cancer cell lines. Assay Drug Dev Technol. 13:356-376, 2015.
Wang, H., Teriete, P., Hu, A., Raveendra-Panickar, D., Pendelton, K., Lazo, J.S., Eiseman, J., Holien, T., Misund, K., Oliynyk, G., Arsenian-Henriksson, M., Cosford, N.D., Sundan, A., and Prochownik, E.V. Direct inhibition of c-Myc-Max heterodimers by celastrol and celastrol-inspired triterpenoids. Oncotarget. 6:32380-32395, 2015.
Grogl, M., Hickman, M., Ellis, W., Hudson, T., Lazo, J.S., Sharlow, E.R., Johnson, J., Berman, J., Sciotti, R.J. Drug discovery algorithm for cutaneous leishmaniasis. Am J Trop Med Hyg. 88:216-221, 2013.
Lazo, J.S. President’s Corner: Comings and Goings. The Pharmacologist. 55:3, 2013.
International collaboration, a vital component of scientific progress. Pharmacology Matters. 6:5, 2013.
Zellefrow, C.D., Sharlow, E.R., Epperly, M.W., Reese, C.E., Shun, T., Lira, A., Greenberger, J.S., and Lazo, J.S.. Identification of druggable targets for radiation mitigation using a small interfering RNA screening assay. Radiation Res. 178:150-150, 2012.
McInnes, C., Estes, K., Baxter, M., Yang, Z., Farag, D. B., Johnston, P., Lazo, J.S., Wng. J. and Wyatt, M.D. Targeting subcellular localization through the Polo-Box domain: Non-ATP competitive inhibitors recapitulate a PLK1 phenotype. Mol Cancer Therap. 11:1683-1692, 2012.
Johnston, P.A., Shinde, S.N., Hua, Y, Shun, T. Y., Lazo, J.S., and Day, B.W. Development and validation of a high-content screening assay to identify inhibitors of cytoplasmic dynein-mediated transport of glucocorticoid receptor to the nucleus. Assay Drug Dev Technol. 10:432-456, 2012.
Svilar, D., Dyavaiah, M., Brown, A.R., Tang, J., McDonald, P.R., Shun, T. Y., Wang, X-H., Lazo, J.S., Pollack, I.F., Begley, T.J. and Sobol, R. W. Alkylation sensitivity screens reveal a conserved cross-species functionome. Mol Cancer Res., 11:1683-1692, 2012.
Zhang, F., Rothermund, K, Gangadharan, S.B., Pommier, Y., Prochownik, E.V., and Lazo, J.S. Phenotypic screening reveals topoisomerase I as a breast cancer stem cell therapeutic target. Oncotarget. 3:998-1010, 2012.
Greenberger, J.S., Clump, D., Kagan, V., Bayir, H., Lazo, J.S., Wipf, P. Li, S., Gao, X., and Epperly, M.W. Strategies for discovery of small molecule radiation protectors and radiation mitigators. Frontiers in Oncology. 1:1-12, 2012.
Bravo-Altamirano, K., George, K.M., Frantz, M.C., Lavalle, C.R., Tandon, M., Leimgruber, S., Sharlow, E.R., Lazo, J.S., Wang, Q.J., and Wipf, P. Synthesis and structure-activity relationships of benzothienothiazepinone inhibitors of Protein Kinase D. ACS Med Chem Lett. 2:154-159, 2011.
Zhang, Y., Xie, Z., Wang, L., Schreiter, B., Lazo, J.S., and Gertsch J, and Xie, X.Q. Mutagenesis and computer modeling studies of a GPCR conserved residue W5.43(194) in ligand recognition and signal transduction for CB2 receptor. Int Immunopharmacol. 11:1303-1310, 2011.
Sharlow, E.R., Mustata Wilson, G., Close, D., Leimgruber, S., Tandon, M., Reed, R.B., Shun, T.Y., Wang, Q.J., Wipf, P., and Lazo, J.S. Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity. PLoS One 6:e25134, 2011.
