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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.


Combination of a thioxodihydroquinazolinone with cisplatin eliminates ovarian cancer stem cell-like cells (CSC-LCs) and shows preclinical potential.

Ma J, Salamoun J, Wipf P, Edwards R, Van Houten B, Qian W.

Oncotarget. 2017 Dec 26;9(5):6042-6054. doi: 10.18632/oncotarget.23679. eCollection 2018 Jan 19.


The GS-nitroxide JP4-039 improves intestinal barrier and stem cell recovery in irradiated mice.

Wei L, Leibowitz BJ, Epperly M, Bi C, Li A, Steinman J, Wipf P, Li S, Zhang L, Greenberger J, Yu J.

Sci Rep. 2018 Feb 1;8(1):2072. doi: 10.1038/s41598-018-20370-9.


Evaluation of mitochondrial bioenergetics, dynamics, endoplasmic reticulum-mitochondria crosstalk, and reactive oxygen species in fibroblasts from patients with complex I deficiency.

Leipnitz G, Mohsen AW, Karunanidhi A, Seminotti B, Roginskaya VY, Markantone DM, Grings M, Mihalik SJ, Wipf P, Van Houten B, Vockley J.

Sci Rep. 2018 Jan 18;8(1):1165. doi: 10.1038/s41598-018-19543-3.


Structure-based virtual screening identifies a small-molecule inhibitor of the profilin 1-actin interaction.

Gau D, Lewis T, McDermott L, Wipf P, Koes D, Roy P.

J Biol Chem. 2018 Feb 16;293(7):2606-2616. doi: 10.1074/jbc.M117.809137. Epub 2017 Dec 27.


New Cav2 calcium channel gating modifiers with agonist activity and therapeutic potential to treat neuromuscular disease.

Wu M, White HV, Boehm BA, Meriney CJ, Kerrigan K, Frasso M, Liang M, Gotway EM, Wilcox MR, Johnson JW, Wipf P, Meriney SD.

Neuropharmacology. 2018 Mar 15;131:176-189. doi: 10.1016/j.neuropharm.2017.12.022. Epub 2017 Dec 12.


Liquid chromatography-tandem mass spectrometric assay for the quantitation of the novel radiation protective agent and radiation mitigator JP4-039 in murine plasma.

Christner S, Guo J, Parise RA, Ringeval M, Hoye AT, Wipf P, Epperly MW, Greenberger JS, Beumer JH, Eiseman JL.

J Pharm Biomed Anal. 2018 Feb 20;150:169-175. doi: 10.1016/j.jpba.2017.12.023. Epub 2017 Dec 12.


Improved Total-Body Irradiation Survival by Delivery of Two Radiation Mitigators that Target Distinct Cell Death Pathways.

Steinman J, Epperly M, Hou W, Willis J, Wang H, Fisher R, Liu B, Bahar I, McCaw T, Kagan V, Bayir H, Yu J, Wipf P, Li S, Huq MS, Greenberger JS.

Radiat Res. 2018 Jan;189(1):68-83. doi: 10.1667/RR14787.1. Epub 2017 Nov 15.


Lambert-Eaton myasthenic syndrome: mouse passive-transfer model illuminates disease pathology and facilitates testing therapeutic leads.

Meriney SD, Tarr TB, Ojala KS, Wu M, Li Y, Lacomis D, Garcia-Ocaña A, Liang M, Valdomir G, Wipf P.

Ann N Y Acad Sci. 2018 Jan;1412(1):73-81. doi: 10.1111/nyas.13512. Epub 2017 Nov 10. Review.


Inhibition of Androgen Receptor Function and Level in Castration-Resistant Prostate Cancer Cells by 2-[(isoxazol-4-ylmethyl)thio]-1-(4-phenylpiperazin-1-yl)ethanone.

Masoodi KZ, Eisermann K, Yang Z, Dar JA, Pascal LE, Nguyen M, O'Malley K, Parrinello E, Feturi FG, Kenefake AN, Nelson JB, Johnston PA, Wipf P, Wang Z.

Endocrinology. 2017 Oct 1;158(10):3152-3161. doi: 10.1210/en.2017-00408.


t-BuOOH induces ferroptosis in human and murine cell lines.

Wenz C, Faust D, Linz B, Turmann C, Nikolova T, Bertin J, Gough P, Wipf P, Schröder AS, Krautwald S, Dietrich C.

