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Items: 44


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 Dec;371(3):652-662. doi: 10.1124/jpet.119.262188. Epub 2019 Oct 10.


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. Review.


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.


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.


Optimization and Evaluation of Antiparasitic Benzamidobenzoic Acids as Inhibitors of Kinetoplastid Hexokinase 1.

Flaherty DP, Harris MT, Schroeder CE, Khan H, Kahney EW, Hackler AL, Patrick SL, Weiner WS, Aubé J, Sharlow ER, Morris JC, Golden JE.

ChemMedChem. 2017 Dec 7;12(23):1994-2005. doi: 10.1002/cmdc.201700592. Epub 2017 Nov 16.


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]


Antiparasitic lethality of sulfonamidebenzamides in kinetoplastids.

Hackler A, Patrick SL, Kahney EW, Flaherty DP, Sharlow ER, Morris JC, Golden JE.

Bioorg Med Chem Lett. 2017 Feb 15;27(4):755-758. doi: 10.1016/j.bmcl.2017.01.043. Epub 2017 Jan 16.


Revisiting Repurposing.

Sharlow ER.

Assay Drug Dev Technol. 2016 Dec;14(10):554-556. Review.


Identification of Novel Plasmodium falciparum Hexokinase Inhibitors with Antiparasitic Activity.

Davis MI, Patrick SL, Blanding WM, Dwivedi V, Suryadi J, Golden JE, Coussens NP, Lee OW, Shen M, Boxer MB, Hall MD, Sharlow ER, Drew ME, Morris JC.

Antimicrob Agents Chemother. 2016 Sep 23;60(10):6023-33. doi: 10.1128/AAC.00914-16. Print 2016 Oct.


Benefits of Strategic Small-Scale Targeted Screening.

Sharlow ER.

Assay Drug Dev Technol. 2016 Aug;14(6):329-32. doi: 10.1089/adt.2016.734. Epub 2016 Jun 24. Review.


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.


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.


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.


Synergistic apoptosis in head and neck squamous cell carcinoma cells by co-inhibition of insulin-like growth factor-1 receptor signaling and compensatory signaling pathways.

Axelrod MJ, Mendez RE, Khalil A, Leimgruber SS, Sharlow ER, Capaldo B, Conaway M, Gioeli DG, Weber MJ, Jameson MJ.

Head Neck. 2015 Dec;37(12):1722-32. doi: 10.1002/hed.23822. Epub 2015 Apr 6.


p70S6 kinase is a critical node that integrates HER-family and PI3 kinase signaling networks.

Axelrod MJ, Gordon V, Mendez RE, Leimgruber SS, Conaway MR, Sharlow ER, Jameson MJ, Gioeli DG, Weber MJ.

Cell Signal. 2014 Aug;26(8):1627-35. doi: 10.1016/j.cellsig.2014.03.013. Epub 2014 Mar 21.


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.


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.


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.


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.


In vitro cytotoxicity, pharmacokinetics, tissue distribution, and metabolism of small-molecule protein kinase D inhibitors, kb-NB142-70 and kb-NB165-09, in mice bearing human cancer xenografts.

Guo J, Clausen DM, Beumer JH, Parise RA, Egorin MJ, Bravo-Altamirano K, Wipf P, Sharlow ER, Wang QJ, Eiseman JL.

Cancer Chemother Pharmacol. 2013 Feb;71(2):331-44. doi: 10.1007/s00280-012-2010-z. Epub 2012 Oct 30.


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.


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.


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.


Protein kinase D as a potential new target for cancer therapy.

LaValle CR, George KM, Sharlow ER, Lazo JS, Wipf P, Wang QJ.

Biochim Biophys Acta. 2010 Dec;1806(2):183-92. doi: 10.1016/j.bbcan.2010.05.003. Epub 2010 May 24. Review.


Chemical genetics of Plasmodium falciparum.

Guiguemde WA, Shelat AA, Bouck D, Duffy S, Crowther GJ, Davis PH, Smithson DC, Connelly M, Clark J, Zhu F, Jiménez-Díaz MB, Martinez MS, Wilson EB, Tripathi AK, Gut J, Sharlow ER, Bathurst I, El Mazouni F, Fowble JW, Forquer I, McGinley PL, Castro S, Angulo-Barturen I, Ferrer S, Rosenthal PJ, Derisi JL, Sullivan DJ, Lazo JS, Roos DS, Riscoe MK, Phillips MA, Rathod PK, Van Voorhis WC, Avery VM, Guy RK.

