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Next-Generation Cell-active Inhibitors of the Undrugged Oncogenic PTP4A3 Phosphatase.

Lazo JS, Blanco IK, Tasker NR, Rastelli EJ, Burnett JC, Garrott SR, Hart DJ, McCloud RL, Hsu KL, Wipf P, Sharlow ER.

J Pharmacol Exp Ther. 2019 Oct 10. pii: jpet.119.262188. doi: 10.1124/jpet.119.262188. [Epub ahead of print]


Tapping the therapeutic potential of protein tyrosine phosphatase 4A with small molecule inhibitors.

Tasker NR, Rastelli EJ, Burnett JC, Sharlow ER, Lazo JS, Wipf P.

Bioorg Med Chem Lett. 2019 Aug 15;29(16):2008-2015. doi: 10.1016/j.bmcl.2019.06.048. Epub 2019 Jun 27. Review.


The Promise and Perils of Compound Discovery Screening with Inducible Pluripotent Cell-Derived Neurons.

Sharlow ER, Koseoglu MM, Bloom GS, Lazo JS.

Assay Drug Dev Technol. 2019 May 16. doi: 10.1089/adt.2019.914. [Epub ahead of print]


In-flow photooxygenation of aminothienopyridinones generates iminopyridinedione PTP4A3 phosphatase inhibitors.

Tasker NR, Rastelli EJ, Blanco IK, Burnett JC, Sharlow ER, Lazo JS, Wipf P.

Org Biomol Chem. 2019 Feb 27;17(9):2448-2466. doi: 10.1039/c9ob00025a.


Aberrant Neuronal Cell Cycle Re-Entry: The Pathological Confluence of Alzheimer's Disease and Brain Insulin Resistance, and Its Relation to Cancer.

Koseoglu MM, Norambuena A, Sharlow ER, Lazo JS, Bloom GS.

J Alzheimers Dis. 2019;67(1):1-11. doi: 10.3233/JAD-180874.


A chemical genetics approach identifies PTP4A3 as a regulator of colon cancer cell adhesion.

McQueeney KE, Salamoun JM, Ahn JG, Pekic P, Blanco IK, Struckman HL, Sharlow ER, Wipf P, Lazo JS.

FASEB J. 2018 Oct;32(10):5661-5673. doi: 10.1096/fj.201701446R. Epub 2018 May 10.


Cutting down the time to identify challenging tumor therapeutic targets and drug combinations using synthetic lethal approaches.

Lazo JS.

F1000Res. 2018 Mar 12;7:308. doi: 10.12688/f1000research.13679.1. eCollection 2018. Review.


Targeting ovarian cancer and endothelium with an allosteric PTP4A3 phosphatase inhibitor.

McQueeney KE, Salamoun JM, Burnett JC, Barabutis N, Pekic P, Lewandowski SL, Llaneza DC, Cornelison R, Bai Y, Zhang ZY, Catravas JD, Landen CN, Wipf P, Lazo JS, Sharlow ER.

Oncotarget. 2017 Dec 30;9(9):8223-8240. doi: 10.18632/oncotarget.23787. eCollection 2018 Feb 2.


Refining Radiation for the Next Century.

Lazo JS.

Mol Cancer Ther. 2018 Feb;17(2):332-335. doi: 10.1158/1535-7163.MCT-17-1244. No abstract available.


High Content Imaging Assays for IL-6-Induced STAT3 Pathway Activation in Head and Neck Cancer Cell Lines.

Johnston PA, Sen M, Hua Y, Camarco DP, Shun TY, Lazo JS, Grandis JR.

Methods Mol Biol. 2018;1683:229-244. doi: 10.1007/978-1-4939-7357-6_14. Erratum in: Methods Mol Biol. 2018;1683:E1.


Reduced brain insulin signaling: A seminal process in Alzheimer's disease pathogenesis.

Bloom GS, Lazo JS, Norambuena A.

Neuropharmacology. 2018 Jul 1;136(Pt B):192-195. doi: 10.1016/j.neuropharm.2017.09.016. Epub 2017 Sep 29. Review.


Small molecule targeting of PTPs in cancer.

Lazo JS, McQueeney KE, Burnett JC, Wipf P, Sharlow ER.

Int J Biochem Cell Biol. 2018 Mar;96:171-181. doi: 10.1016/j.biocel.2017.09.011. Epub 2017 Sep 21. Review.


New Approaches to Difficult Drug Targets: The Phosphatase Story.

Lazo JS, McQueeney KE, Sharlow ER.

SLAS Discov. 2017 Jul 1:2472555217721142. doi: 10.1177/2472555217721142. [Epub ahead of print]


Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors.