Arch Toxicol. 2018 Feb;92(2):759-775. doi: 10.1007/s00204-017-2066-y. Epub 2017 Oct 3.


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.


N-Acetyl-l-Cysteine Protects Astrocytes against Proteotoxicity without Recourse to Glutathione.

Gleixner AM, Hutchison DF, Sannino S, Bhatia TN, Leak LC, Flaherty PT, Wipf P, Brodsky JL, Leak RK.

Mol Pharmacol. 2017 Nov;92(5):564-575. doi: 10.1124/mol.117.109926. Epub 2017 Aug 22.


Indole synthesis by palladium-catalyzed tandem allylic isomerization - furan Diels-Alder reaction.

Xu J, Wipf P.

Org Biomol Chem. 2017 Aug 30;15(34):7093-7096. doi: 10.1039/c7ob01654a.


Mechanism of action of selective inhibitors of IL-6 induced STAT3 pathway in head and neck cancer cell lines.

Sen M, Johnston PA, Pollock NI, DeGrave K, Joyce SC, Freilino ML, Hua Y, Camarco DP, Close DA, Huryn DM, Wipf P, Grandis JR.

J Chem Biol. 2017 May 11;10(3):129-141. doi: 10.1007/s12154-017-0169-9. eCollection 2017 Jul.


Inhibition of Androgen Receptor Nuclear Localization and Castration-Resistant Prostate Tumor Growth by Pyrroloimidazole-based Small Molecules.

Masoodi KZ, Xu Y, Dar JA, Eisermann K, Pascal LE, Parrinello E, Ai J, Johnston PA, Nelson JB, Wipf P, Wang Z.

Mol Cancer Ther. 2017 Oct;16(10):2120-2129. doi: 10.1158/1535-7163.MCT-17-0176. Epub 2017 Jun 27.


Induction of TGF-β by Irradiation or Chemotherapy in Fanconi Anemia (FA) Mouse Bone Marrow Is Modulated by Small Molecule Radiation Mitigators JP4-039 and MMS350.

Epperly MW, Rhieu BH, Franicola D, Dixon T, Cao S, Zhang X, Shields D, Wang H, Wipf P, Greenberger JS.

In Vivo. 2017 Mar-Apr;31(2):159-168.


A threonine turnstile defines a dynamic amphiphilic binding motif in the AAA ATPase p97 allosteric binding site.

Burnett JC, Lim C, Peyser BD, Samankumara LP, Kovaliov M, Colombo R, Bulfer SL, LaPorte MG, Hermone AR, McGrath CF, Arkin MR, Gussio R, Huryn DM, Wipf P.

Org Biomol Chem. 2017 May 16;15(19):4096-4114. doi: 10.1039/c7ob00526a.


A structure-activity relationship study of ABCC2 inhibitors.

Wissel G, Deng F, Kudryavtsev P, Ghemtio L, Wipf P, Xhaard H, Kidron H.

Eur J Pharm Sci. 2017 May 30;103:60-69. doi: 10.1016/j.ejps.2017.02.005. Epub 2017 Feb 7.


ACS Medicinal Chemistry Letters: Technology Notes.

Wipf P.

ACS Med Chem Lett. 2017 Jan 12;8(1):1-2. doi: 10.1021/acsmedchemlett.6b00484. eCollection 2017 Jan 12. No abstract available.


Effectiveness of Analogs of the GS-Nitroxide, JP4-039, as Total Body Irradiation Mitigators.

Epperly MW, Sacher JR, Krainz T, Zhang X, Wipf P, Liang M, Fisher R, Li S, Wang H, Greenberger JS.

In Vivo. 2017 Jan 2;31(1):39-43.


Lipidomics Characterization of Biosynthetic and Remodeling Pathways of Cardiolipins in Genetically and Nutritionally Manipulated Yeast Cells.

Tyurina YY, Lou W, Qu F, Tyurin VA, Mohammadyani D, Liu J, Hüttemann M, Frasso MA, Wipf P, Bayir H, Greenberg ML, Kagan VE.

ACS Chem Biol. 2017 Jan 20;12(1):265-281. doi: 10.1021/acschembio.6b00995. Epub 2016 Dec 16.


Eight-Step Enantioselective Total Synthesis of (-)-Cycloclavine.

McCabe SR, Wipf P.

Angew Chem Int Ed Engl. 2017 Jan 2;56(1):324-327. doi: 10.1002/anie.201608820. Epub 2016 Nov 18.


Total Synthesis and Biological Evaluation of Tubulysin Analogues.