Nature. 2010 May 20;465(7296):311-5. doi: 10.1038/nature09099.


A target-based high throughput screen yields Trypanosoma brucei hexokinase small molecule inhibitors with antiparasitic activity.

Sharlow ER, Lyda TA, Dodson HC, Mustata G, Morris MT, Leimgruber SS, Lee KH, Kashiwada Y, Close D, Lazo JS, Morris JC.

PLoS Negl Trop Dis. 2010 Apr 13;4(4):e659. doi: 10.1371/journal.pntd.0000659.


Anti-leishmanial drug discovery: rising to the challenges of a highly neglected disease.

Sharlow ER, Grögl M, Johnson J, Lazo JS.

Mol Interv. 2010 Apr;10(2):72-5. doi: 10.1124/mi.10.2.4. Review. No abstract available.


Identification of potent chemotypes targeting Leishmania major using a high-throughput, low-stringency, computationally enhanced, small molecule screen.

Sharlow ER, Close D, Shun T, Leimgruber S, Reed R, Mustata G, Wipf P, Johnson J, O'Neil M, Grögl M, Magill AJ, Lazo JS.

PLoS Negl Trop Dis. 2009 Nov 3;3(11):e540. doi: 10.1371/journal.pntd.0000540.


Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone.

Sharlow ER, Giridhar KV, LaValle CR, Chen J, Leimgruber S, Barrett R, Bravo-Altamirano K, Wipf P, Lazo JS, Wang QJ.

J Biol Chem. 2008 Nov 28;283(48):33516-26. doi: 10.1074/jbc.M805358200. Epub 2008 Sep 30.


Development, validation and implementation of immobilized metal affinity for phosphochemicals (IMAP)-based high-throughput screening assays for low-molecular-weight compound libraries.

Sharlow ER, Leimgruber S, Yellow-Duke A, Barrett R, Wang QJ, Lazo JS.

Nat Protoc. 2008;3(8):1350-63. doi: 10.1038/nprot.2008.111.


Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L.

Shah PP, Myers MC, Beavers MP, Purvis JE, Jing H, Grieser HJ, Sharlow ER, Napper AD, Huryn DM, Cooperman BS, Smith AB 3rd, Diamond SL.

Mol Pharmacol. 2008 Jul;74(1):34-41. doi: 10.1124/mol.108.046219. Epub 2008 Apr 10.


Development and implementation of a miniaturized high-throughput time-resolved fluorescence energy transfer assay to identify small molecule inhibitors of polo-like kinase 1.

Sharlow ER, Leimgruber S, Shun TY, Lazo JS.

Assay Drug Dev Technol. 2007 Dec;5(6):723-35. doi: 10.1089/adt.2007.102.


A Phase I pharmacokinetic and pharmacodynamic study of PX-12, a novel inhibitor of thioredoxin-1, in patients with advanced solid tumors.

Ramanathan RK, Kirkpatrick DL, Belani CP, Friedland D, Green SB, Chow HH, Cordova CA, Stratton SP, Sharlow ER, Baker A, Dragovich T.

Clin Cancer Res. 2007 Apr 1;13(7):2109-14.


The protease-activated receptor-2 upregulates keratinocyte phagocytosis.

Sharlow ER, Paine CS, Babiarz L, Eisinger M, Shapiro S, Seiberg M.

J Cell Sci. 2000 Sep;113 ( Pt 17):3093-101.


Hematopoietic cell phosphatase negatively regulates erythropoietin-induced hemoglobinization in erythroleukemic SKT6 cells.

Sharlow ER, Pacifici R, Crouse J, Batac J, Todokoro K, Wojchowski DM.

Blood. 1997 Sep 15;90(6):2175-87.


Epo-induced hemoglobinization of SKT6 cells is mediated by minimal cytoplasmic domains of the Epo or prolactin receptors without modulation of GATA-1 or EKLF.

Reese TT, Gregory RC, Sharlow ER, Pacifici RE, Crouse JA, Todokoro K, Wojchowski DM.

Growth Factors. 1997;14(2-3):161-76.


Human T-lymphotropic virus type I infection in the Solomon Islands.

Yanagihara R, Ajdukiewicz AB, Garruto RM, Sharlow ER, Wu XY, Alemaena O, Sale H, Alexander SS, Gajudusek DC.

Am J Trop Med Hyg. 1991 Feb;44(2):122-30.


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