LaPorte MG, Wang Z, Colombo R, Garzan A, Peshkov VA, Liang M, Johnston PA, Schurdak ME, Sen M, Camarco DP, Hua Y, Pollock NI, Lazo JS, Grandis JR, Wipf P, Huryn DM.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3581-5. doi: 10.1016/j.bmcl.2016.06.017. Epub 2016 Jun 9.


Photooxygenation of an amino-thienopyridone yields a more potent PTP4A3 inhibitor.

Salamoun JM, McQueeney KE, Patil K, Geib SJ, Sharlow ER, Lazo JS, Wipf P.

Org Biomol Chem. 2016 Jul 6;14(27):6398-402. doi: 10.1039/c6ob00946h.


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.

Johnston PA, Nguyen MM, Dar JA, Ai J, Wang Y, Masoodi KZ, Shun T, Shinde S, Camarco DP, Hua Y, Huryn DM, Wilson GM, Lazo JS, Nelson JB, Wipf P, Wang Z.

Assay Drug Dev Technol. 2016 May;14(4):226-39. doi: 10.1089/adt.2016.716.


A Small Molecule Screen Exposes mTOR Signaling Pathway Involvement in Radiation-Induced Apoptosis.

Sharlow ER, Leimgruber S, Lira A, McConnell MJ, Norambuena A, Bloom GS, Epperly MW, Greenberger JS, Lazo JS.

ACS Chem Biol. 2016 May 20;11(5):1428-37. doi: 10.1021/acschembio.5b00909. Epub 2016 Mar 14.


Drugging Undruggable Molecular Cancer Targets.

Lazo JS, Sharlow ER.

Annu Rev Pharmacol Toxicol. 2016;56:23-40. doi: 10.1146/annurev-pharmtox-010715-103440. Epub 2015 Nov 2. Review.


Direct inhibition of c-Myc-Max heterodimers by celastrol and celastrol-inspired triterpenoids.

Wang H, Teriete P, Hu A, Raveendra-Panickar D, Pendelton K, Lazo JS, Eiseman J, Holien T, Misund K, Oliynyk G, Arsenian-Henriksson M, Cosford ND, Sundan A, Prochownik EV.

Oncotarget. 2015 Oct 20;6(32):32380-95. doi: 10.18632/oncotarget.6116.


HCS campaign to identify selective inhibitors of IL-6-induced STAT3 pathway activation in head and neck cancer cell lines.

Johnston PA, Sen M, Hua Y, Camarco DP, Shun TY, Lazo JS, Wilson GM, Resnick LO, LaPorte MG, Wipf P, Huryn DM, Grandis JR.

Assay Drug Dev Technol. 2015 Sep;13(7):356-76. doi: 10.1089/adt.2015.663.


Synthesis and biological evaluation of 3-aminoisoquinolin-1(2H)-one based inhibitors of the dual-specificity phosphatase Cdc25B.

George Rosenker KM, Paquette WD, Johnston PA, Sharlow ER, Vogt A, Bakan A, Lazo JS, Wipf P.

Bioorg Med Chem. 2015 Jun 15;23(12):2810-8. doi: 10.1016/j.bmc.2015.01.043. Epub 2015 Jan 31.


2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway.

LaPorte MG, da Paz Lima DJ, Zhang F, Sen M, Grandis JR, Camarco D, Hua Y, Johnston PA, Lazo JS, Resnick LO, Wipf P, Huryn DM.

Bioorg Med Chem Lett. 2014 Nov 1;24(21):5081-5. doi: 10.1016/j.bmcl.2014.09.001. Epub 2014 Sep 15.


Deletion of Ptp4a3 reduces clonogenicity and tumor-initiation ability of colitis-associated cancer cells in mice.

Cramer JM, Zimmerman MW, Thompson T, Homanics GE, Lazo JS, Lagasse E.

Stem Cell Res. 2014 Jul;13(1):164-171. doi: 10.1016/j.scr.2014.05.004. Epub 2014 May 27.


Investigational inhibitors of PTP4A3 phosphatase as antineoplastic agents.

Sharlow ER, Wipf P, McQueeney KE, Bakan A, Lazo JS.

Expert Opin Investig Drugs. 2014 May;23(5):661-73. doi: 10.1517/13543784.2014.892579. Epub 2014 Mar 13. Review.


Protein-tyrosine phosphatase 4A3 (PTP4A3) promotes vascular endothelial growth factor signaling and enables endothelial cell motility.

Zimmerman MW, McQueeney KE, Isenberg JS, Pitt BR, Wasserloos KA, Homanics GE, Lazo JS.