Colombo R, Wang Z, Han J, Balachandran R, Daghestani HN, Camarco DP, Vogt A, Day BW, Mendel D, Wipf P.

J Org Chem. 2016 Nov 4;81(21):10302-10320. Epub 2016 Aug 5.


A Topical Mitochondria-Targeted Redox-Cycling Nitroxide Mitigates Oxidative Stress-Induced Skin Damage.

Brand RM, Epperly MW, Stottlemyer JM, Skoda EM, Gao X, Li S, Huq S, Wipf P, Kagan VE, Greenberger JS, Falo LD Jr.

J Invest Dermatol. 2017 Mar;137(3):576-586. doi: 10.1016/j.jid.2016.09.033. Epub 2016 Oct 26.


A Mitochondrial-Targeted Nitroxide Is a Potent Inhibitor of Ferroptosis.

Krainz T, Gaschler MM, Lim C, Sacher JR, Stockwell BR, Wipf P.

ACS Cent Sci. 2016 Sep 28;2(9):653-659. Epub 2016 Sep 7.


Dihydropyrimidinones and -thiones with improved activity against human polyomavirus family members.

Manos-Turvey A, Al-Ashtal HA, Needham PG, Hartline CB, Prichard MN, Wipf P, Brodsky JL.

Bioorg Med Chem Lett. 2016 Oct 15;26(20):5087-5091. doi: 10.1016/j.bmcl.2016.08.080. Epub 2016 Aug 25.


Elucidating Mitochondrial Electron Transport Chain Supercomplexes in the Heart During Ischemia-Reperfusion.

Jang S, Lewis TS, Powers C, Khuchua Z, Baines CP, Wipf P, Javadov S.

Antioxid Redox Signal. 2017 Jul 1;27(1):57-69. doi: 10.1089/ars.2016.6635. Epub 2016 Nov 11.


Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer.

Johnson JK, Skoda EM, Zhou J, Parrinello E, Wang D, O'Malley K, Eyer BR, Kazancioglu M, Eisermann K, Johnston PA, Nelson JB, Wang Z, Wipf P.

ACS Med Chem Lett. 2016 May 27;7(8):785-90. doi: 10.1021/acsmedchemlett.6b00186. eCollection 2016 Aug 11.


Allosteric Modulation of Phosphatase Activity May Redefine Therapeutic Value.

Salamoun JM, Wipf P.

J Med Chem. 2016 Sep 8;59(17):7771-2. doi: 10.1021/acs.jmedchem.6b01210. Epub 2016 Aug 19.


Hydrophosphination of Bicyclo[1.1.0]butane-1-carbonitriles.

Milligan JA, Busacca CA, Senanayake CH, Wipf P.

Org Lett. 2016 Sep 2;18(17):4300-3. doi: 10.1021/acs.orglett.6b02051. Epub 2016 Aug 12.


Combined chemical-genetic approach identifies cytosolic HSP70 dependence in rhabdomyosarcoma.

Sabnis AJ, Guerriero CJ, Olivas V, Sayana A, Shue J, Flanagan J, Asthana S, Paton AW, Paton JC, Gestwicki JE, Walter P, Weissman JS, Wipf P, Brodsky JL, Bivona TG.

Proc Natl Acad Sci U S A. 2016 Aug 9;113(32):9015-20. doi: 10.1073/pnas.1603883113. Epub 2016 Jul 22.


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.


Total synthesis, biosynthesis and biological profiles of clavine alkaloids.

McCabe SR, Wipf P.

Org Biomol Chem. 2016 Jul 7;14(25):5894-913. doi: 10.1039/c6ob00878j. Epub 2016 May 24. Review.


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.


Synthesis and Evaluation of Potent KCNQ2/3-Specific Channel Activators.

Kumar M, Reed N, Liu R, Aizenman E, Wipf P, Tzounopoulos T.

Mol Pharmacol. 2016 Jun;89(6):667-77. doi: 10.1124/mol.115.103200. Epub 2016 Mar 22.


Click chemistry: Straining to react.

Milligan JA, Wipf P.

Nat Chem. 2016 Apr;8(4):296-7. doi: 10.1038/nchem.2485. No abstract available.


Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway.

Alverez C, Bulfer SL, Chakrasali R, Chimenti MS, Deshaies RJ, Green N, Kelly M, LaPorte MG, Lewis TS, Liang M, Moore WJ, Neitz RJ, Peshkov VA, Walters MA, Zhang F, Arkin MR, Wipf P, Huryn DM.

