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Items: 27


PTPRT epigenetic silencing defines lung cancer with STAT3 activation and can direct STAT3 targeted therapies.

Sen M, Kindsfather A, Danilova L, Zhang F, Colombo R, LaPorte MG, Kurland BF, Huryn DM, Wipf P, Herman JG.

Epigenetics. 2019 Oct 13:1-14. doi: 10.1080/15592294.2019.1676597. [Epub ahead of print]


Optimization of Phenyl Indole Inhibitors of the AAA+ ATPase p97.

LaPorte MG, Burnett JC, Colombo R, Bulfer SL, Alverez C, Chou TF, Neitz RJ, Green N, Moore WJ, Yue Z, Li S, Arkin MR, Wipf P, Huryn DM.

ACS Med Chem Lett. 2018 Sep 18;9(11):1075-1081. doi: 10.1021/acsmedchemlett.8b00372. eCollection 2018 Nov 8.


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.


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.


Electrophilic Oxidation and [1,2]-Rearrangement of the Biindole Core of Birinapant.

Deng Y, Haimowitz T, LaPorte MG, Rippin SR, Alexander MD, Kumar PT, Hendi MS, Lee YH, Condon SM.

ACS Med Chem Lett. 2016 Jan 9;7(3):318-23. doi: 10.1021/acsmedchemlett.5b00461. eCollection 2016 Mar 10.


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.


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.


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.


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.


Birinapant, a smac-mimetic with improved tolerability for the treatment of solid tumors and hematological malignancies.

Condon SM, Mitsuuchi Y, Deng Y, LaPorte MG, Rippin SR, Haimowitz T, Alexander MD, Kumar PT, Hendi MS, Lee YH, Benetatos CA, Yu G, Kapoor GS, Neiman E, Seipel ME, Burns JM, Graham MA, McKinlay MA, Li X, Wang J, Shi Y, Feltham R, Bettjeman B, Cumming MH, Vince JE, Khan N, Silke J, Day CL, Chunduru SK.

J Med Chem. 2014 May 8;57(9):3666-77. doi: 10.1021/jm500176w. Epub 2014 Apr 15.


Birinapant (TL32711), a bivalent SMAC mimetic, targets TRAF2-associated cIAPs, abrogates TNF-induced NF-κB activation, and is active in patient-derived xenograft models.

Benetatos CA, Mitsuuchi Y, Burns JM, Neiman EM, Condon SM, Yu G, Seipel ME, Kapoor GS, Laporte MG, Rippin SR, Deng Y, Hendi MS, Tirunahari PK, Lee YH, Haimowitz T, Alexander MD, Graham MA, Weng D, Shi Y, McKinlay MA, Chunduru SK.

Mol Cancer Ther. 2014 Apr;13(4):867-79. doi: 10.1158/1535-7163.MCT-13-0798. Epub 2014 Feb 21. Erratum in: Mol Cancer Ther. 2014 Sep;13(9):2246-7. Dosage error in article text.


Radical [3 + 2]-annulation of divinylcyclopropanes: rapid synthesis of complex meloscine analogs.

Zhang H, Jeon KO, Hay EB, Geib SJ, Curran DP, LaPorte MG.

Org Lett. 2014 Jan 3;16(1):94-7. doi: 10.1021/ol403078e. Epub 2013 Dec 6.


Condensation reactions of guanidines with bis-electrophiles: Formation of highly nitrogenous heterocycles.

Arnold DM, Laporte MG, Anderson SM, Wipf P.

Tetrahedron. 2013 Sep 9;69(36):7719-7731.


Construction of a spirooxindole amide library through nitrile hydrozirconation-acylation-cyclization cascade.

LaPorte MG, Tsegay S, Hong KB, Lu C, Fang C, Wang L, Xie XQ, Floreancig PE.

ACS Comb Sci. 2013 Jul 8;15(7):344-9. doi: 10.1021/co4000387. Epub 2013 Jun 26.


Synthesis and in silico screening of a library of β-carboline-containing compounds.

Brummond KM, Goodell JR, Laporte MG, Wang L, Xie XQ.

Beilstein J Org Chem. 2012;8:1048-58. Epub 2012 Jul 10.