J Biol Chem. 2014 Feb 28;289(9):5904-13. doi: 10.1074/jbc.M113.480038. Epub 2014 Jan 8.


Auranofin is an apoptosis-simulating agent with in vitro and in vivo anti-leishmanial activity.

Sharlow ER, Leimgruber S, Murray S, Lira A, Sciotti RJ, Hickman M, Hudson T, Leed S, Caridha D, Barrios AM, Close D, Grögl M, Lazo JS.

ACS Chem Biol. 2014 Mar 21;9(3):663-72. doi: 10.1021/cb400800q. Epub 2013 Dec 23.


High-content pSTAT3/1 imaging assays to screen for selective inhibitors of STAT3 pathway activation in head and neck cancer cell lines.

Johnston PA, Sen M, Hua Y, Camarco D, Shun TY, Lazo JS, Grandis JR.

Assay Drug Dev Technol. 2014 Jan-Feb;12(1):55-79. doi: 10.1089/adt.2013.524. Epub 2013 Oct 15.


Pharmacologic profiling of phosphoinositide 3-kinase inhibitors as mitigators of ionizing radiation-induced cell death.

Lazo JS, Sharlow ER, Epperly MW, Lira A, Leimgruber S, Skoda EM, Wipf P, Greenberger JS.

J Pharmacol Exp Ther. 2013 Dec;347(3):669-80. doi: 10.1124/jpet.113.208421. Epub 2013 Sep 25.


Evaluation of potential ionizing irradiation protectors and mitigators using clonogenic survival of human umbilical cord blood hematopoietic progenitor cells.

Goff JP, Shields DS, Wang H, Skoda EM, Sprachman MM, Wipf P, Garapati VK, Atkinson J, London B, Lazo JS, Kagan V, Epperly MW, Greenberger JS.

Exp Hematol. 2013 Nov;41(11):957-66. doi: 10.1016/j.exphem.2013.08.001. Epub 2013 Aug 7.


Targeted deletion of the metastasis-associated phosphatase Ptp4a3 (PRL-3) suppresses murine colon cancer.

Zimmerman MW, Homanics GE, Lazo JS.

PLoS One. 2013;8(3):e58300. doi: 10.1371/journal.pone.0058300. Epub 2013 Mar 28.


Drug discovery algorithm for cutaneous leishmaniasis.

Grogl M, Hickman M, Ellis W, Hudson T, Lazo JS, Sharlow ER, Johnson J, Berman J, Sciotti RJ.

Am J Trop Med Hyg. 2013 Feb;88(2):216-21. doi: 10.4269/ajtmh.11-0812. Review.


Effector kinase coupling enables high-throughput screens for direct HIV-1 Nef antagonists with antiretroviral activity.

Emert-Sedlak LA, Narute P, Shu ST, Poe JA, Shi H, Yanamala N, Alvarado JJ, Lazo JS, Yeh JI, Johnston PA, Smithgall TE.

Chem Biol. 2013 Jan 24;20(1):82-91. doi: 10.1016/j.chembiol.2012.11.005.


Alkylation sensitivity screens reveal a conserved cross-species functionome.

Svilar D, Dyavaiah M, Brown AR, Tang JB, Li J, McDonald PR, Shun TY, Braganza A, Wang XH, Maniar S, St Croix CM, Lazo JS, Pollack IF, Begley TJ, Sobol RW.

Mol Cancer Res. 2012 Dec;10(12):1580-96. doi: 10.1158/1541-7786.MCR-12-0168. Epub 2012 Oct 4.


Phenotypic screening reveals topoisomerase I as a breast cancer stem cell therapeutic target.

Zhang F, Rothermund K, Gangadharan SB, Pommier Y, Prochownik EV, Lazo JS.

Oncotarget. 2012 Sep;3(9):998-1010.


Targeting subcellular localization through the polo-box domain: non-ATP competitive inhibitors recapitulate a PLK1 phenotype.

McInnes C, Estes K, Baxter M, Yang Z, Farag DB, Johnston P, Lazo JS, Wang J, Wyatt MD.

Mol Cancer Ther. 2012 Aug;11(8):1683-92. doi: 10.1158/1535-7163.MCT-12-0006-T. Epub 2012 Jul 30.


Development and validation of a high-content screening assay to identify inhibitors of cytoplasmic dynein-mediated transport of glucocorticoid receptor to the nucleus.

Johnston PA, Shinde SN, Hua Y, Shun TY, Lazo JS, Day BW.

Assay Drug Dev Technol. 2012 Oct;10(5):432-56. doi: 10.1089/adt.2012.456. Epub 2012 Jul 25.


Identification of druggable targets for radiation mitigation using a small interfering RNA screening assay.