ACS Med Chem Lett. 2015 Dec 22;7(2):182-7. doi: 10.1021/acsmedchemlett.5b00396. eCollection 2016 Feb 11.


Mitochondrial targeting of XJB-5-131 attenuates or improves pathophysiology in HdhQ150 animals with well-developed disease phenotypes.

Polyzos A, Holt A, Brown C, Cosme C, Wipf P, Gomez-Marin A, Castro MR, Ayala-Peña S, McMurray CT.

Hum Mol Genet. 2016 May 1;25(9):1792-802. doi: 10.1093/hmg/ddw051. Epub 2016 Feb 21.


2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition.

Banerjee S, Bartesaghi A, Merk A, Rao P, Bulfer SL, Yan Y, Green N, Mroczkowski B, Neitz RJ, Wipf P, Falconieri V, Deshaies RJ, Milne JL, Huryn D, Arkin M, Subramaniam S.

Science. 2016 Feb 19;351(6275):871-5. doi: 10.1126/science.aad7974. Epub 2016 Jan 28.


Intraoral Mitochondrial-Targeted GS-Nitroxide, JP4-039, Radioprotects Normal Tissue in Tumor-Bearing Radiosensitive Fancd2(-/-) (C57BL/6) Mice.

Shinde A, Berhane H, Rhieu BH, Kalash R, Xu K, Goff J, Epperly MW, Franicola D, Zhang X, Dixon T, Shields D, Wang H, Wipf P, Parmar K, Guinan E, Kagan V, Tyurin V, Ferris RL, Zhang X, Li S, Greenberger JS.

Radiat Res. 2016 Feb;185(2):134-50. doi: 10.1667/RR14035.1. Epub 2016 Jan 20.


Antioxidant Approaches to Management of Ionizing Irradiation Injury.

Greenberger J, Kagan V, Bayir H, Wipf P, Epperly M.

Antioxidants (Basel). 2015 Jan 23;4(1):82-101. doi: 10.3390/antiox4010082.


Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97.

Alverez C, Arkin MR, Bulfer SL, Colombo R, Kovaliov M, LaPorte MG, Lim C, Liang M, Moore WJ, Neitz RJ, Yan Y, Yue Z, Huryn DM, Wipf P.

ACS Med Chem Lett. 2015 Oct 23;6(12):1225-30. doi: 10.1021/acsmedchemlett.5b00364. eCollection 2015 Dec 10.


Discovery and Characterization of a Biologically Active Non-ATP-Competitive p38 MAP Kinase Inhibitor.

Wilson BA, Alam MS, Guszczynski T, Jakob M, Shenoy SR, Mitchell CA, Goncharova EI, Evans JR, Wipf P, Liu G, Ashwell JD, O'Keefe BR.

J Biomol Screen. 2016 Mar;21(3):277-89. doi: 10.1177/1087057115615518. Epub 2015 Nov 4.


Bis-cyclopropane analog of disorazole C1 is a microtubule-destabilizing agent active in ABCB1-overexpressing human colon cancer cells.

Wu S, Guo Z, Hopkins CD, Wei N, Chu E, Wipf P, Schmitz JC.

Oncotarget. 2015 Dec 1;6(38):40866-79. doi: 10.18632/oncotarget.5885.


Mitochondria-targeted antioxidant preserves contractile properties and mitochondrial function of skeletal muscle in aged rats.

Javadov S, Jang S, Rodriguez-Reyes N, Rodriguez-Zayas AE, Soto Hernandez J, Krainz T, Wipf P, Frontera W.

Oncotarget. 2015 Nov 24;6(37):39469-81. doi: 10.18632/oncotarget.5783.


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 of anti-inflammatory α-and β-linked acetamidopyranosides as inhibitors of toll-like receptor 4 (TLR4).

Wipf P, Eyer BR, Yamaguchi Y, Zhang F, Neal MD, Sodhi CP, Good M, Branca M, Prindle T Jr, Lu P, Brodsky JL, Hackam DJ.

Tetrahedron Lett. 2015 Jun 3;56(23):3097-3100.


Mitochondrial targeted β-lapachone induces mitochondrial dysfunction and catastrophic vacuolization in cancer cells.

Ma J, Lim C, Sacher JR, Van Houten B, Qian W, Wipf P.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4828-33. doi: 10.1016/j.bmcl.2015.06.073. Epub 2015 Jun 26.

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