The discovery and structure-activity relationships of pyrano[3,4-b]indole-based inhibitors of hepatitis C virus NS5B polymerase.

Jackson RW, LaPorte MG, Herbertz T, Draper TL, Gaboury JA, Rippin SR, Patel R, Chunduru SK, Benetatos CA, Young DC, Burns CJ, Condon SM.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3227-31. doi: 10.1016/j.bmcl.2011.04.052. Epub 2011 Apr 21.


Diversity-oriented synthesis of a library of substituted tetrahydropyrones using oxidative carbon-hydrogen bond activation and click chemistry.

Zaware N, Laporte MG, Farid R, Liu L, Wipf P, Floreancig PE.

Molecules. 2011 May 2;16(5):3648-62. doi: 10.3390/molecules16053648.


Chemical methodology as a source of small-molecule checkpoint inhibitors and heat shock protein 70 (Hsp70) modulators.

Huryn DM, Brodsky JL, Brummond KM, Chambers PG, Eyer B, Ireland AW, Kawasumi M, Laporte MG, Lloyd K, Manteau B, Nghiem P, Quade B, Seguin SP, Wipf P.

Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6757-62. doi: 10.1073/pnas.1015251108. Epub 2011 Apr 18.


The discovery and structure-activity relationships of pyrano[3,4-b]indole based inhibitors of hepatitis C virus NS5B polymerase.

LaPorte MG, Draper TL, Miller LE, Blackledge CW, Leister LK, Amparo E, Hussey AR, Young DC, Chunduru SK, Benetatos CA, Rhodes G, Gopalsamy A, Herbertz T, Burns CJ, Condon SM.

Bioorg Med Chem Lett. 2010 May 1;20(9):2968-73. doi: 10.1016/j.bmcl.2010.03.002. Epub 2010 Mar 6.


The discovery of pyrano[3,4-b]indole-based allosteric inhibitors of HCV NS5B polymerase with in vivo activity.

Laporte MG, Jackson RW, Draper TL, Gaboury JA, Galie K, Herbertz T, Hussey AR, Rippin SR, Benetatos CA, Chunduru SK, Christensen JS, Coburn GA, Rizzo CJ, Rhodes G, O'Connell J, Howe AY, Mansour TS, Collett MS, Pevear DC, Young DC, Gao T, Tyrrell DL, Kneteman NM, Burns CJ, Condon SM.

ChemMedChem. 2008 Oct;3(10):1508-15. doi: 10.1002/cmdc.200800168. No abstract available.


Tetrahydrobenzothiophene inhibitors of hepatitis C virus NS5B polymerase.

Laporte MG, Lessen TA, Leister L, Cebzanov D, Amparo E, Faust C, Ortlip D, Bailey TR, Nitz TJ, Chunduru SK, Young DC, Burns CJ.

Bioorg Med Chem Lett. 2006 Jan 1;16(1):100-3. Epub 2005 Nov 2.


Total syntheses of the Securinega alkaloids (+)-14,15-dihydronorsecurinine, (-)-norsecurinine, and phyllanthine.

Han G, LaPorte MG, Folmer JJ, Werner KM, Weinreb SM.

J Org Chem. 2000 Oct 6;65(20):6293-306.


A New Enantioselective Approach to Total Synthesis of the Securinega Alkaloids: Application to (-)-Norsecurinine and Phyllanthine.

Han G, LaPorte MG, Folmer JJ, Werner KM, Weinreb SM.

Angew Chem Int Ed Engl. 2000 Jan;39(1):237-240.


[Types of canalar neuralgia: value and technics of local injections].

Laporte MG.

Bord Med. 1970 Oct;3(10):2442 passim. French. No abstract available.


[Procedure to follow in essential cervico-brachial neuralgia].

Laporte MG.

Bord Med. 1970 Jun;3(6):1683-6. French. No abstract available.


[Procedure to follow in case of lumbago].

Laporte MG.

Bord Med. 1970 Apr;3(4):1111-2 passim. French. No abstract available.


[Treatment of osteoporosis].

Laporte MG.

Bord Med. 1970 Jan;3(1):187-8 passim. French. No abstract available.


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