Zellefrow CD, Sharlow ER, Epperly MW, Reese CE, Shun T, Lira A, Greenberger JS, Lazo JS.

Radiat Res. 2012 Sep;178(3):150-9. Epub 2012 Jul 2.


Design, Synthesis, and Biological Evaluation of PKD Inhibitors.

George KM, Frantz MC, Bravo-Altamirano K, Lavalle CR, Tandon M, Leimgruber S, Sharlow ER, Lazo JS, Wang QJ, Wipf P.

Pharmaceutics. 2011;3(2):186-228. doi: 10.3390/pharmaceutics3020186.


Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity.

Sharlow ER, Mustata Wilson G, Close D, Leimgruber S, Tandon M, Reed RB, Shun TY, Wang QJ, Wipf P, Lazo JS.

PLoS One. 2011;6(10):e25134. doi: 10.1371/journal.pone.0025134. Epub 2011 Oct 5.


Identification of Inhibitors of Trypanosoma brucei Hexokinases.

Sharlow E, Golden JE, Dodson H, Morris M, Hesser M, Lyda T, Leimgruber S, Schroeder CE, Flaherty DP, Weiner WS, Simpson D, Lazo JS, Aubé J, Morris JC.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Dec 15 [updated 2011 Jun 24].


Identification of chemosensitivity nodes for vinblastine through small interfering RNA high-throughput screens.

Kitchens CA, McDonald PR, Shun TY, Pollack IF, Lazo JS.

J Pharmacol Exp Ther. 2011 Dec;339(3):851-8. doi: 10.1124/jpet.111.184879. Epub 2011 Aug 31.


Metastasis-associated phosphatase PRL-2 regulates tumor cell migration and invasion.

Wang Y, Lazo JS.

Oncogene. 2012 Feb 16;31(7):818-27. doi: 10.1038/onc.2011.281. Epub 2011 Jul 18.


Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.

Bravo-Altamirano K, George KM, Frantz MC, Lavalle CR, Tandon M, Leimgruber S, Sharlow ER, Lazo JS, Wang QJ, Wipf P.

ACS Med Chem Lett. 2011 Feb 14;2(2):154-159.


Molecular interventions (2001-2011): an experiment completed.

Lazo JS.

Mol Interv. 2011 Apr;11(2):62. doi: 10.1124/mi.11.2.0. No abstract available.


Mutagenesis and computer modeling studies of a GPCR conserved residue W5.43(194) in ligand recognition and signal transduction for CB2 receptor.

Zhang Y, Xie Z, Wang L, Schreiter B, Lazo JS, Gertsch J, Xie XQ.

Int Immunopharmacol. 2011 Sep;11(9):1303-10. doi: 10.1016/j.intimp.2011.04.013. Epub 2011 May 1.


A simplified synthesis of novel dictyostatin analogues with in vitro activity against epothilone B-resistant cells and antiangiogenic activity in zebrafish embryos.

Vollmer LL, Jiménez M, Camarco DP, Zhu W, Daghestani HN, Balachandran R, Reese CE, Lazo JS, Hukriede NA, Curran DP, Day BW, Vogt A.

Mol Cancer Ther. 2011 Jun;10(6):994-1006. doi: 10.1158/1535-7163.MCT-10-1048. Epub 2011 Apr 13.


Compound acquisition and prioritization algorithm for constructing structurally diverse compound libraries.

Ma C, Lazo JS, Xie XQ.

ACS Comb Sci. 2011 May 9;13(3):223-31. doi: 10.1021/co100033m. Epub 2011 Apr 18.


Strategies for discovery of small molecule radiation protectors and radiation mitigators.

Greenberger JS, Clump D, Kagan V, Bayir H, Lazo JS, Wipf P, Li S, Gao X, Epperly MW.

Front Oncol. 2012 Jan 13;1:59. doi: 10.3389/fonc.2011.00059. eCollection 2011.


Identifying actives from HTS data sets: practical approaches for the selection of an appropriate HTS data-processing method and quality control review.

Shun TY, Lazo JS, Sharlow ER, Johnston PA.

J Biomol Screen. 2011 Jan;16(1):1-14. doi: 10.1177/1087057110389039. Epub 2010 Dec 15.


Automated high-content live animal drug screening using C. elegans expressing the aggregation prone serpin α1-antitrypsin Z.

Gosai SJ, Kwak JH, Luke CJ, Long OS, King DE, Kovatch KJ, Johnston PA, Shun TY, Lazo JS, Perlmutter DH, Silverman GA, Pak SC.

PLoS One. 2010 Nov 12;5(11):e15460. doi: 10.1371/journal.pone.0015460.

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